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The aim of the present study was to evaluate the effect of DAU 6215 (N-(endo-8-methyl-8-azabicyclo[3.2.1]oct-3-yl)-2, 3-dihydro-2-oxo-1H-benzimidazol-1-carboxamide, hydrochloride), which is a 5HT-3 receptor antagonist, chemically different from the other 5HT-3 antagonists, on a wide variety of animal models sensitive to anxiolytics. Nine animal models were(More)
The study reports the functional affinity of an amidino derivative of pirenzepine, guanylpirenzepine, for muscarinic receptors mediating relaxation of rat duodenum, inhibition of rabbit vas deferens twitch contraction (both receptors previously classified as M1), guinea pig negative inotropism (M2) and ileal contraction (M3). Unlike pirenzepine,(More)
BIMT 17 (1-[2-[4-(3-trifluoromethyl phenyl) piperazin-1-yl] ethyl] benzimidazol- [1H]-2-one), a 5-HT1A receptor agonist/5-HT2A receptor antagonist (see Borsini et al., accompanying paper), in a dose range of 1–10 mg/kg i.v., dose-dependently inhibited the electrical activity of rat medial prefronto-cortical neurons, whereas buspirone, in a dose range of(More)
The muscarinic receptors responsible for two effects elicited by McN-A-343, i.e. the relaxation of the rat duodenum and the inhibition of the twitch contraction of rabbit vas deferens, were investigated by use of derivatives of 4-diphenyl acetoxy-N-methyl piperidine methobromide (4-DAMP). Both receptors had been previously identified as M1 on the basis of(More)
The pharmacological profile of six representative members of a novel class of 5-HT3 receptor antagonists is described. The compounds are esters and amides of benzimidazolone-1-carboxylic acid with a basic azabicycloalkyl moiety (compounds 1-3) and their respective ethyl derivatives (compounds 4-6). In isolated preparations (rabbit heart and guinea pig(More)
In the search for antidepressant agents with a rapid onset of action, we have found that compound BIMT 17 (1-[2-[4-(3-trifluoromethylphenyl)piperazin1-yl]ethyl]benzimidazol-[1H]-2-one) shows a good affinity for cerebral cortical 5-HT1A (pK i = 7.72) and 5-HT2A (pK i = 6.90) receptors, with no appreciable affinity for the other 5-HT receptor subtypes,(More)
Mifentidine, a representative compound of a novel class of H2-antagonists, has been investigated for its ability to interact with H2-receptors and to inhibit gastric acid secretion. Affinity estimates (K B) of mifentidine obtained fromin vitro studies on cardiac and gastric mucosal histamine (H2) receptors were in the 20–50 nM range. Mifentidine appeared to(More)
The protective effect of cimetidine, ranitidine and a newer H2-receptor antagonist, mifentidine (proposed INN), on models of gastric and duodenal damage, caused by activation of H2 receptors, was studied. Gastric erosions were induced in rats by intravenous dimaprit (100 mg/kg) while duodenal damage was investigated in guinea pigs following subcutaneous(More)
Structure-activity considerations of N alpha-guanylhistamine, the first compound found with detectable H2-antagonist activity, led to the synthesis of a series of conformationally rigid guanylhistamine analogues, namely, (imidazolylphenyl)guanidines, imidazolylbenzamidines, and (imidazolylphenyl)formamidines. It was found that in the guanidine and(More)