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Localization of agonist and competitive antagonist binding sites on nicotinic acetylcholine receptors
(Pergamon-Elsevier Science Ltd, 2000-06-01)
Identification of all residues involved in the recognition and binding of cholinergic ligands (e.g. agonists, competitive antagonists, and noncompetitive agonists) is a primary objective to understand which structural ...
Number and Locations of Agonist Binding Sites Required to Activate Homomeric Cys-Loop Receptors
(Society for Neuroscience, 2009)
Stoichiometry for activation of neuronal alpha7 nicotinic receptors
(National Academy of Sciences, 2013-12)
Neuronal α7 nicotinic receptors elicit rapid cation influx in response to acetylcholine (ACh) or its hydrolysis product choline. They contribute to cognition, synaptic plasticity, and neuroprotection and have been implicated ...
Non-equivalent ligand selectivity of agonist sites in (α4β2) 2α4 nicotinic acetylcholine receptors: A key determinant of agonist efficacy
(American Society for Biochemistry and Molecular Biology Inc., 2014)
The α4β2 nicotinic acetylcholine receptor (nAChR) is the most abundant nAChR type in the brain, and this receptor type exists in alternate (α4β2)2α4 and (α4β2)2β2 forms, which are activated by agonists with strikingly ...
Molecular modeling of salsolinol, a full Gi protein agonist of the μ-opioid receptor, within the receptor binding site
(Blackwell Publishing Ltd, 2019)
(R/S)-Salsolinol is a full agonist of the μ-opioid receptor (μOR) Gi protein pathway via its (S)-enantiomer and is functionally selective as it does not promote β-arrestin recruitment. Compared to (S)-salsolinol, the ...
Tiotidine, a histamine H2 receptor inverse agonist that binds with high affinity to an inactive G-protein-coupled form of the receptor. Experimental support for the cubic ternary complex model.
(American Society for Pharmacology and Experimental Therapeutics, 2003-08-01)
Knowing the importance for research and pharmacological uses of proper ligand classification into agonists, inverse agonists, and antagonists, the aim of this work was to study the behavior of tiotidine, a controversial ...