[The antiparkinson activity of muscarinic antagonists depending on their selectivity for individual m-cholinoreceptor subtypes].
The dependence between the activity parameters of muscarine antagonists in the prevention of haloperidol catalepsy in rats and those in tests characterizing the interaction of ligands and various subtypes of m-cholinoceptors was studied. It was established by constructing the mathematical dependence that blockade of m1-cholinoceptors increases, while that of m2-cholinoceptors reduces the antiparkinsonian activity of the drugs. The activity of the muscarine antagonist pentiphan in the prevention of haloperidol-induced catalepsy in rats exceeds the activity of such traditional antiparkinsonian drugs as cyclodol and amedin.
Kosmachev
A B
AB
Laboratory of Biochemistry, Institute of Toxicology, Russian Federation Ministry of Health, St. Petersburg, Russia.
Beliaev
V A
VA
Khrabrova
A V
AV
Fil'ko
O A
OA
Libman
N M
NM
D000818:Animals; D000978:Antiparkinson Agents / Q000494:pharmacology* / Q000627:therapeutic use; D002375:Catalepsy / Q000139:chemically induced / Q000517:prevention & control; D004195:Disease Models, Animal; D018492:Dopamine Antagonists; D004353:Drug Evaluation, Preclinical; D004347:Drug Interactions; D005260:Female; D006220:Haloperidol; D006801:Humans; D007231:Infant, Newborn; D008297:Male; D018727:Muscarinic Antagonists / Q000494:pharmacology* / Q000627:therapeutic use; D051381:Rats; D011976:Receptors, Muscarinic / Q000145:classification / Q000187:drug effects*; D012044:Regression Analysis
D000978:Antiparkinson Agents; D018492:Dopamine Antagonists; D018727:Muscarinic Antagonists; D011976:Receptors, Muscarinic; D006220:Haloperidol
Antiparkinsonicheskaia aktivnost' muskarinovykh antagonistov v zavisimosti ot ikh izbiratel'nosti k otdel'nym podtipam m-kholinoretseptorov.