Abstract
Cardiovascular studies have been made in anaesthetized cats with SK&F 93319, an antagonist of histamine at both H1- and H2-receptors. SK&F 93319, 8 X 10(-8) and 4 X 10(-7) mol kg-1 min-1 antagonized depressor responses to injections of histamine and the maximum displacement of histamine dose-response curves exceeded that which can be obtained with either an H1-receptor antagonist or an H2-receptor antagonist alone. SK&F 93319, 8 X 10(-8) and 4 X 10(-7) mol kg-1 min-1, also caused dose-dependent antagonism of histamine-induced falls in blood pressure and total peripheral resistance during intravenous infusions of histamine. SK&F 93319 inhibited depressor responses to intravenous injections of 2-(2-aminoethyl)pyridine, dimaprit and impromidine. The displacement of the 2-(2-aminoethyl)pyridine dose-response curve was similar to the displacement of histamine dose-response curves. SK&F 93319 caused greater displacement of dimaprit or impromidine dose-response curves than of histamine or 2-(2-aminoethyl)pyridine dose-response curves. SK&F 93319 was an effective antagonist of histamine, 2-(2-aminoethyl)pyridine or dimaprit-induced vasodilatation in femoral and gastric vasculature. SK&F 93319 has been shown to be an effective antagonist of vascular responses to histamine in anaesthetized cats. SK&F 93319 appeared to be more effective as an H2-receptor antagonist than as an H1-receptor antagonist in these vascular studies.
Full text
PDF





Selected References
These references are in PubMed. This may not be the complete list of references from this article.
- Black J. W., Duncan W. A., Durant C. J., Ganellin C. R., Parsons E. M. Definition and antagonism of histamine H 2 -receptors. Nature. 1972 Apr 21;236(5347):385–390. doi: 10.1038/236385a0. [DOI] [PubMed] [Google Scholar]
- Black J. W., Owen D. A., Parsons M. E. An analysis of the depressor responses to histamine in the cat and dog: involvement of both H1- and H2-receptors. Br J Pharmacol. 1975 Jul;54(3):319–324. doi: 10.1111/j.1476-5381.1975.tb07571.x. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Chipman P., Glover W. E. Histamine H2-receptors in the human peripheral circulation. Br J Pharmacol. 1976 Apr;56(4):494–496. doi: 10.1111/j.1476-5381.1976.tb07463.x. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Durant G. J., Duncan W. A., Ganellin C. R., Parsons M. E., Blakemore R. C., Rasmussen A. C. Impromidine (SK&F 92676) is a very potent and specific agonist for histamine H2 receptors. Nature. 1978 Nov 23;276(5686):403–405. doi: 10.1038/276403a0. [DOI] [PubMed] [Google Scholar]
- Durant G. J., Ganellin C. R., Parsons M. E. Chemical differentiation of histamine H1- and H2-receptor agonists. J Med Chem. 1975 Sep;18(9):905–909. doi: 10.1021/jm00243a009. [DOI] [PubMed] [Google Scholar]
- Flynn S. B., Johnston B. M., Owen D. A. The cardiovascular response to dimaprit, a selective histamine H2-receptor agonist. Br J Pharmacol. 1977 Sep;61(1):101–107. [PMC free article] [PubMed] [Google Scholar]
- Flynn S. B., Owen D. A. Histamine receptors in peripheral vascular beds in the cat. Br J Pharmacol. 1975 Oct;55(2):181–188. doi: 10.1111/j.1476-5381.1975.tb07627.x. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Harvey C. A., Owen D. A., Shaw K. D. Evidence for both histamine H1- and H2-receptors in the gastric vasculature of the cat. Br J Pharmacol. 1980 May;69(1):21–27. doi: 10.1111/j.1476-5381.1980.tb10878.x. [DOI] [PMC free article] [PubMed] [Google Scholar]
- Harvey C. A., Owen D. A. Time dependence of the interaction between histamine and histamine receptor antagonists in the cardiovascular system [proceedings]. Br J Pharmacol. 1980 Jan;68(1):187P–187P. [PMC free article] [PubMed] [Google Scholar]
- Owen D. A., Harvey C. A., Boyce M. J. Effects of histamine on the circulatory system. Klin Wochenschr. 1982 Sep 1;60(17):972–977. doi: 10.1007/BF01716957. [DOI] [PubMed] [Google Scholar]
- Owen D. A., Harvey C. A., Gristwood R. W. Cardiovascular studies with impromidine (SK&F 92676), a new very potent and specific histamine H2-receptor agonist. J Pharm Pharmacol. 1979 Sep;31(9):577–582. doi: 10.1111/j.2042-7158.1979.tb13595.x. [DOI] [PubMed] [Google Scholar]
- Owen D. A. The effects of histamine and some histamine-like agonists on blood pressure in the cat. Br J Pharmacol. 1975 Oct;55(2):173–179. doi: 10.1111/j.1476-5381.1975.tb07626.x. [DOI] [PMC free article] [PubMed] [Google Scholar]