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. 1983 Dec;80(4):711–717. doi: 10.1111/j.1476-5381.1983.tb10062.x

Beta-adrenoceptors of the human myocardium: determination of beta 1 and beta 2 subtypes by radioligand binding.

A Heitz, J Schwartz, J Velly
PMCID: PMC2045057  PMID: 6100846

Abstract

beta-Adrenoceptors of the human myocardium were investigated with binding studies using 125iodocyanopindolol (ICYP) as ligand. Inhibition of ICYP-binding by betaxolol (a selective beta 1-antagonist) and ICI 118551 (a selective beta 2-blocking drug) resulted in non-linear Scatchard-plots suggesting that both beta-adrenoceptor subtypes are present in human left atrium and left ventricle. Computer analysis of the data gave a beta 1/beta 2-adrenoceptor ratio of approximately 65:35 both for left atrium and for left ventricle.

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Selected References

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  1. Ablad B., Carlsson E., Ek L. Pharmacological studies of two new cardioselective adrenergic beta-receptor antagonists. Life Sci I. 1973 Feb 1;12(3):107–119. doi: 10.1016/0024-3205(73)90368-8. [DOI] [PubMed] [Google Scholar]
  2. Berlin N. I., Berman M., Berk P. D., Phang J. M., Waldmann T. A. The application of multicompartmental analysis to problems of clinical medicine. Combined clinical staff conference at the National Institutes of Health. Ann Intern Med. 1968 Feb;68(2):423–448. doi: 10.7326/0003-4819-68-2-423. [DOI] [PubMed] [Google Scholar]
  3. Bryan L. J., Cole J. J., O'Donnell S. R., Wanstall J. C. A study designed to explore the hypothesis that beta-1 adrenoceptors are "innervated" receptors and beta-2 adrenoceptors are "hormonal" receptors. J Pharmacol Exp Ther. 1981 Feb;216(2):395–400. [PubMed] [Google Scholar]
  4. Carlsson E., Dahlöf C. G., Hedberg A., Persson H., Tångstrand B. Differentiation of cardiac chronotropic and inotropic effects of beta-adrenoceptor agonists. Naunyn Schmiedebergs Arch Pharmacol. 1977 Nov;300(2):101–105. doi: 10.1007/BF00505039. [DOI] [PubMed] [Google Scholar]
  5. Chidsey C. A., Braunwald E. Sympathetic activity and neurotransmitter depletion in congestive heart failure. Pharmacol Rev. 1966 Mar;18(1):685–700. [PubMed] [Google Scholar]
  6. Engel G., Hoyer D., Berthold R., Wagner H. (+/-)[125Iodo] cyanopindolol, a new ligand for beta-adrenoceptors: identification and quantitation of subclasses of beta-adrenoceptors in guinea pig. Naunyn Schmiedebergs Arch Pharmacol. 1981;317(4):277–285. doi: 10.1007/BF00501307. [DOI] [PubMed] [Google Scholar]
  7. Harms H. H. Isoproterenol antagonism of cardioselective beta adrenergic receptor blocking agents: a comparative study of human and guinea-pig cardiac and bronchial beta adrenergic receptors. J Pharmacol Exp Ther. 1976 Nov;199(2):329–335. [PubMed] [Google Scholar]
  8. Hedberg A., Minneman K. P., Molinoff P. B. Differential distribution of beta-1 and beta-2 adrenergic receptors in cat and guinea-pig heart. J Pharmacol Exp Ther. 1980 Mar;212(3):503–508. [PubMed] [Google Scholar]
  9. Larregue M., Gallet P., de Giacomoni P., Rat J. P. Dermite du siège en W chez le nourrisson. Ann Pediatr (Paris) 1976 Feb 2;23(2):149–152. [PubMed] [Google Scholar]
  10. Minneman K. P., Hegstrand L. R., Molinoff P. B. Simultaneous determination of beta-1 and beta-2-adrenergic receptors in tissues containing both receptor subtypes. Mol Pharmacol. 1979 Jul;16(1):34–46. [PubMed] [Google Scholar]
  11. O'Donnell S. R., Wanstall J. C. Evidence that ICI 118, 551 is a potent, highly Beta 2-selective adrenoceptor antagonist and can be used to characterize Beta-adrenoceptor populations in tissues. Life Sci. 1980 Aug 25;27(8):671–677. doi: 10.1016/0024-3205(80)90008-9. [DOI] [PubMed] [Google Scholar]
  12. Schwartz J., Velly J. The beta-adrenoceptor of pig coronary arteries: determination of beta 1 and beta 2 subtypes by radioligand binding. Br J Pharmacol. 1983 Jun;79(2):409–414. doi: 10.1111/j.1476-5381.1983.tb11013.x. [DOI] [PMC free article] [PubMed] [Google Scholar]
  13. Schümann H. J., Wagner J., Knorr A., Reidemeister J. C., Sadony V., Schramm G. Demonstration in human atrial preparations of alpha-adrenoceptors mediating positive inotropic effects. Naunyn Schmiedebergs Arch Pharmacol. 1978 May;302(3):333–336. doi: 10.1007/BF00508304. [DOI] [PubMed] [Google Scholar]
  14. Wagner J., Schümann H. J., Knorr A., Rohm N., Reidemeister J. C. Stimulation by adrenaline and dopamine but not by noradrenaline of myocardial alpha-adrenoceptors mediating positive inotropic effects in human atrial preparations. Naunyn Schmiedebergs Arch Pharmacol. 1980 May;312(1):99–102. doi: 10.1007/BF00502581. [DOI] [PubMed] [Google Scholar]
  15. Williams E. M., Raine A. E., Cabrera A. A., Whyte J. M. The effects of prolonged beta-adrenoceptor blockade on heart weight and cardiac intracellular potentials in rabbits. Cardiovasc Res. 1975 Sep;9(5):579–592. doi: 10.1093/cvr/9.5.579. [DOI] [PubMed] [Google Scholar]

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