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Chemical Compound Review

CHEMBL131872     (3S)-3-[[(1S)-1-[[(1S)-1- [[(1S)-1-[[1...

Synonyms: CHEBI:321472, AC1NSK2B, GR64349, NCGC00167319-01
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Disease relevance of GR64349


Psychiatry related information on GR64349


High impact information on GR64349

  • The design and synthesis of potent and selective neurokinin NK-2 receptor agonists 12 (GR64349) and 31 are described, together with structure-activity relationships for related analogues [3].
  • Intradermal injections of the NK1 receptor agonist GR73632 produced dose-dependent scratching, while the NK2 agonist GR64349 and the NK3 agonist senktide were without effects [4].
  • 5. Background activity was significantly enhanced by GR73632, GR64349, SP and NKA but not by senktide or NKB [5].
  • By contrast, the selective NK-2 and NK-3 receptor agonists, GR64349 and [MePhe7]NKB, produced concentration-dependent pressor responses and were more potent than SP (116 +/- 8 and 134 +/- 15 mm Hg increases in PP at 33.3 nmol, respectively).(ABSTRACT TRUNCATED AT 250 WORDS)[6]
  • In vivo, in the anaesthetised guinea-pig, GR159897 (0.12 i.v.) potently antagonised bronchoconstriction induced by GR64349 (dose-ratio = 28), with a long duration of action (3 h) [7].

Gene context of GR64349

  • However, only the NK-2 receptor agonist, GR64349, inhibited drinking without producing other behavioural effects [8].
  • GR73632 (0.1 and 0.3 nmol/kg) and GR64349 (0.3 nmol/kg), but not h.alpha CGRP (0.01-0.3 nmol/kg) or substance P(0.01-1.0 nmol/kg), then produced a more prolonged increase in CBF, the peak effect occurring 10-15 min after injection [9].
  • In contrast, in RbT, only NKA and the selective NK2-receptor agonist, GR64349 were potent, indicating the presence of NK2-receptors [10].
  • However, in GPT both NK1- and NK2-receptors appear to mediate contraction to NKs since NKA, GR73632 and GR64349 were highly potent and SP and SPOMe moderately potent agonists [10].

Analytical, diagnostic and therapeutic context of GR64349

  • Prominent increases in ventricular contractility and perfusion pressure also occurred with 32 nmol of GR64349 (25 +/- 6 and 33 +/- 4%, respectively). ¿Sar(9), Met(O(2))(11)SP was unique in having a high potency for decreasing ventricular contractility and perfusion pressure [1].


  1. Tachykinin receptor subtypes in the isolated guinea pig heart and their role in mediating responses to neurokinin A. Chang, Y., Hoover, D.B., Hancock, J.C., Smith, F.M. J. Pharmacol. Exp. Ther. (2000) [Pubmed]
  2. Behavioural consequences following infusion of selective neurokinin agonists into the median raphe nucleus of the rat. Mason, G.S., Elliott, P.J. Neuropharmacology (1992) [Pubmed]
  3. Conformationally constrained tachykinin analogues: potent and highly selective neurokinin NK-2 receptor agonists. Deal, M.J., Hagan, R.M., Ireland, S.J., Jordan, C.C., McElroy, A.B., Porter, B., Ross, B.C., Stephens-Smith, M., Ward, P. J. Med. Chem. (1992) [Pubmed]
  4. Substance P induction of itch-associated response mediated by cutaneous NK1 tachykinin receptors in mice. Andoh, T., Nagasawa, T., Satoh, M., Kuraishi, Y. J. Pharmacol. Exp. Ther. (1998) [Pubmed]
  5. Modulation of excitatory amino acid responses by tachykinins and selective tachykinin receptor agonists in the rat spinal cord. Cumberbatch, M.J., Chizh, B.A., Headley, P.M. Br. J. Pharmacol. (1995) [Pubmed]
  6. Pharmacological characterization of the pressor response to tachykinins in isolated perfused rat kidney. Chen, Y., Hoover, D.B. J. Pharmacol. Exp. Ther. (1993) [Pubmed]
  7. GR159897, a potent non-peptide antagonist at tachykinin NK2 receptors. Beresford, I.J., Sheldrick, R.L., Ball, D.I., Turpin, M.P., Walsh, D.M., Hawcock, A.B., Coleman, R.A., Hagan, R.M., Tyers, M.B. Eur. J. Pharmacol. (1995) [Pubmed]
  8. Role of NK-2 receptors in the antidipsogenic activity of neurokinins in the mouse. Walsh, D.M., Elliott, P.J., Hagan, R.M. Gen. Pharmacol. (1992) [Pubmed]
  9. The influence of neurokinins and calcitonin gene-related peptide on cerebral blood flow in anaesthetized guinea-pigs. Beattie, D.T., McNeil, D.K., Connor, H.E. Neuropeptides (1993) [Pubmed]
  10. Characterisation of the neurokinin receptors mediating contraction of isolated tracheal preparations from a variety of species. Sheldrick, R.L., Ball, D.I., Coleman, R.A. Agents Actions Suppl. (1990) [Pubmed]
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