Beta-adrenoceptors in cardiac disease

Pharmacol Ther. 1993 Dec;60(3):405-30. doi: 10.1016/0163-7258(93)90030-h.


The human heart contains both beta 1 and beta 2-adrenoceptors; both mediate positive inotropic and chronotropic effects. In chronic heart failure, beta-adrenoceptor number is reduced, presumably, by down-regulation by endogenous noradrenaline which is elevated due to increased sympathetic activity. Since the human heart contains only a few spare receptors for beta-adrenoceptor-mediated positive inotropic effects and the amount of spare receptors declines in chronic heart failure, it is not surprising that the reduced beta-adrenoceptor number is accompanied by decreased contractile responses to beta-adrenoceptor agonists (including endogenous catecholamines), and the extent of decrease in maximal inotropic response is more pronounced as the disease becomes more advanced. Moreover, in chronic heart failure myocardial G(i)-protein, which inhibits cAMP formation, is increased, which might further contribute to the reduction in beta-adrenoceptor-mediated effects. It appears that, at present, the best therapy for severe heart failure is a successful heart transplant, since in the transplanted heart beta-adrenoceptor number and function seems to be normalized. Moreover, the data currently available do not suggest any development of super- or subsensitivity of postsynaptic cardiac beta-adrenoceptors in the transplanted human heart.

Publication types

  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • Adrenergic beta-Agonists / pharmacology
  • Adrenergic beta-Antagonists / pharmacology
  • Amino Acid Sequence
  • Down-Regulation
  • Heart / drug effects
  • Heart Diseases / metabolism*
  • Heart Diseases / physiopathology
  • Heart Transplantation
  • Humans
  • Molecular Sequence Data
  • Myocardial Contraction / drug effects
  • Receptors, Adrenergic, beta / chemistry
  • Receptors, Adrenergic, beta / drug effects
  • Receptors, Adrenergic, beta / physiology*


  • Adrenergic beta-Agonists
  • Adrenergic beta-Antagonists
  • Receptors, Adrenergic, beta