[The antiparkinson activity of muscarinic antagonists depending on their selectivity for individual m-cholinoreceptor subtypes].

Abstract

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.

• Authors: A B Kosmachev, V A Beliaev, A V Khrabrova, O A Fil'ko, N M Libman
• Journal: Eksperimental'naia i klinicheskaia farmakologiia (Eksp Klin Farmakol) 1998 Sep-Oct Vol. 61 Issue 5 Pg. 3-5 ISSN: 0869-2092 [Print] Russia (Federation)
• Vernacular Title: Antiparkinsonicheskaia aktivnost' muskarinovykh antagonistov v zavisimosti ot ikh izbiratel'nosti k otdel'nym podtipam m-kholinoretseptorov.
• PMID: 9854621 (Publication Type: English Abstract, Journal Article, Research Support, Non-U.S. Gov't)

Chemical References

• Antiparkinson Agents
• Dopamine Antagonists
• Muscarinic Antagonists
• Receptors, Muscarinic
• Haloperidol

Topics

• Animals
• Antiparkinson Agents (pharmacology, therapeutic use)
• Catalepsy (chemically induced, prevention & control)
• Disease Models, Animal
• Dopamine Antagonists
• Drug Evaluation, Preclinical
• Drug Interactions
• Female
• Haloperidol
• Humans
• Infant, Newborn
• Male
• Muscarinic Antagonists (pharmacology, therapeutic use)
• Rats
• Receptors, Muscarinic (classification, drug effects)
• Regression Analysis