ISSN:
1420-908X
Source:
Springer Online Journal Archives 1860-2000
Topics:
Medicine
Notes:
Abstract Dimaprit analogues having alkyl substituents on the isothiourea group have no detectable H2-agonist activity on the guinea-pig atrium. N-Methyldimaprit [S-[3-(N,N-dimethylamino)propyl]-N′-methylisothiourea] (SK&F92054) is identified as a compound which may serve as a suitable chemical control when studying the actions of dimaprit at putative H2-histamine receptors. Concentrations of N-methyl-dimaprit (up to 3×10−3 M) had no agonist activityin vitro on the guinea-pig atrium (〈0.005% of the activity of histamine), rat uterus (up to 2×10−3M) or as a stimulant of guinea-pig ventricular adenylate cyclase (up to 10−3 M). N-Methyldimaprit at 10−3 M also did not significantly stimulate acid secretion in the rat isolated stomach preparation; it was a very weak stimulant of gastric acid secretion (〈0.2% of the activity of histamine)in vivo in the lumen-perfused stomach of the anaesthetised rat but exhibited marked tachyphylaxis on repeated administration. N-Methyldimaprit, has two basic centres, macroscopic pKa values 8.31 and 9.58 at 40°C.
Type of Medium:
Electronic Resource
URL:
http://dx.doi.org/10.1007/BF01977251
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