Sustained treatment with a 5-HT2A receptor agonist causes functional desensitization and reductions in agonist-labeled 5-HT2A receptors despite increases in receptor protein levels in rats
نویسندگان
چکیده
منابع مشابه
Phosphorylation of Galpha11 protein contributes to agonist-induced desensitization of 5-HT2A receptor signaling.
Agonist treatment causes desensitization of many G protein-coupled receptor systems. Recent advances have delineated changes in receptors in the desensitization response; however, the role of G proteins remains unclear. We investigated the role of phosphorylation of Galpha q/11 proteins in agonist-induced desensitization of serotonin 2A (5-HT2A) receptors. In an embryonic rat cortical cell line...
متن کاملInverse Agonist Activity of several 5-HT2A Receptor Antagonists at the Constitutively Active Human 5- HT2A receptor
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 کاملIdentification of two serine residues essential for agonist-induced 5-HT2A receptor desensitization.
5-HT(2A) serotonin receptors represent the principal molecular targets for LSD-like hallucinogens and atypical antipsychotic drugs. It has been proposed that a dysregulation of 5-HT(2A) receptor-mediated signaling may contribute to the pathogenesis of schizophrenia and related diseases. A major mechanism for the attenuation of GPCR signaling following agonist activation typically involves the p...
متن کاملAntagonist functional selectivity: 5-HT2A serotonin receptor antagonists differentially regulate 5-HT2A receptor protein level in vivo.
Dysregulation of the 5-HT(2A) receptor is implicated in both the etiology and treatment of schizophrenia. Although the essential role of 5-HT(2A) receptors in atypical antipsychotic drug actions is widely accepted, the contribution of 5-HT(2A) down-regulation to their efficacy is not known. We hypothesized that down-regulation of cortical 5-HT(2A) receptors contributes to the therapeutic action...
متن کامل5-HT2A Serotonin Receptor Density in Adult Male Rats’ Hippocampus after Morphine-based Conditioned Place Preference
Introduction: A close interaction exists between the brain opioid and serotonin (5-HT) neurotransmitter systems. Brain neurotransmitter 5-HT plays an important role in the regulation of reward-related processing. However, a few studies have investigated the potential role of 5-HT2A receptors in this behavior. Therefore, the aim of the present study was to assess the influence of...
متن کاملذخیره در منابع من
با ذخیره ی این منبع در منابع من، دسترسی به آن را برای استفاده های بعدی آسان تر کنید
ژورنال
عنوان ژورنال: Neuropharmacology
سال: 2008
ISSN: 0028-3908
DOI: 10.1016/j.neuropharm.2008.06.001