Analysis of mecamylamine stereoisomers on human nicotinic receptor subtypes.
- R. Papke, P. Sanberg, R. Shytle
- Biology, ChemistryJournal of Pharmacology and Experimental…
- 1 May 2001
It is suggested that in chronic (i.e., therapeutic) application, S-(+)-mecamylamine might be preferable to R-(-)-micylamine in terms of equilibrium inactivation of neuronal receptors with decreased side effects associated with muscle-type receptors.
Positive allosteric modulators as an approach to nicotinic acetylcholine receptor-targeted therapeutics: advantages and limitations.
Investigation of the Molecular Mechanism of the α7 Nicotinic Acetylcholine Receptor Positive Allosteric Modulator PNU-120596 Provides Evidence for Two Distinct Desensitized States
The characterization of prolonged bursts of single-channel currents that occur with PNU-120596 provide a remarkable contrast to the behavior of the channels in the absence of the PAM, which shows a 100,000-fold increase in Popen compared with receptors in the nonpotentiated state.
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.
Analysis of 3-(4-hydroxy, 2-Methoxybenzylidene)anabaseine selectivity and activity at human and rat alpha-7 nicotinic receptors.
- E. Meyer, A. Kuryatov, V. Gerzanich, J. Lindstrom, R. Papke
- BiologyJournal of Pharmacology and Experimental…
- 1 December 1998
The studies suggest that the efficacy of GTS-21 in primates may depend on a pro-drug function, and 4OH-G TS-21 was protective in both human and rat cell lines, although GTS -21 was effective only in the latter.
An evaluation of neuronal nicotinic acetylcholine receptor activation by quaternary nitrogen compounds indicates that choline is selective for the α7 subtype
Merging old and new perspectives on nicotinic acetylcholine receptors.
- R. Papke
- Biology, ChemistryBiochemical Pharmacology
- 1 May 2014
A novel nicotinic agonist facilitates induction of long-term potentiation in the rat hippocampus
Characterization of the neuroprotective and toxic effects of α7 nicotinic receptor activation in PC12 cells
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…
- Dustin K. Williams, C. Peng, Matthew R. Kimbrell, R. Papke
- BiologyMolecular Pharmacology
- 1 October 2012
Despite reduced potentiation at body temperatures, use of type II positive allosteric modulators may put cells that naturally express high levels of α7 nAChRs, such as neurons in the hippocampus and hypothalamus, at risk.