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Agonist and Antagonist Receptor Binding

  • Chapter
The Tachykinin Receptors

Part of the book series: The Receptors ((REC))

Abstract

Substance P (SP), neurokinin A (NKA), and neurokinin B (NKB) are members of the tachykinin family of peptides that share the carboxy terminal sequence Phe-X-Gly-Leu-Met-NH2. These mammalian tachykinins elicit their effects through three different receptors known as NK1NK2and NK3. Pharmacological and biochemical studies suggest that substance P is the preferred endogenous ligand for the NKI receptor, whereas neurokinin A and neurokinin B have highest affinity for NK2 and NK3 receptors, respectively (Buck and Burcher, 1986; Maggio, 1988; Quirion and Dam, 1988; Guard and Watson, 1991). The characterization of the NKINK2and NK3 receptors as distinct sites was confirmed with the cloning and sequencing of separate cDNAs encoding each of the receptors (Masu et al., 1987; Sasai and Nakanishi, 1989; Yokota et al., 1989; Gerard et al., 1990; Hershey and Krause, 1990; Shigemoto et al., 1990; Hershey et al., 1991). The deduced amino acid sequence and hydropathy analysis suggest that all three of the tachykinin receptors contain seven transmembrane spanning domains and sequence similarity with other members of the superfamily of G-proteincoupled receptors. Maximal sequence homology among NKINK2and NK3 receptors is found in the putative core transmembrane domains, whereas homology is lowest at the amino and carboxy terminal ends (Nakanishi, 1991).

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Authors
  1. Stafford McLean
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  2. John A. Lowe III
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Editors and Affiliations

  1. Biopharm Consultists, Tucson, AZ, USA

    Stephen H. Buck

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© 1994 Springer Science+Business Media New York

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McLean, S., Lowe, J.A. (1994). Agonist and Antagonist Receptor Binding. In: Buck, S.H. (eds) The Tachykinin Receptors. The Receptors. Humana Press, Totowa, NJ. https://doi.org/10.1007/978-1-4612-0301-8_4

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  • DOI: https://doi.org/10.1007/978-1-4612-0301-8_4

  • Publisher Name: Humana Press, Totowa, NJ

  • Print ISBN: 978-1-4612-6699-0

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