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Direct evidence for an interaction of β-adrenergic blockers with the 5-HT receptor

Nature volume 267, pages 289–290 (1977)Cite this article

Abstract

ADVANCES in neurotransmitter receptor identification and quantification by biochemical techniques involving radiolabelled analogues of putative neurotransmitters have led to the characterisation of a number of receptor systems in mammalian brain tissue1; these include the catecholamines2,3, 5-HT4, glycine5 and GABA6 receptors. The development of these techniques has provided a means of screening chemical compounds for their effects on different receptor systems7. The central nervous system effects of (±)-propranolol (Inderal, ICI) in animals are well documented8,9. This drug has therapeutic benefit in man in anxiety10, and is also reported to have similar benefit in schizophrenia11,12, essential tremor13 and drug dependence14. The origin of these effects is not understood but theories about its mode of action include β-adrenergic blockade15, membrane stabilisation8 and a 5-HT receptor blocking action16,17. We report here that propranolol a stereospecific affinity for the 5-HT receptor from rat brain which is similar in magnitude to the putative 5-HT receptor blocking drug methylsergide.

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Authors and Affiliations

  1. Biochemistry Department, Imperial Chemical Industries Limited, Pharmaceuticals Division, Mereside, Alderley Park, Macclesfield, Cheshire, UK

    DEREK N. MIDDLEMISS, LOUISE BLAKEBOROUGH & STEPHEN R. LEATHER

Authors
  1. DEREK N. MIDDLEMISS
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  2. LOUISE BLAKEBOROUGH
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  3. STEPHEN R. LEATHER
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MIDDLEMISS, D., BLAKEBOROUGH, L. & LEATHER, S. Direct evidence for an interaction of β-adrenergic blockers with the 5-HT receptor. Nature 267, 289–290 (1977). https://doi.org/10.1038/267289a0

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