Roger L Papke

Roger L Papke, Ph.D.

PROFESSOR

Department: MD-PHARMACOLOGY / THERAPEUTICS
Business Phone: (352) 392-4712
Business Email: rlpapke@ufl.edu

Accomplishments

Exemplary Teacher
2016 · UF College of Medicine
Co-recipient of R&D 100
2004 · R&D 100 Conference
Top Ten Basic Science Faculty
2002 · UF College of Medicine

Research Profile

The Papke Lab studies the physiology, pharmacology, and biophysics of neurotransmitter receptors with a special emphasis on the function of nicotinic acetylcholine receptors in the brain. These are the receptors that mediate the effects of nicotine on human behavior. The lab studies how these neuronal nicotinic acetylcholine receptors function as ligand-gated ion channels, identifying parts of the molecule that are involved with the binding of neurotransmitter and the conformational change associated with receptor activation. The lab is also characterizing the selectivity of experimental nicotinic agonists for specific receptor subtypes in the brain. With this understanding, they hope to identify the mechanisms through which nicotine-like substances may alleviate some of the learning and memory impairments in animal models of dementia. The ongoing clinical development of new experimental drugs may lead to novel therapeutics for the treatment of Alzheimer’s disease.

Areas of Interest
  • Nicotine Addiction
  • Smoking Cessation

Publications

2021
Nicotine: Understanding the big picture while also studying the details.
Neuropharmacology. 196 [DOI] 10.1016/j.neuropharm.2021.108715. [PMID] 34271018.
2021
Stable desensitization of α7 nicotinic acetylcholine receptors by NS6740 requires interaction with S36 in the orthosteric agonist binding site.
European journal of pharmacology. 905 [DOI] 10.1016/j.ejphar.2021.174179. [PMID] 34004208.
2021
Sulfonium Ligands of the α7 nAChR.
Molecules (Basel, Switzerland). 26(18) [DOI] 10.3390/molecules26185643. [PMID] 34577114.
2021
The Allosteric Activation of α7 nAChR by α-Conotoxin MrIC Is Modified by Mutations at the Vestibular Site.
Toxins. 13(8) [DOI] 10.3390/toxins13080555. [PMID] 34437426.
2021
Therapeutic Targeting of α7 Nicotinic Acetylcholine Receptors.
Pharmacological reviews. 73(3):1118-1149 [DOI] 10.1124/pharmrev.120.000097. [PMID] 34301823.
2020
A silent agonist of α7 nicotinic acetylcholine receptors modulates inflammation ex vivo and attenuates EAE.
Brain, behavior, and immunity. 87:286-300 [DOI] 10.1016/j.bbi.2019.12.014. [PMID] 31874200.
2020
Allosterically Potentiated α7 Nicotinic Acetylcholine Receptors: Reduced Calcium Permeability and Current-Independent Control of Intracellular Calcium.
Molecular pharmacology. 98(6):695-709 [DOI] 10.1124/molpharm.120.000012. [PMID] 33020143.
2020
Betel Nut (areca) and Smokeless Tobacco Use in Myanmar.
Substance use & misuse. 55(9):1385-1394 [DOI] 10.1080/10826084.2019.1624774. [PMID] 31220988.
2020
Betel Quid, Health, and Addiction.
Substance use & misuse. 55(9):1528-1532 [DOI] 10.1080/10826084.2019.1666147. [PMID] 32569542.
2020
Cholinergic Receptors and Addiction.
Current topics in behavioral neurosciences. 45:123-151 [DOI] 10.1007/7854_2020_139. [PMID] 32451953.
2020
Design, synthesis, and electrophysiological evaluation of NS6740 derivatives: Exploration of the structure-activity relationship for alpha7 nicotinic acetylcholine receptor silent activation.
European journal of medicinal chemistry. 205 [DOI] 10.1016/j.ejmech.2020.112669. [PMID] 32810771.
2020
Differing Activity Profiles of the Stereoisomers of 2,3,5,6TMP-TQS, a Putative Silent Allosteric Modulator of α7 nAChR.
Molecular pharmacology. 98(4):292-302 [DOI] 10.1124/mol.120.119958. [PMID] 32690627.
2020
Effects of α7 Nicotinic Acetylcholine Receptor Positive Allosteric Modulator on BDNF, NKCC1 and KCC2 Expression in the Hippocampus following Lipopolysaccharide-induced Allodynia and Hyperalgesia in a Mouse Model of Inflammatory Pain.
CNS & neurological disorders drug targets. [DOI] 10.2174/1871527319666201230102616. [PMID] 33380307.
2020
In Silico Modeling of the α7 Nicotinic Acetylcholine Receptor: New Pharmacological Challenges Associated with Multiple Modes of Signaling.
Mini reviews in medicinal chemistry. 20(10):841-864 [DOI] 10.2174/1389557520666200130105256. [PMID] 32000651.
2020
Nicotinic Acetylcholine Receptor Accessory Subunits Determine the Activity Profile of Epibatidine Derivatives.
Molecular pharmacology. 98(4):328-342 [DOI] 10.1124/molpharm.120.000037. [PMID] 32690626.
2020
Nicotinic acetylcholine receptors: Conventional and unconventional ligands and signaling.
Neuropharmacology. 168 [DOI] 10.1016/j.neuropharm.2020.108021. [PMID] 32146229.
2019
Allosteric Agonism of α7 Nicotinic Acetylcholine Receptors: Receptor Modulation Outside the Orthosteric Site.
Molecular pharmacology. 95(6):606-614 [DOI] 10.1124/mol.119.115758. [PMID] 30944209.
2019
Cracking the Betel Nut: Cholinergic Activity of Areca Alkaloids and Related Compounds.
Nicotine & tobacco research : official journal of the Society for Research on Nicotine and Tobacco. 21(6):805-812 [DOI] 10.1093/ntr/ntx187. [PMID] 29059390.
2019
Heteromeric Neuronal Nicotinic Acetylcholine Receptors with Mutant β Subunits Acquire Sensitivity to α7-Selective Positive Allosteric Modulators.
The Journal of pharmacology and experimental therapeutics. 370(2):252-268 [DOI] 10.1124/jpet.119.259499. [PMID] 31175218.
2019
Impact of modulation of the α7 nicotinic acetylcholine receptor on nicotine reward in the mouse conditioned place preference test.
Psychopharmacology. 236(12):3593-3599 [DOI] 10.1007/s00213-019-05331-y. [PMID] 31302720.
2019
Macroscopic and Microscopic Activation of α7 Nicotinic Acetylcholine Receptors by the Structurally Unrelated Allosteric Agonist-Positive Allosteric Modulators (ago-PAMs) B-973B and GAT107.
Molecular pharmacology. 95(1):43-61 [DOI] 10.1124/mol.118.113340. [PMID] 30348894.
2019
Synthesis, Pharmacological Characterization, and Structure-Activity Relationships of Noncanonical Selective Agonists for α7 nAChRs.
Journal of medicinal chemistry. 62(22):10376-10390 [DOI] 10.1021/acs.jmedchem.9b01467. [PMID] 31675224.
2019
The α7 nicotinic acetylcholine receptor positive allosteric modulator prevents lipopolysaccharide-induced allodynia, hyperalgesia and TNF-α in the hippocampus in mice.
Pharmacological reports : PR. 71(6):1168-1176 [DOI] 10.1016/j.pharep.2019.07.001. [PMID] 31655281.
2019
The α7 nicotinic receptor silent agonist R-47 prevents and reverses paclitaxel-induced peripheral neuropathy in mice without tolerance or altering nicotine reward and withdrawal.
Experimental neurology. 320 [DOI] 10.1016/j.expneurol.2019.113010. [PMID] 31299179.
2018
B-973, a Novel α7 nAChR Ago-PAM: Racemic and Asymmetric Synthesis, Electrophysiological Studies, and in Vivo Evaluation.
ACS medicinal chemistry letters. 9(11):1144-1148 [DOI] 10.1021/acsmedchemlett.8b00407. [PMID] 30429960.
2018
New Insights on Neuronal Nicotinic Acetylcholine Receptors as Targets for Pain and Inflammation: A Focus on α7 nAChRs.
Current neuropharmacology. 16(4):415-425 [DOI] 10.2174/1570159X15666170818102108. [PMID] 28820052.
2018
Novel 5-(quinuclidin-3-ylmethyl)-1,2,4-oxadiazoles to investigate the activation of the α7 nicotinic acetylcholine receptor subtype: Synthesis and electrophysiological evaluation.
European journal of medicinal chemistry. 160:207-228 [DOI] 10.1016/j.ejmech.2018.10.015. [PMID] 30342362.
2018
NS6740, an α7 nicotinic acetylcholine receptor silent agonist, disrupts hippocampal synaptic plasticity.
Neuroscience letters. 677:6-13 [DOI] 10.1016/j.neulet.2018.04.025. [PMID] 29679680.
2018
Persistent activation of α7 nicotinic ACh receptors associated with stable induction of different desensitized states.
British journal of pharmacology. 175(11):1838-1854 [DOI] 10.1111/bph.13851. [PMID] 28477386.
2018
Pharmacological modulation of the α7 nicotinic acetylcholine receptor in a mouse model of mecamylamine-precipitated nicotine withdrawal.
Psychopharmacology. 235(7):1897-1905 [DOI] 10.1007/s00213-018-4879-7. [PMID] 29549391.
2018
The Antinociceptive and Anti-Inflammatory Properties of the α7 nAChR Weak Partial Agonist p-CF3 N,N-diethyl-N’-phenylpiperazine.
The Journal of pharmacology and experimental therapeutics. 367(2):203-214 [DOI] 10.1124/jpet.118.249904. [PMID] 30111636.
2017
Anti-inflammatory Silent Agonists.
ACS medicinal chemistry letters. 8(10):989-991 [DOI] 10.1021/acsmedchemlett.7b00368. [PMID] 29057037.
2017
Design, synthesis, and biological activity of 5′-phenyl-1,2,5,6-tetrahydro-3,3′-bipyridine analogues as potential antagonists of nicotinic acetylcholine receptors.
Bioorganic & medicinal chemistry letters. 27(18):4350-4353 [DOI] 10.1016/j.bmcl.2017.08.025. [PMID] 28838693.
2017
Identification of α7 Nicotinic Acetylcholine Receptor Silent Agonists Based on the Spirocyclic Quinuclidine-Δ2 -Isoxazoline Scaffold: Synthesis and Electrophysiological Evaluation.
ChemMedChem. 12(16):1335-1348 [DOI] 10.1002/cmdc.201700162. [PMID] 28494140.
2017
Rabies virus modifies host behaviour through a snake-toxin like region of its glycoprotein that inhibits neurotransmitter receptors in the CNS.
Scientific reports. 7(1) [DOI] 10.1038/s41598-017-12726-4. [PMID] 28993633.
2017
Role of the α7 Nicotinic Acetylcholine Receptor and RIC-3 in the Cholinergic Anti-inflammatory Pathway.
Central nervous system agents in medicinal chemistry. 17(2):90-99 [DOI] 10.2174/1871524916666160829114533. [PMID] 27573666.
2017
Sulfonium as a Surrogate for Ammonium: A New α7 Nicotinic Acetylcholine Receptor Partial Agonist with Desensitizing Activity.
Journal of medicinal chemistry. 60(18):7928-7934 [DOI] 10.1021/acs.jmedchem.7b00875. [PMID] 28885019.
2017
The interaction between alpha 7 nicotinic acetylcholine receptor and nuclear peroxisome proliferator-activated receptor-α represents a new antinociceptive signaling pathway in mice
Experimental Neurology. 194-201 [DOI] 10.1016/j.expneurol.2017.06.014. [PMID] 28606623.
2017
The Interaction Between Alpha 7 Nicotinic Acetylcholine Receptor and Nuclear Peroxisome Proliferator-Activated Receptor-Alpha Represents a New Antinociceptive Signaling Pathway in Mice
Experimental Neurology. 295:194-201 [DOI] 10.1016/j.expneuro1.2017.06.014.
2017
The interaction between alpha 7 nicotinic acetylcholine receptor and nuclear peroxisome proliferator-activated receptor-α represents a new antinociceptive signaling pathway in mice.
Experimental neurology. 295:194-201 [DOI] 10.1016/j.expneurol.2017.06.014. [PMID] 28606623.
2017
The α7 nicotinic acetylcholine receptor positive allosteric modulator attenuates lipopolysaccharide-induced activation of hippocampal IκB and CD11b gene expression in mice.
Drug discoveries & therapeutics. 11(4):206-211 [DOI] 10.5582/ddt.2017.01038. [PMID] 28867753.
2016
Critical Molecular Determinants of α7 Nicotinic Acetylcholine Receptor Allosteric Activation: SEPARATION OF DIRECT ALLOSTERIC ACTIVATION AND POSITIVE ALLOSTERIC MODULATION.
The Journal of biological chemistry. 291(10):5049-67 [DOI] 10.1074/jbc.M115.692392. [PMID] 26742843.
2016
Dissection of N,N-diethyl-N’-phenylpiperazines as α7 nicotinic receptor silent agonists.
Bioorganic & medicinal chemistry. 24(2):286-93 [DOI] 10.1016/j.bmc.2015.12.017. [PMID] 26707847.
2016
Imaging of cerebral α4β2* nicotinic acetylcholine receptors with (-)-[(18)F]Flubatine PET: Implementation of bolus plus constant infusion and sensitivity to acetylcholine in human brain.
NeuroImage. 141:71-80 [DOI] 10.1016/j.neuroimage.2016.07.026. [PMID] 27426839.
2016
The α7 nicotinic receptor dual allosteric agonist and positive allosteric modulator GAT107 reverses nociception in mouse models of inflammatory and neuropathic pain.
British journal of pharmacology. 173(16):2506-20 [DOI] 10.1111/bph.13528. [PMID] 27243753.
2015
Looking below the surface of nicotinic acetylcholine receptors.
Trends in pharmacological sciences. 36(8):514-23 [DOI] 10.1016/j.tips.2015.05.002. [PMID] 26067101.
2015
Nicotinic Activity of Arecoline, the Psychoactive Element of “Betel Nuts”, Suggests a Basis for Habitual Use and Anti-Inflammatory Activity.
PloS one. 10(10) [DOI] 10.1371/journal.pone.0140907. [PMID] 26488401.
2015
The analgesic-like properties of the alpha7 nAChR silent agonist NS6740 is associated with non-conducting conformations of the receptor.
Neuropharmacology. 91:34-42 [DOI] 10.1016/j.neuropharm.2014.12.002. [PMID] 25497451.
2015
The α7 nicotinic receptor agonist ABT-107 protects against nigrostriatal damage in rats with unilateral 6-hydroxydopamine lesions.
Experimental neurology. 263:277-84 [DOI] 10.1016/j.expneurol.2014.09.015. [PMID] 25261754.
2015
Two novel α7 nicotinic acetylcholine receptor ligands: in vitro properties and their efficacy in collagen-induced arthritis in mice.
PloS one. 10(1) [DOI] 10.1371/journal.pone.0116227. [PMID] 25617631.
2014
Discovery and optimization of Lu AF58801, a novel, selective and brain penetrant positive allosteric modulator of alpha-7 nicotinic acetylcholine receptors: attenuation of subchronic phencyclidine (PCP)-induced cognitive deficits in rats following oral administration.
Bioorganic & medicinal chemistry letters. 24(1):288-93 [DOI] 10.1016/j.bmcl.2013.11.022. [PMID] 24291041.
2014
Diverse strategies targeting α7 homomeric and α6β2* heteromeric nicotinic acetylcholine receptors for smoking cessation.
Annals of the New York Academy of Sciences. 1327:27-45 [DOI] 10.1111/nyas.12421. [PMID] 24730978.
2014
Merging old and new perspectives on nicotinic acetylcholine receptors.
Biochemical pharmacology. 89(1):1-11 [DOI] 10.1016/j.bcp.2014.01.029. [PMID] 24486571.
2014
Rare human nicotinic acetylcholine receptor α4 subunit (CHRNA4) variants affect expression and function of high-affinity nicotinic acetylcholine receptors.
The Journal of pharmacology and experimental therapeutics. 348(3):410-20 [DOI] 10.1124/jpet.113.209767. [PMID] 24385388.
2014
The activity of GAT107, an allosteric activator and positive modulator of α7 nicotinic acetylcholine receptors (nAChR), is regulated by aromatic amino acids that span the subunit interface.
The Journal of biological chemistry. 289(7):4515-31 [DOI] 10.1074/jbc.M113.524603. [PMID] 24362025.
2014
The cytisine derivatives, CC4 and CC26, reduce nicotine-induced conditioned place preference in zebrafish by acting on heteromeric neuronal nicotinic acetylcholine receptors.
Psychopharmacology. 231(24):4681-93 [DOI] 10.1007/s00213-014-3619-x. [PMID] 24862365.
2014
The minimal pharmacophore for silent agonism of the α7 nicotinic acetylcholine receptor.
The Journal of pharmacology and experimental therapeutics. 350(3):665-80 [DOI] 10.1124/jpet.114.215236. [PMID] 24990939.
2014
Varenicline and cytisine diminish the dysphoric-like state associated with spontaneous nicotine withdrawal in rats.
Neuropsychopharmacology : official publication of the American College of Neuropsychopharmacology. 39(2):455-65 [DOI] 10.1038/npp.2013.216. [PMID] 23966067.
2013
Differential modulation of brain nicotinic acetylcholine receptor function by cytisine, varenicline, and two novel bispidine compounds: emergent properties of a hybrid molecule.
The Journal of pharmacology and experimental therapeutics. 347(2):424-37 [DOI] 10.1124/jpet.113.206904. [PMID] 23959137.
2013
Discovery of Lu Af58801, a Novel, Selective and Brain Penetrant Positive Allosteric Modulator of Alpha-7 Nicotinic Acetylcholine Receptors: Attenuation of Subchronic Phencyclidine (Pcp)-Induced Cognitive Deficits in Rats Following Oral Administration
Biochemical Pharmacology. 86(8) [DOI] 10.1016/j.bcp.2013.08.046.
2013
Expeditious synthesis, enantiomeric resolution, and enantiomer functional characterization of (4-(4-bromophenyl)-3a,4,5,9b-tetrahydro-3H-cyclopenta[c]quinoline-8-sulfonamide (4BP-TQS): an allosteric agonist-positive allosteric modulator of α7 nicotinic acetylcholine receptors.
Journal of medicinal chemistry. 56(21):8943-7 [DOI] 10.1021/jm401267t. [PMID] 24090443.
2013
Multiple modes of α7 nAChR noncompetitive antagonism of control agonist-evoked and allosterically enhanced currents.
Molecular pharmacology. 84(3):459-75 [DOI] 10.1124/mol.113.086462. [PMID] 23839567.
2013
Point-to-point ligand-receptor interactions across the subunit interface modulate the induction and stabilization of conformational states of alpha7 nAChR by benzylidene anabaseines.
Biochemical pharmacology. 85(6):817-28 [DOI] 10.1016/j.bcp.2013.01.010. [PMID] 23352650.
2013
Silent Agonists for Alpha7 Nicotinic Acetylcholine Receptor
. 246
2013
Similar activity of mecamylamine stereoisomers in vitro and in vivo.
European journal of pharmacology. 720(1-3):264-75 [DOI] 10.1016/j.ejphar.2013.10.018. [PMID] 24161916.
2013
Stereochemical Requirements Within the Tetrahydroquinoline Scaffold for the Positive Allosteric Modulation At Alpha7 Nicotinic Acetylcholine Receptors
. 246
2013
Synthesis and evaluation of a conditionally-silent agonist for the α7 nicotinic acetylcholine receptor.
Bioorganic & medicinal chemistry letters. 23(14):4145-9 [DOI] 10.1016/j.bmcl.2013.05.039. [PMID] 23746476.
2013
The 3,7-diazabicyclo[3.3.1]nonane scaffold for subtype selective nicotinic acetylcholine receptor (nAChR) ligands. Part 1: the influence of different hydrogen bond acceptor systems on alkyl and (hetero)aryl substituents.
Bioorganic & medicinal chemistry. 21(23):7283-308 [DOI] 10.1016/j.bmc.2013.09.059. [PMID] 24156938.
2013
The 3,7-diazabicyclo[3.3.1]nonane scaffold for subtype selective nicotinic acetylcholine receptor ligands. Part 2: carboxamide derivatives with different spacer motifs.
Bioorganic & medicinal chemistry. 21(23):7309-29 [DOI] 10.1016/j.bmc.2013.09.060. [PMID] 24145137.
2012
Intrinsically low open probability of α7 nicotinic acetylcholine receptors can be overcome by positive allosteric modulation and serum factors leading to the generation of excitotoxic currents at physiological temperatures.
Molecular pharmacology. 82(4):746-59 [PMID] 22828799.
View on: PubMed
2012
Potential state-selective hydrogen bond formation can modulate activation and desensitization of the α7 nicotinic acetylcholine receptor.
The Journal of biological chemistry. 287(26):21957-69 [DOI] 10.1074/jbc.M112.339796. [PMID] 22556416.
2012
The nicotinic acetylcholine receptors of zebrafish and an evaluation of pharmacological tools used for their study.
Biochemical pharmacology. 84(3):352-65 [DOI] 10.1016/j.bcp.2012.04.022. [PMID] 22580045.
2012
Use of an α3β4 nicotinic acetylcholine receptor subunit concatamer to characterize ganglionic receptor subtypes with specific subunit composition reveals species-specific pharmacologic properties.
Neuropharmacology. 63(4):538-46 [DOI] 10.1016/j.neuropharm.2012.04.035. [PMID] 22580377.
2012
α7β2 nicotinic acetylcholine receptors assemble, function, and are activated primarily via their α7-α7 interfaces.
Molecular pharmacology. 81(2):175-88 [DOI] 10.1124/mol.111.074088. [PMID] 22039094.
2011
Cysteine accessibility analysis of the human alpha7 nicotinic acetylcholine receptor ligand-binding domain identifies L119 as a gatekeeper.
Neuropharmacology. 60(1):159-71 [DOI] 10.1016/j.neuropharm.2010.07.014. [PMID] 20650284.
2011
Electrophysiological perspectives on the therapeutic use of nicotinic acetylcholine receptor partial agonists.
The Journal of pharmacology and experimental therapeutics. 337(2):367-79 [DOI] 10.1124/jpet.110.177485. [PMID] 21285282.
2011
Emerging Evidence for Multiple Binding Modes Leading To Different Functional States for Human Alpha7 Nachr
. 241
2011
Investigation of the molecular mechanism of the α7 nicotinic acetylcholine receptor positive allosteric modulator PNU-120596 provides evidence for two distinct desensitized states.
Molecular pharmacology. 80(6):1013-32 [DOI] 10.1124/mol.111.074302. [PMID] 21885620.
2011
Positive allosteric modulators as an approach to nicotinic acetylcholine receptor-targeted therapeutics: advantages and limitations.
Biochemical pharmacology. 82(8):915-30 [DOI] 10.1016/j.bcp.2011.05.001. [PMID] 21575610.
2011
Positive and Negative Cooperativity of Agonist and Allosteric Modulator Binding in Alpha7 Nachr: Looking for the Therapeutic Window
Biochemical Pharmacology. 82(8) [DOI] 10.1016/j.bcp.2011.07.024.
2011
The effective opening of nicotinic acetylcholine receptors with single agonist binding sites.
The Journal of general physiology. 137(4):369-84 [DOI] 10.1085/jgp.201010587. [PMID] 21444659.
2011
The Twin Drug Approach for Novel Nicotinic Acetylcholine Receptor (Nachr) Ligands: Synthesis and Structure-Affinity Relationships
Biochemical Pharmacology. 82(8) [DOI] 10.1016/j.bcp.2011.07.016.
2010
Activation and inhibition of mouse muscle and neuronal nicotinic acetylcholine receptors expressed in Xenopus oocytes.
The Journal of pharmacology and experimental therapeutics. 333(2):501-18 [DOI] 10.1124/jpet.109.164566. [PMID] 20100906.
2010
alpha4beta2 Nicotinic acetylcholine receptors, willing if able.
British journal of pharmacology. 160(8):1903-5 [DOI] 10.1111/j.1476-5381.2010.00868.x. [PMID] 20649588.
2010
Biochemical and functional properties of distinct nicotinic acetylcholine receptors in the superior cervical ganglion of mice with targeted deletions of nAChR subunit genes.
The European journal of neuroscience. 31(6):978-93 [DOI] 10.1111/j.1460-9568.2010.07133.x. [PMID] 20377613.
2010
Discovery of novel alpha7 nicotinic receptor antagonists.
Bioorganic & medicinal chemistry letters. 20(16):4825-30 [DOI] 10.1016/j.bmcl.2010.06.103. [PMID] 20638843.
2010
Tethered agonist analogs as site-specific probes for domains of the human α7 nicotinic acetylcholine receptor that differentially regulate activation and desensitization.
Molecular pharmacology. 78(6):1012-25 [DOI] 10.1124/mol.110.066662. [PMID] 20823218.
2010
Tricks of perspective: insights and limitations to the study of macroscopic currents for the analysis of nAChR activation and desensitization.
Journal of molecular neuroscience : MN. 40(1-2):77-86 [DOI] 10.1007/s12031-009-9261-0. [PMID] 19672724.
2010
Working with OpusXpress: methods for high volume oocyte experiments.
Methods (San Diego, Calif.). 51(1):121-33 [DOI] 10.1016/j.ymeth.2010.01.012. [PMID] 20085813.
2009
Activation and desensitization of nicotinic alpha7-type acetylcholine receptors by benzylidene anabaseines and nicotine.
The Journal of pharmacology and experimental therapeutics. 329(2):791-807 [DOI] 10.1124/jpet.108.150151. [PMID] 19223664.
2009
Atypical antipsychotics as noncompetitive inhibitors of alpha4beta2 and alpha7 neuronal nicotinic receptors.
Neuropharmacology. 57(2):183-91 [DOI] 10.1016/j.neuropharm.2009.05.003. [PMID] 19481556.
2009
Cytisine-based nicotinic partial agonists as novel antidepressant compounds.
The Journal of pharmacology and experimental therapeutics. 329(1):377-86 [DOI] 10.1124/jpet.108.149609. [PMID] 19164465.
2009
Differential regulation of receptor activation and agonist selectivity by highly conserved tryptophans in the nicotinic acetylcholine receptor binding site.
The Journal of pharmacology and experimental therapeutics. 330(1):40-53 [DOI] 10.1124/jpet.109.151225. [PMID] 19339660.
2009
High Throughput Electrophysiology With Xenopus Oocytes
Combinatorial Chemistry and High Throughput Screening. 12:38-50
2009
High throughput electrophysiology with Xenopus oocytes.
Combinatorial chemistry & high throughput screening. 12(1):38-50 [PMID] 19149490.
View on: PubMed
2009
Positive modulation of alpha7 nAChR responses in rat hippocampal interneurons to full agonists and the alpha7-selective partial agonists, 4OH-GTS-21 and S 24795.
Neuropharmacology. 56(4):821-30 [PMID] 19705574.
View on: PubMed
2009
Selective inhibition of acetylcholine-evoked responses of alpha7 neuronal nicotinic acetylcholine receptors by novel tris- and tetrakis-azaaromatic quaternary ammonium antagonists.
Molecular pharmacology. 76(3):652-66 [DOI] 10.1124/mol.109.056176. [PMID] 19556356.
2009
Synthesis of H-bonding probes of alpha7 nAChR agonist selectivity.
Bioorganic & medicinal chemistry letters. 19(2):474-6 [DOI] 10.1016/j.bmcl.2008.11.044. [PMID] 19081250.
2009
TC-5619: an alpha7 neuronal nicotinic receptor-selective agonist that demonstrates efficacy in animal models of the positive and negative symptoms and cognitive dysfunction of schizophrenia.
Biochemical pharmacology. 78(7):803-12 [DOI] 10.1016/j.bcp.2009.05.030. [PMID] 19482012.
2008
Extending the analysis of nicotinic receptor antagonists with the study of alpha6 nicotinic receptor subunit chimeras.
Neuropharmacology. 54(8):1189-200 [DOI] 10.1016/j.neuropharm.2008.03.010. [PMID] 18448138.
2008
Modeling binding modes of alpha7 nicotinic acetylcholine receptor with ligands: the roles of Gln117 and other residues of the receptor in agonist binding.
Journal of medicinal chemistry. 51(20):6293-302 [DOI] 10.1021/jm800607u. [PMID] 18826295.
2008
Modulation of spontaneous hippocampal synaptic events with 5-hydroxyindole, 4OH-GTS-21, and rAAV-mediated alpha7 nicotinic receptor gene transfer.
Brain research. 1203:51-60 [DOI] 10.1016/j.brainres.2008.02.011. [PMID] 18321476.
2008
Multiple pharmacophores for the selective activation of nicotinic alpha7-type acetylcholine receptors.
Molecular pharmacology. 74(6):1496-511 [DOI] 10.1124/mol.108.048892. [PMID] 18768388.
2008
Neuronal nicotinic receptors as brain targets for pharmacotherapy of drug addiction.
CNS & neurological disorders drug targets. 7(5):422-41 [PMID] 19128201.
View on: PubMed
2008
PATE gene clusters code for multiple, secreted TFP/Ly-6/uPAR proteins that are expressed in reproductive and neuron-rich tissues and possess neuromodulatory activity.
The Journal of biological chemistry. 283(24):16928-39 [DOI] 10.1074/jbc.M801454200. [PMID] 18387948.
2008
Region-specific effects of N,N’-dodecane-1,12-diyl-bis-3-picolinium dibromide on nicotine-induced increase in extracellular dopamine in vivo.
British journal of pharmacology. 153(4):792-804 [PMID] 18059317.
View on: PubMed
2007
alpha7 Nicotinic receptor gene delivery into mouse hippocampal neurons leads to functional receptor expression, improved spatial memory-related performance, and tau hyperphosphorylation.
Neuroscience. 145(1):314-22 [PMID] 17218065.
View on: PubMed
2007
Discovery of a novel nicotinic receptor antagonist for the treatment of nicotine addiction: 1-(3-Picolinium)-12-triethylammonium-dodecane dibromide (TMPD).
Biochemical pharmacology. 74(8):1271-82 [PMID] 17727820.
View on: PubMed
2007
Partial agonist and neuromodulatory activity of S 24795 for alpha7 nAChR responses of hippocampal interneurons.
Neuropharmacology. 53(1):134-44 [PMID] 17544457.
View on: PubMed
2007
Quinuclidines as selective agonists for alpha-7 nicotinic acetylcholine receptors.
Bioorganic & medicinal chemistry letters. 17(6):1520-2 [PMID] 17276680.
View on: PubMed
2007
Reversal of agonist selectivity by mutations of conserved amino acids in the binding site of nicotinic acetylcholine receptors.
The Journal of biological chemistry. 282(8):5899-909 [PMID] 17189260.
View on: PubMed
2007
The pharmacological activity of nicotine and nornicotine on nAChRs subtypes: relevance to nicotine dependence and drug discovery.
Journal of neurochemistry. 101(1):160-7 [PMID] 17241116.
View on: PubMed
2006
Estimation of both the potency and efficacy of alpha7 nAChR agonists from single-concentration responses.
Life sciences. 78(24):2812-9 [PMID] 16343553.
View on: PubMed
2005
An alpha7 nicotinic acetylcholine receptor gain-of-function mutant that retains pharmacological fidelity.
Molecular pharmacology. 68(6):1863-76 [PMID] 16186249.
View on: PubMed
2005
Functional central nicotinic acetylcholine receptor antagonism by systemic administration of Tinuvin 770 (BTMPS).
Current Alzheimer research. 2(2):141-7 [PMID] 15974911.
View on: PubMed
2005
In vivo characterization of a novel inhibitor of CNS nicotinic receptors.
European journal of pharmacology. 521(1-3):43-8 [PMID] 16181622.
View on: PubMed
2005
Medial septal/diagonal band cells express multiple functional nicotinic receptor subtypes that are correlated with firing frequency.
Neuroscience letters. 389(3):163-8 [PMID] 16112453.
View on: PubMed
2005
Molecular dissection of tropisetron, an alpha7 nicotinic acetylcholine receptor-selective partial agonist.
Neuroscience letters. 378(3):140-4 [PMID] 15781147.
View on: PubMed
2005
Multiple calcium channels and kinases mediate alpha7 nicotinic receptor neuroprotection in PC12 cells.
Journal of neurochemistry. 94(4):926-33 [PMID] 15969741.
View on: PubMed
2005
Rhesus monkey alpha7 nicotinic acetylcholine receptors: comparisons to human alpha7 receptors expressed in Xenopus oocytes.
European journal of pharmacology. 524(1-3):11-8 [PMID] 16266703.
View on: PubMed
2005
Septal innervation regulates the function of alpha7 nicotinic receptors in CA1 hippocampal interneurons.
Experimental neurology. 195(2):342-52 [PMID] 16000197.
View on: PubMed
2005
The characterization of a novel rigid nicotine analog with alpha7-selective nAChR agonist activity and modulation of agonist properties by boron inclusion.
Bioorganic & medicinal chemistry letters. 15(17):3874-80 [PMID] 16005216.
View on: PubMed
2005
The effects of subunit composition on the inhibition of nicotinic receptors by the amphipathic blocker 2,2,6,6-tetramethylpiperidin-4-yl heptanoate.
Molecular pharmacology. 67(6):1977-90 [PMID] 15761116.
View on: PubMed
2004
A single point mutation confers properties of the muscle-type nicotinic acetylcholine receptor to homomeric alpha7 receptors.
Molecular pharmacology. 66(1):169-77 [PMID] 15213309.
View on: PubMed
2004
Activity of alpha7-selective agonists at nicotinic and serotonin 5HT3 receptors expressed in Xenopus oocytes.
Bioorganic & medicinal chemistry letters. 14(8):1849-53 [PMID] 15050614.
View on: PubMed
2004
Effects at a distance in alpha 7 nAChR selective agonists: benzylidene substitutions that regulate potency and efficacy.
Neuropharmacology. 46(7):1023-38 [PMID] 15081799.
View on: PubMed
2004
Hydroxy metabolites of the Alzheimer’s drug candidate 3-[(2,4-dimethoxy)benzylidene]-anabaseine dihydrochloride (GTS-21): their molecular properties, interactions with brain nicotinic receptors, and brain penetration.
Molecular pharmacology. 65(1):56-67 [PMID] 14722237.
View on: PubMed
2004
Taurine-induced long-lasting potentiation in the rat hippocampus shows a partial dissociation from total hippocampal taurine content and independence from activation of known taurine transporters.
Journal of neurochemistry. 89(5):1195-205 [PMID] 15147512.
View on: PubMed
2004
The neuroprotective effect of 2-(3-pyridyl)-1-azabicyclo[3.2.2]nonane (TC-1698), a novel alpha7 ligand, is prevented through angiotensin II activation of a tyrosine phosphatase.
The Journal of pharmacology and experimental therapeutics. 309(1):16-27 [PMID] 14722323.
View on: PubMed
2004
The structural basis for GTS-21 selectivity between human and rat nicotinic alpha7 receptors.
Molecular pharmacology. 66(1):14-24 [PMID] 15213292.
View on: PubMed
2003
Modulation of inhibitory synaptic activity by a non-alpha4beta2, non-alpha7 subtype of nicotinic receptors in the substantia gelatinosa of adult rat spinal cord.
Pain. 101(1-2):13-23 [PMID] 12507696.
View on: PubMed
2003
Nicotinic receptors on local circuit neurons in dentate gyrus: a potential role in regulation of granule cell excitability.
Journal of neurophysiology. 89(6):3018-28 [PMID] 12611982.
View on: PubMed
2003
Regulation of neuronal function by choline and 4OH-GTS-21 through alpha 7 nicotinic receptors.
Journal of neurophysiology. 89(4):1797-806 [PMID] 12611953.
View on: PubMed
2002
Activation and inhibition of native neuronal alpha-bungarotoxin-sensitive nicotinic ACh receptors.
Brain research. 948(1-2):33-46 [PMID] 12383953.
View on: PubMed
2002
Comparative pharmacology of rat and human alpha7 nAChR conducted with net charge analysis.
British journal of pharmacology. 137(1):49-61 [PMID] 12183330.
View on: PubMed
2002
Enhanced inhibition of a mutant neuronal nicotinic acetylcholine receptor by agonists: protection of function by (E)-N-methyl-4-(3-pyridinyl)-3-butene-1-amine (TC-2403).
The Journal of pharmacology and experimental therapeutics. 301(2):765-73 [PMID] 11961083.
View on: PubMed
2001
2-(2-Piperidyl)- and 2-(2-pyrrolidyl)chromans as nicotine agonists: synthesis and preliminary pharmacological characterization.
Journal of medicinal chemistry. 44(26):4704-15 [PMID] 11741488.
View on: PubMed
2001
Analysis of mecamylamine stereoisomers on human nicotinic receptor subtypes.
The Journal of pharmacology and experimental therapeutics. 297(2):646-56 [PMID] 11303054.
View on: PubMed
2001
Inhibition of wild-type and mutant neuronal nicotinic acetylcholine receptors by local anesthetics.
Molecular pharmacology. 60(6):1365-74 [PMID] 11723244.
View on: PubMed
2000
alpha7 receptor-selective agonists and modes of alpha7 receptor activation.
European journal of pharmacology. 393(1-3):179-95 [PMID] 10771012.
View on: PubMed
2000
Subtype-selective inhibition of neuronal nicotinic acetylcholine receptors by cocaine is determined by the alpha4 and beta4 subunits.
Molecular pharmacology. 58(1):109-19 [PMID] 10860932.
View on: PubMed
2000
The activation and inhibition of human nicotinic acetylcholine receptor by RJR-2403 indicate a selectivity for the alpha4beta2 receptor subtype.
Journal of neurochemistry. 75(1):204-16 [PMID] 10854263.
View on: PubMed
1999
Antagonist activities of mecamylamine and nicotine show reciprocal dependence on beta subunit sequence in the second transmembrane domain.
British journal of pharmacology. 127(6):1337-48 [PMID] 10455283.
View on: PubMed
1999
Characterization of the neuroprotective and toxic effects of alpha7 nicotinic receptor activation in PC12 cells.
Brain research. 830(2):218-25 [PMID] 10366678.
View on: PubMed
1999
Lithium modulates desensitization of the glutamate receptor subtype gluR3 in Xenopus oocytes.
Neuroscience letters. 277(3):153-6 [PMID] 10626836.
View on: PubMed
1999
Subtype-specific effects of lithium on glutamate receptor function.
Journal of neurophysiology. 81(4):1506-12 [PMID] 10200187.
View on: PubMed
1998
Analysis of 3-(4-hydroxy, 2-Methoxybenzylidene)anabaseine selectivity and activity at human and rat alpha-7 nicotinic receptors.
The Journal of pharmacology and experimental therapeutics. 287(3):918-25 [PMID] 9864273.
View on: PubMed
1998
Lithium homeostasis in Xenopus oocytes: implications for the study of signal transduction.
Life sciences. 63(19):1715-24 [PMID] 9806227.
View on: PubMed
1998
Neurobiology of lithium: an update.
The Journal of clinical psychiatry. 59 Suppl 6:37-47 [PMID] 9674936.
View on: PubMed
1998
Neuroprotective and memory-related actions of novel alpha-7 nicotinic agents with different mixed agonist/antagonist properties.
The Journal of pharmacology and experimental therapeutics. 284(3):1026-32 [PMID] 9495863.
View on: PubMed
1998
Sensitivity to voltage-independent inhibition determined by pore-lining region of the acetylcholine receptor.
Biophysical journal. 74(5):2306-17 [PMID] 9591658.
View on: PubMed
1998
Synapse-specific accumulation of lithium in intracellular microdomains: a model for uncoupling coincidence detection in the brain.
Synapse (New York, N.Y.). 28(4):271-9 [PMID] 9517835.
View on: PubMed
1998
The correction of alpha7 nicotinic acetylcholine receptor concentration-response relationships in Xenopus oocytes.
Neuroscience letters. 256(3):163-6 [PMID] 9855365.
View on: PubMed
1997
3-[2,4-Dimethoxybenzylidene]anabaseine (DMXB) selectively activates rat alpha7 receptors and improves memory-related behaviors in a mecamylamine-sensitive manner.
Brain research. 768(1-2):49-56 [PMID] 9369300.
View on: PubMed
1997
Activation and inhibition of rat neuronal nicotinic receptors by ABT-418.
British journal of pharmacology. 120(3):429-38 [PMID] 9031746.
View on: PubMed
1997
Anabaseine is a potent agonist on muscle and neuronal alpha-bungarotoxin-sensitive nicotinic receptors.
The Journal of pharmacology and experimental therapeutics. 283(3):979-92 [PMID] 9399967.
View on: PubMed
1996
An evaluation of neuronal nicotinic acetylcholine receptor activation by quaternary nitrogen compounds indicates that choline is selective for the alpha 7 subtype.
Neuroscience letters. 213(3):201-4 [PMID] 8873149.
View on: PubMed
1996
Differentiation of ionic currents in CNS progenitor cells: dependence upon substrate attachment and epidermal growth factor.
Experimental neurology. 140(2):206-17 [PMID] 8690063.
View on: PubMed
1996
Muscle-type nicotinic acetylcholine receptor delta subunit determines sensitivity to noncompetitive inhibitors, while gamma subunit regulates divalent permeability.
Neuropharmacology. 35(11):1547-56 [PMID] 9025102.
View on: PubMed
1995
Characterization of a series of anabaseine-derived compounds reveals that the 3-(4)-dimethylaminocinnamylidine derivative is a selective agonist at neuronal nicotinic alpha 7/125I-alpha-bungarotoxin receptor subtypes.
Molecular pharmacology. 47(1):164-71 [PMID] 7838125.
View on: PubMed
1994
A novel nicotinic agonist facilitates induction of long-term potentiation in the rat hippocampus.
Neuroscience letters. 168(1-2):130-4 [PMID] 8028765.
View on: PubMed
1994
Inhibition of nicotinic acetylcholine receptors by bis (2,2,6,6-tetramethyl- 4-piperidinyl) sebacate (Tinuvin 770), an additive to medical plastics.
The Journal of pharmacology and experimental therapeutics. 268(2):718-26 [PMID] 8113983.
View on: PubMed
1994
Partial agonist properties of cytisine on neuronal nicotinic receptors containing the beta 2 subunit.
Molecular pharmacology. 45(1):142-9 [PMID] 8302273.
View on: PubMed
1993
The amino terminal half of the nicotinic beta-subunit extracellular domain regulates the kinetics of inhibition by neuronal bungarotoxin.
Proceedings. Biological sciences. 252(1334):141-8 [PMID] 8391703.
View on: PubMed
1993
The kinetic properties of neuronal nicotinic receptors: genetic basis of functional diversity.
Progress in neurobiology. 41(4):509-31 [PMID] 7692467.
View on: PubMed
1991
Brain nicotinic receptor genes.
NIDA research monograph. 111:3-23 [PMID] 1775184.
View on: PubMed
1991
Identification of cultured cells expressing ligand-gated cationic channels.
Protein expression and purification. 2(2-3):108-16 [PMID] 1726559.
View on: PubMed
1991
The nicotinic receptor genes.
Clinical neuropharmacology. 14 Suppl 1:S45-61 [PMID] 1913709.
View on: PubMed
1991
The role of the beta 4-subunit in determining the kinetic properties of rat neuronal nicotinic acetylcholine alpha 3-receptors.
The Journal of physiology. 440:95-112 [PMID] 1725184.
View on: PubMed
1990
The brain nicotinic acetylcholine receptor gene family.
Progress in brain research. 86:195-203 [PMID] 2087557.
View on: PubMed
1989
Characterization of nicotinic acetylcholine receptor channels of the TE671 human medulloblastoma clonal line.
Neuroscience letters. 96(2):207-12 [PMID] 2467233.
View on: PubMed
1989
Mechanisms of noncompetitive inhibition of acetylcholine-induced single-channel currents.
The Journal of general physiology. 93(5):785-811 [PMID] 2472461.
View on: PubMed
1989
Single-channel currents of rat neuronal nicotinic acetylcholine receptors expressed in Xenopus oocytes.
Neuron. 3(5):589-96 [PMID] 2484342.
View on: PubMed
1988
Relationships of agonist properties to the single channel kinetics of nicotinic acetylcholine receptors.
Biophysical journal. 53(1):1-10 [PMID] 2449251.
View on: PubMed
1986
Effects of pineal factors on the action potentials of sympathetic neurons.
Cellular and molecular neurobiology. 6(4):381-95 [PMID] 3548991.
View on: PubMed

Patents

Published April 2018
Nicotinic Acetylcholine Receptor Silent Agonists
#US-2018-0298002-A1
Issued January 2016
Therapies to Improve Smoking Cessation in Neuropsychiatric and Depressed Patients
#9,233,109
Issued March 2015
Compositions and Methods for Selective Inhibition of Nicotine Acetylcholine Receptors (DIV of 10282
#8,980,923
Published October 2009
Use of a Novel a7 nAChR Antagonist to Treat Cancer and AIDs
#2010-0179186
Issued May 2009
Compositions and Methods for Selective Inhibition of Nicotine Acetylcholine Receptors
#7,531,555
Published November 2008
Selective Inhibitors of Neuronal Nicontic Acetylcholine Receptors(DIV)
#US-2009-0062339-A1
Issued February 2005
Compositions and Methods for Treatment of Neurological Disorders
#6,852,741
Issued November 1999
Cinnamylidene Anabaseine Compounds For Brain Disorders
#5,977,144

Teaching Profile

Courses Taught
2020-2021
IDH2930 (Un)common read
2018-2021
GMS6560 Molecules to Man: Past, Present and Future Therapeutic Strategies for Disease
2019-2021
GMS6520 Medical Pharmacology and Therapeutics I: The Nervous System
2020-2021
PAS5026 Pharmacotherapeu 2
2015-2016,2018-2021,2020-2021
GMS6009 Principles of Drug Action and Therapeutics
2006-2012,2014-2020
GMS6592 Ion Channels Journal Club: Pharmacology, Biophysics, and Neuroscience of Excitable Membranes
2011-2021
DEN6262 Prin of Pharmacology
2009,2011-2018,2018-2019
GMS6052 Ion Channels of Excitable Membranes
2019
GMS6705 Functional Human Neuroanatomy
2018
GMS7980 Research for Doctoral Dissertation
2014,2016
MDU4002 Introduction to Medical Science Seminar 2
2013-2014
BMS6031 Foundations of Med
2014
GMS6023 Principles of Neuroscience III: Molecular Neuropharmacology and its Clinical Application
2006
PHA4904 Pharmacology Research
2021
GMS6552 Cell Signaling & Therapeutics

Contact Details

Phones:
Business:
(352) 392-4712
Emails:
Business:
rlpapke@ufl.edu