Characteristics of muscarinic cholinoceptors in airways of antigen-induced airway hyperresponsive rats.
The antagonist and agonist binding sites of muscarinic receptors were investigated by using membrane preparations of airways from nonsensitized normal control, sensitized control and repeatedly antigen challenged rats. The in vitro bronchial responsiveness to ACh was markedly increased in repeatedly antigen challenged group but not in sensitized control group. No significant difference was observed in receptor density and antagonist affinity among these three groups. The affinity of ACh for high-affinity agonist binding sites of repeatedly antigen challenged group was much greater than those in the other groups; the affinity significantly reduced in the presence of GTP gamma S. We concluded that enhanced G protein level might be involved in inducing airway hyperresponsiveness in rats.
Chiba
Y
Y
Department of Pharmacology, School of Pharmacy, Hoshi University, Tokyo, Japan.
Misawa
M
M
D000109:Acetylcholine / Q000494:pharmacology*; D000818:Animals; D000941:Antigens / Q000633:toxicity*; D001665:Binding Sites; D016535:Bronchial Hyperreactivity / Q000139:chemically induced* / Q000378:metabolism; D003198:Computer Simulation; D004305:Dose-Response Relationship, Drug; D016244:Guanosine 5'-O-(3-Thiotriphosphate) / Q000494:pharmacology; D008297:Male; D018721:Muscarinic Agonists / Q000494:pharmacology*; D018727:Muscarinic Antagonists / Q000494:pharmacology*; D051381:Rats; D017208:Rats, Wistar; D011976:Receptors, Muscarinic / Q000187:drug effects* / Q000378:metabolism
D000941:Antigens; D018721:Muscarinic Agonists; D018727:Muscarinic Antagonists; D011976:Receptors, Muscarinic; D016244:Guanosine 5'-O-(3-Thiotriphosphate); D000109:Acetylcholine