Regulation of the CHAPS-solubilized muscarinic receptors by an inhibitory GTP binding protein (Gi) in the brain of neonatal and adult rats
作者： Ashok K Singh
DOI: 10.1016/0300-9629(94)90128-7
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摘要: Abstract CHAPS-solubilized muscarinic receptors (mAChRs) retain selective agonist or antagonist binding and sensitivity to GTP ADP-ribosylation by pertussis toxin that ribosylates a group of G protein called Gi. This suggests CHAPS solubilizes the mAChR-Gi complex both from neonatal adult neurons. The gradient centrifugation solubilized samples indicated contain mostly Gi-coupled mAChR (mAChRn,) exhibiting high affinity for [3H]OxM, but comparable quantity Gi coupled (mAChRa1) uncoupled mAChRs (mAChRa2) low agonist. [3H]OxM dissociation mAChRn mAChRa1 was sensitive GTP. However, effects were Na+ not mAChRa1. cholera abolished on mAChRn, suggesting NaCl affects interacting with receptor complex. subtype composition mAChRa2 studied determining ic 50 Ki values inhibition subtype-selective antagonists in receptors. exhibited differences distribution subtypes, containing M1-mAChR subspecies M1−, M2- M3-mAChR subspecies. pirenzepine-induced M1-mAChRn M1-mAChRa1 GTP-induced modulated Na+, effect not. functional between M1-mAChRa1.
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