[Effect of M3-choline receptor blockade on the ability of muscarinic antagonists to prevent catalepsy induced by haloperidol in rats].
A relationship between the indices of efficacy of the muscarinic antagonists in preventing the haloperidol catalepsy and their activity in the tests characterizing the interaction of these ligands with various subtypes of m-cholinoreceptors was studied in rats. A mathematical model was formulated that confirmed the previous conclusion concerning the role of of the m1- and m2-cholinoreceptor blockade in the antiparkinsonian activity of muscarinic antagonists. It was established that blocking of the m3-cholinoreceptors decreases the anticataleptic activity of m-cholinoblockers with respect to haloperidol. It is suggested that the high antihaloperidol activity of pentiphine (an acetyleneamine alcohol) is explained by its dopaminomimetic properties rather than by the anticholinergic activity.
Kosmachev
A B
AB
Institute of Toxicology, Ministry of Public Health of the Russian Federation, ul. Bekhtereva 1, St. Petersburg, 193019 Russia.
Beliaev
V A
VA
Khrabrova
A V
AV
Libman
N M
NM
Dolgo-Saburov
V B
VB
D000818:Animals; D000978:Antiparkinson Agents / Q000494:pharmacology*; D002375:Catalepsy / Q000139:chemically induced / Q000517:prevention & control*; D018492:Dopamine Antagonists; D005260:Female; D006220:Haloperidol; D008297:Male; D008954:Models, Biological; D018727:Muscarinic Antagonists / Q000494:pharmacology*; D051381:Rats; D043587:Receptor, Muscarinic M3; D011976:Receptors, Muscarinic / Q000187:drug effects*; D012044:Regression Analysis
D000978:Antiparkinson Agents; D018492:Dopamine Antagonists; D018727:Muscarinic Antagonists; D043587:Receptor, Muscarinic M3; D011976:Receptors, Muscarinic; D006220:Haloperidol