Evolution of β-blockers: from anti-anginal drugs to ligand-directed signalling

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Baker, Jillian G. ; Hill, Stephen J. ; Summers, Roger J. (2011)
  • Publisher: Elsevier
  • Journal: Trends in Pharmacological Sciences, volume 32, issue 4-2, pages 227-234 (issn: 0165-6147, eissn: 1873-3735)
  • Related identifiers: doi: 10.1016/j.tips.2011.02.010, pmc: PMC3081074
  • Subject: Toxicology | Review | Pharmacology

Sir James Black developed β-blockers, one of the most useful groups of drugs in use today. Not only are they being used for their original purpose to treat angina and cardiac arrhythmias, but they are also effective therapeutics for hypertension, cardiac failure, glaucoma, migraine and anxiety. Recent studies suggest that they might also prove useful in diseases as diverse as osteoporosis, cancer and malaria. They have also provided some of the most useful tools for pharmacological research that have underpinned the development of concepts such as receptor subtype selectivity, agonism and inverse agonism, and ligand-directed signalling bias. This article examines how β-blockers have evolved and indicates how they might be used in the future.
  • References (134)
    134 references, page 1 of 14

    1 Black, J. (2010) A life in new drug research. Br. J. Pharmacol. 160 (Suppl. 1), S15-S25

    2 Black, J.W. et al. (1985) An operational model of pharmacological agonism: the effect of E/[A] curve shape on agonist dissociation constant estimation. Br. J. Pharmacol. 84, 561-571

    3 Lyall, J. (2010) James Black: Nobel prize winning pharmacologist who invented b blockers. Br. Med. J. 340, c1817

    4 Ahlquist, R.P. (1948) A study of the adrenotropic receptors. Am. J. Physiol. 153, 586-600

    5 Powell, C.E. and Slater, I.H. (1958) Blocking of inhibitory adrenergic receptors by a dichloro analog of isoproterenol. J. Pharmacol. Exp. Ther. 122, 480-488

    6 Black, J.W. et al. (1965) Comparison of some properties of pronethalol and propranolol. Br. J. Pharmacol. Chemother 25, 577-591

    7 Black, J.W. and Prichard, B.N. (1973) Activation and blockade of badrenoceptors in common cardiac disorders. Br. Med. Bull. 29, 163-167

    8 Prichard, B.N. (1964) Hypotensive action of pronethalol. Br. Med. J. 1, 1227-1228

    9 Prichard, B.N. and Gillam, P.M. (1964) Use of propranolol (Inderal) in treatment of hypertension. Br. Med. J. 2, 725-727

    10 Prichard, B.N. (1978) The second Lilly Prize Lecture, University of Newcastle, July 1977. (b-Adrenergic receptor blockade in hypertension, past, present and future. Br. J. Clin. Pharmacol. 5, 379-399

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