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British Journal of Pharmacology logoLink to British Journal of Pharmacology
. 1982 Jun;76(2):305–311. doi: 10.1111/j.1476-5381.1982.tb09221.x

Effects of impromidine, a specific H2-receptor agonist and 2(2-pyridyl)-ethylamine, an H1-receptor agonist, on stimulation-induced release of [3H]-noradrenaline in guinea-pig isolated atria.

M J Rand, D F Story, H Wong-Dusting
PMCID: PMC2071780  PMID: 6212093

Abstract

1 The specific histamine H2-receptor agonist, impromidine (3-100 nmol/l), increased the rate and force of beating of guinea-pig isolated atria. These effects were blocked by the H2-receptor antagonist, cimetidine (30 mumol/l), but not by the H1-receptor antagonist, mepyramine (0.1 mumol/l). 2 In atria that had previously been incubated in [3H]-noradrenaline, impromidine (3-100 nmol/l) had no effect on the resting efflux of radioactivity, but concentrations of 50 and 100 nmol/l significantly increased the efflux induced by electrical stimulation (2 Hz for 10 s) of the intramural sympathetic nerves by approximately 38%; lower concentrations (3, 10 and 25 nmol/l) had no effect. 3 The effect of impromidine in enhancing stimulation-induced efflux of radioactivity was abolished by cimetidine (30 mumol/l) and by mepyramine (0.1 mumol/l). It was unaffected by the alpha-adrenoceptor antagonist, phentolamine (30 mumol/l). 4 Impromidine produced some inhibition of the uptake of [3H]-noradrenaline, but this did not account for the enhancement of the stimulation-induced efflux of radioactivity, since impromidine (50 mumol/l) still increased release in the presence of cocaine (30 mumol/l). 5 The specific H1-receptor agonist, 2-(2-pyridyl)-ethylamine (10-100 mumol/l), increased both the resting and stimulation-induced efflux of radioactivity. These effects were not blocked by mepyramine (0.1 mumol/l) or the beta-adrenoceptor antagonist, metoprolol (0.1 mumol/l). 6 The prejunctional inhibitory histamine receptors in guniea-pig atria are not classifiable into H1- or H2-type by the use of relatively specific postjunctional histamine H1- or H2-receptor agonists and antagonists.

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Selected References

These references are in PubMed. This may not be the complete list of references from this article.

  1. Bertaccini G., Coruzzi G. Effect of impromidine (SK&F 92676) on the isolated papillary muscle of the guinea-pig. Br J Pharmacol. 1981 Feb;72(2):197–199. doi: 10.1111/j.1476-5381.1981.tb09113.x. [DOI] [PMC free article] [PubMed] [Google Scholar]
  2. Curwain B. P., Turner N. C. Comparison of the agonist activity of impromidine (SK & F 92676) in anaesthetized rabbits and on the rabbit isolated fundic mucosa. Br J Pharmacol. 1981 Aug;73(4):917–919. doi: 10.1111/j.1476-5381.1981.tb08746.x. [DOI] [PMC free article] [PubMed] [Google Scholar]
  3. 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]
  4. 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]
  5. Flynn S. B., Gristwood R. W., Owen D. A. 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. Br J Pharmacol. 1979 Jan;65(1):127–137. doi: 10.1111/j.1476-5381.1979.tb17341.x. [DOI] [PMC free article] [PubMed] [Google Scholar]
  6. Hughes M. J. A question of the specificity of rabbit atrial chronotropic histamine receptors and agents which affect their activity. J Clin Pharmacol. 1980 Jan;20(1):10–19. doi: 10.1002/j.1552-4604.1980.tb01661.x. [DOI] [PubMed] [Google Scholar]
  7. Karch F. E., Ingram J., Oravec J., Cohen J. Evidence for a histamine-component of the heart rate response to stellate ganglion stimulation. Pharmacol Res Commun. 1977 Jun;9(6):553–562. doi: 10.1016/s0031-6989(77)80083-0. [DOI] [PubMed] [Google Scholar]
  8. Lokhandwala M. F. Inhibition of sympathetic nervous system by histamine:studies with H1- and H2-receptor antagonists. J Pharmacol Exp Ther. 1978 Jul;206(1):115–122. [PubMed] [Google Scholar]
  9. Majewski H., McCulloch M. W., Rand M. J., Story D. F. Adrenaline activation of prejunctional beta-adrenoceptors in guinea-pig atria. Br J Pharmacol. 1980;71(2):435–444. doi: 10.1111/j.1476-5381.1980.tb10956.x. [DOI] [PMC free article] [PubMed] [Google Scholar]
  10. McCulloch M. W., Rand M. J., Story D. F. Resting and stimulation-induced efflux of tritium from guinea-pig atria incubated with 3-H-noradrenaline. Clin Exp Pharmacol Physiol. 1974 Jul-Aug;1(4):275–289. doi: 10.1111/j.1440-1681.1974.tb00550.x. [DOI] [PubMed] [Google Scholar]
  11. McGrath M. A., Shepherd J. T. Inhibition of adrenergic neurotransmission in canine vascular smooth muscle by histamine: mediation by H2-receptors. Circ Res. 1976 Oct;39(4):566–573. doi: 10.1161/01.res.39.4.566. [DOI] [PubMed] [Google Scholar]
  12. Medgett I. C., McCulloch M. W., Rand M. J. Partial agonist of clonidine on prejunctional and postjunctional alpha-adrenoceptors. Naunyn Schmiedebergs Arch Pharmacol. 1978 Oct;304(3):215–221. doi: 10.1007/BF00507961. [DOI] [PubMed] [Google Scholar]
  13. Parsons M., Sykes C. Impromidine (SK & F 92676) acts as a partial agonist on the isolated whole stomach of the rat. Br J Pharmacol. 1980 May;69(1):6–7. doi: 10.1111/j.1476-5381.1980.tb10874.x. [DOI] [PMC free article] [PubMed] [Google Scholar]
  14. Powell J. R. Effects of histamine on vascular sympathetic neuroeffector transmission. J Pharmacol Exp Ther. 1979 Mar;208(3):360–365. [PubMed] [Google Scholar]
  15. Rand M. J., Story D. F., Wong-Dusting H. K. Effects of histamine on the resting and stimulation-induced release of [3H]-noradrenaline in guinea-pig isolated atria. Br J Pharmacol. 1982 Jan;75(1):57–64. doi: 10.1111/j.1476-5381.1982.tb08757.x. [DOI] [PMC free article] [PubMed] [Google Scholar]
  16. Starke K. Regulation of noradrenaline release by presynaptic receptor systems. Rev Physiol Biochem Pharmacol. 1977;77:1–124. doi: 10.1007/BFb0050157. [DOI] [PubMed] [Google Scholar]
  17. Westfall T. C. Local regulation of adrenergic neurotransmission. Physiol Rev. 1977 Oct;57(4):659–728. doi: 10.1152/physrev.1977.57.4.659. [DOI] [PubMed] [Google Scholar]

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