High-Affinity Agonist Binding Correlates with Efficacy (Intrinsic Activity) at the Human Serotonin 5-HT2A and 5-HT2C Receptors: Evidence Favoring the Ternary Complex and Two-State Models of Agonist Action
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منابع مشابه
High-affinity agonist binding is not sufficient for agonist efficacy at 5-hydroxytryptamine2A receptors: evidence in favor of a modified ternary complex model.
In this study, the relationship between high-affinity agonist binding and second messenger production was examined at native and mutant 5-hydroxytryptamine2A receptors. At native 5-hydroxytryptamine2A receptors all agonists, with the exception of quipazine, discriminated between high- and low-affinity states of the receptor, as determined by analysis of competition binding assays. There was no ...
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The 5-hydroxytryptamine type 2A (5-HT(2A)) receptor and the 5-HT(2C) receptor are closely related members of the G-protein-coupled receptors activated by serotonin that share very similar pharmacological profiles and cellular signaling pathways. These receptors express a canonical class I PDZ ligand (SXV) at their C-terminal extremity. Here, we have identified proteins that interact with the PD...
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This study was designed to examine the effects of intracerebroventricular (ICV) injection of ketanserin(5-HT2a receptor antagonist) and SB242084 (5-HT2c receptor antagonist) on harmaline induced feeding anddrinking response in 24-h food-deprived (FD24) broiler cockerels. At first, guide cannula was surgicallyimplanted in the right lateral ventricle of chickens. In experiment 1, birds were injec...
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INTRODUCTION: 5-HT2A receptors are of significant clinical interest because of their potential involvement in mediating a variety of physiological functions, including platelet aggregation, thrombus formation, coronary artery spasm, vascular smooth muscle contraction, appetite, sleep, cognition, perception, mood, and other central nervous system functions. Different antagonists such as ketanser...
متن کاملSerotonin 5-HT2a and 5-HT2c receptors stimulate amyloid precursor protein ectodomain secretion.
Alzheimer's disease amyloid consists of amyloid beta-peptides (Abeta) derived from the larger precursor amyloid precursor protein (APP). Non-amyloidogenic APP processing involves regulated cleavage within the Abeta domain followed by secretion of the ectodomain (APPs). APPs secretion can be stimulated by muscarinic acetylcholine receptors coupled to phospholipases and kinases. To determine whet...
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ژورنال
عنوان ژورنال: Journal of Neurochemistry
سال: 2008
ISSN: 0022-3042
DOI: 10.1046/j.1471-4159.1999.0722127.x