The tachycardia-inducing effects of atropine, N-methylscopolammonium and N-butylscopolammonium were studied in the conscious dog, both in the presence and absence of sympathetic innervation. These effects were compared with the anticholinergic effects of the drugs on the muscarinic cholinoceptors of guinea-pig isolated atria. The order of potency for inhibition of the effects of acetylcholine on the isolated atria was N-methylscopolammonium greater than atropine greater than N-butylscopolammonium. This order was the same for the tachycardia-inducing potencies. Maximal tachycardia with these three drugs was less marked in the absence of sympathetic innervation than in its presence. However, the doses of atropine and of N-butylscopolammonium required to block the effects of vagal influence were greater. Sympathectomy had no effect on the vagolytic potency of N-methylscopolammonium. In the case of atropine and N-methyl-scopolammonium there was good correlation between anticholinergic and tachycardia-inducing potencies. The tachycardiac effects of these compounds can be explained by their anticholinergic effect. The tachycardia-inducing potency of N-butylscopolammonium was greater than its anticholinergic potency.

1975-11-01·Neuropharmacology2区 · 医学

Central effects of scopolamine and (+)-amphetamine on locomotor activity: Interaction with strain and stress variables

2区 · 医学

Article

作者: H. Anisman ; Diane Cygan

Application of footshock to 3 strains of mice augmented strain dependently the locomotor activity induced by (+)-amphetamine sulfate (I) [51-63-8] (5-10 mg/kg, i.p.) and eliminated scopolamine-HBr [114-49-8] (1-10 mg/kg, i.p.) induced suppression of activity independent of strain.Scopolamine methylsulfate [18067-13-5] (0.9-9 mg/kg, i.p.) and p-hydroxyamphetamine-HBr [306-21-8] (0.63-6.3 mg/kg, i.p.) did not affect pre- or postshock activity.FLA-63 eliminated the I-shock synergism and indicated norepinephrine mediated the shock induced augmentation by I.

1974-01-01·Chemical and Pharmaceutical Bulletin4区 · 医学

Metabolism of Methylscopolammonium Methylsulfate (DD-234) in Rats

4区 · 医学

Article

作者: Hakusui, Hideo ; Sano, Mitsuji

Eight metabolites were detected in the urine and feces of rats after oral and s.c. administration of DD 234 (methylscopolammonium methyl sulfate)(I) [18067-13-5].Characteristics of the metabolic pathway were that the quaternary ammonium moiety was unchanged, the major pathway involved oxidation at the para position of the benzene ring to introduce hydroxy and methoxy groups, and the minor products were the apo-derivative, glucuronide of I, and scopine derivativeAbsorption and excretion were examined by using 14C-labeled I, and the excreted total radioactivities were 82.2% of the oral dose and 93.6% of the s.c. dose in urine and feces.In respiratory air 14CO2 was not detectable.Comparison of the metabolic pathway with that of tertiary scopolamine was discussed.

100 项与 N-Methylscopolamine methylsulfate 相关的药物交易

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