Analgetic Activity of a Quinazoline

Role of muscarinic receptor subtypes in central antinociception

“…administered acetylcholine (ACh) (Pedigo et al, 1975) and both direct and indirect muscarinic agonists such as oxotremorine (George et al, 1962;Bartolini et al, 1980;1987a) and its precursor tremorine (Lenke, 1958), arecoline (Herz, 1962), pilocarpine (Hendershot & Forsaith, 1959;Chernov et al, 1967), physostigmine (Harris et al, 1969;Ireson, 1970) and diisopropyl phosphorofluoridate (DFP) (Lentz et al, 1969) induce antinociception in the laboratory animal. Since such antinociception is completely antagonized by atropine (Bartolini et al, 1987a), a muscarinic receptor should be involved.…”

Biological Activities of Diazonium Compounds: Induction of Hypothermia or Writhing by 4 (Or 5)-Diazoimidazole-5 (Or 4)-Carboxamide and Their Antagonism by Analgesics

“…The inhibition of drug-induced writhing in mice has been proposed as a screening test for analgesics (1, 2, 5-7), although non-analgesic drugs also inhibit writhing (2,8,9).In the present experiments, intraperitoneal injection of the diazonium compound, 4 (or 5)-diazoimidazole-5 (or 4)-carboxamide had a profound effect on body temper ature and induced the writhing syndrome. Both the severe hypothermia and writhing following its inejction could be ameliorated with analgesics.…”

“…The inhibition of drug-induced writhing in mice has been proposed as a screening test for analgesics (1, 2, 5-7), although non-analgesic drugs also inhibit writhing (2,8,9).…”