[Effect of biotransformation on the receptor selectivity of muscarinic antagonists in vivo].
In the experiments in vivo it is found that the receptor selectivity of muscarine antagonist glypine is time-dependent unlike atropine, amedine, benzhexol, benactyzine, and thropacin. Using modulation of the metabolic system activity it is shown that upon biotransformation glypine forms active metabolites that differs in receptor selectivity of the action.
Kosmachev
A B
AB
Institute of Toxicology, Ministry of Public Health, St. Petersburg, Russia.
Titkova
T A
TA
Fil'ko
O A
OA
Libman
N M
NM
D000818:Animals; D001115:Arecoline; D001285:Atropine / Q000493:pharmacokinetics / Q000494:pharmacology; D001535:Benactyzine / Q000493:pharmacokinetics / Q000494:pharmacology; D001711:Biotransformation; D018679:Cholinergic Agonists; D004006:Dichlorvos / Q000633:toxicity; D005260:Female; D008024:Ligands; D008297:Male; D008333:Mandelic Acids / Q000493:pharmacokinetics / Q000494:pharmacology; D018727:Muscarinic Antagonists / Q000493:pharmacokinetics / Q000494:pharmacology*; D051381:Rats; D043643:Receptor, Muscarinic M1; D043585:Receptor, Muscarinic M2; D011976:Receptors, Muscarinic / Q000187:drug effects*; D014202:Tremor / Q000139:chemically induced / Q000378:metabolism; D014282:Trihexyphenidyl / Q000493:pharmacokinetics / Q000494:pharmacology; D014326:Tropanes / Q000493:pharmacokinetics / Q000494:pharmacology
D018679:Cholinergic Agonists; D008024:Ligands; D008333:Mandelic Acids; D018727:Muscarinic Antagonists; D043643:Receptor, Muscarinic M1; D043585:Receptor, Muscarinic M2; D011976:Receptors, Muscarinic; D014326:Tropanes; C016215:amedin; C003727:tropacine; C026280:glipin; D001115:Arecoline; D001535:Benactyzine; D014282:Trihexyphenidyl; D001285:Atropine; D004006:Dichlorvos