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Tachykinin receptors and the potential of tachykinin antagonists as clinically effective analgesics and anti-inflammatory agents

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Pain and Neurogenic Inflammation

Part of the book series: Progress in Inflammation Research ((PIR))

Abstract

Tachykinins (also known as neurokinins) share a common C-terminal sequence, Phe-X-Gly-Leu-Met-NH2 (where X is Phe, Tyr, Val or Ile). Substance P was the first to be discovered and is the best characterised. Other tachykinins notable for their widespread distribution in mammalian tissues, including the peripheral and central nervous system, are neurokinins A and B. The biological actions of tachykinins are through G-protein linked receptors designated NK1, NK2 and NK3 and there has been an assumption that the preferred agonists were substance P, neurokinin A and neurokinin B respectively [1], [2]. However, the receptor selectivity of these peptides is relatively poor. There is a mismatch between tachykinin-containing neurones and fibres and their corresponding receptor in certain brain regions and this is particularly apparent in the case of neurokinin A since NK2 receptor expression appears to be extremely low in the adult mammalian nervous system [3]. A novel NK4 receptor has been proposed and it appears that there are two NK3 receptors designated A and B [4].

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  1. Merck Sharp and Dohme Research Laboratories, Neuroscience Research Centre, Terlings Park, Harlow, Essex, CM20 2QR, UK

    Raymond G. Hill & Nadia M. J. Rupniak

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  1. Cardiovascular Research Centre, Division of Biomedical Sciences, King’s College London, Manresa Road, SW3 6LX, London, UK

    Susan D. Brain

  2. Messengers and Signalling Group, Division of Biomedical Sciences, King’s College London, Manresa Road, SW3 6LX, London, UK

    Philip K. Moore

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Hill, R.G., Rupniak, N.M.J. (1999). Tachykinin receptors and the potential of tachykinin antagonists as clinically effective analgesics and anti-inflammatory agents. In: Brain, S.D., Moore, P.K. (eds) Pain and Neurogenic Inflammation. Progress in Inflammation Research. Birkhäuser, Basel. https://doi.org/10.1007/978-3-0348-8753-3_16

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  • DOI: https://doi.org/10.1007/978-3-0348-8753-3_16

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