Literature DB >> 2946343

Impromidine is a partial histamine H2-receptor agonist on human ventricular myocardium.

T A English, R W Gristwood, D A Owen, J Wallwork.   

Abstract

The inotropic effects of impromidine have been studied and compared with those of histamine on human isolated left ventricular preparations stimulated at 1 Hz. Both drugs caused concentration-related increases in force of contraction and were of similar potency, although the maximum response to impromidine was markedly and significantly less than that to histamine. The positive inotropic responses of impromidine were inhibited by cimetidine 1 X 10(-5) M, consistent with histamine H2-receptor involvement. Impromidine 1 X 10(-4) M inhibited maximal responses to histamine to a level equal to the maximal impromidine response; however, impromidine did not inhibit responses to isoprenaline. Positive inotropic activity and inhibition of maximal responses to histamine occurred over a similar impromidine concentration-range. Impromidine displaced histamine concentration-response curves to the right, whereas mepyramine had no effect on responses to histamine. It is concluded that impromidine has positive inotropic activity on the human ventricle, that the response is mediated via histamine H2-receptors, and that impromidine is a partial agonist compared with histamine.

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Year:  1986        PMID: 2946343      PMCID: PMC1917005          DOI: 10.1111/j.1476-5381.1986.tb10265.x

Source DB:  PubMed          Journal:  Br J Pharmacol        ISSN: 0007-1188            Impact factor:   8.739


  9 in total

1.  Definition and antagonism of histamine H 2 -receptors.

Authors:  J W Black; W A Duncan; C J Durant; C R Ganellin; E M Parsons
Journal:  Nature       Date:  1972-04-21       Impact factor: 49.962

2.  Impromidine (SK&F 92676) is a very potent and specific agonist for histamine H2 receptors.

Authors:  G J Durant; W A Duncan; C R Ganellin; M E Parsons; R C Blakemore; A C Rasmussen
Journal:  Nature       Date:  1978-11-23       Impact factor: 49.962

3.  Pharmacological characterization of cardiac histamine receptors: sensitivity to H1-and H2-receptor agonists and antagonists.

Authors:  R Levi; N Capurro; C H Lee
Journal:  Eur J Pharmacol       Date:  1975-02       Impact factor: 4.432

4.  Differentiation of the roles of histamine H1- and H2-receptors in the mediation of the effects of histamine in the isolated working heart of the guinea-pig.

Authors:  S B Flynn; R W Gristwood; D A Owen
Journal:  Br J Pharmacol       Date:  1979-01       Impact factor: 8.739

5.  Inotropic and electrophysiological effects of histamine on human ventricular heart muscle.

Authors:  L Eckel; R W Gristwood; H Nawrath; D A Owen; P Satter
Journal:  J Physiol       Date:  1982-09       Impact factor: 5.182

6.  Impromidine (SK & F 92676) acts as a partial agonist on the isolated whole stomach of the rat.

Authors:  M Parsons; C Sykes
Journal:  Br J Pharmacol       Date:  1980-05       Impact factor: 8.739

7.  Cardiovascular studies with impromidine (SK&F 92676), a new very potent and specific histamine H2-receptor agonist.

Authors:  D A Owen; C A Harvey; R W Gristwood
Journal:  J Pharm Pharmacol       Date:  1979-09       Impact factor: 3.765

8.  Effective stimulation of cardiac contractility and myocardial metabolism by impromidine and dimaprit--two new H2-agonistic compounds--in the surviving, catecholamine-insensitive myocardium after coronary occlusion.

Authors:  G Baumann; S B Felix; G Riess; U Loher; L Ludwig; H Blömer
Journal:  J Cardiovasc Pharmacol       Date:  1982 Jul-Aug       Impact factor: 3.105

9.  Effect of impromidine (SK&F 92676) on the isolated papillary muscle of the guinea-pig.

Authors:  G Bertaccini; G Coruzzi
Journal:  Br J Pharmacol       Date:  1981-02       Impact factor: 8.739

  9 in total
  2 in total

Review 1.  The Roles of Cardiovascular H2-Histamine Receptors Under Normal and Pathophysiological Conditions.

Authors:  Joachim Neumann; Uwe Kirchhefer; Stefan Dhein; Britt Hofmann; Ulrich Gergs
Journal:  Front Pharmacol       Date:  2021-12-20       Impact factor: 5.810

2.  A three-parameter two-state model of receptor function that incorporates affinity, efficacy, and signal amplification.

Authors:  Peter Buchwald
Journal:  Pharmacol Res Perspect       Date:  2017-04-27
  2 in total

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