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Chemical Compound Review

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

Synonyms: CHEMBL106124, SureCN5238634, CHEBI:276891, LS-96168, CTK8E9092, ...
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Disease relevance of Senktide

  • Conversely, intrathecal senktide (10 nmol) induced thermal hyperalgesia, indicated by decreased withdrawal latency to radiant heat [1].
  • R116301 did not affect senktide-induced miosis (>5 mg/kg, s.c.) in rabbits, confirming the absence of an interaction with the NK(3) receptor [2].
  • 2. Tachycardia was elicited by the NK(1) ([Sar(9),Met(O(2))(11)]SP) and NK(2) ([betaAla(8)]NKA(4-10)) agonists at 25 and 100 pmol while the NK(3) agonist (senktide, 50 and 100 pmol) had no significant effect [3].
  • The ID injection of the selective NK1, SP methyl-ester (1-30 nmol), NK2, [beta-Ala8]-neurokinin A4-10) (beta-Ala, 0.3-30 nmol), or NK3, senktide (1-10 nmol) agonists, caused extensive edema formation with mean ED50s of 0.48 nmol, 0.41 nmol, and 0.18 nmol, respectively [4].
  • The microinjection of 1-10 ng of suc-[Asp5, Me-Phe8]-SP(6-11) (senktide, a selective neurokinin B receptor peptide) into the NTS caused long-lasting hypertension and tachycardia [5].

Psychiatry related information on Senktide

  • 2. Wet-dog shakes, but not locomotor activity, elicited by senktide i.c.v. were significantly reduced by SR142801 but not by SR142806, confirming the involvement of NK3 tachykinin receptors in wet-dog shake behaviour [6].
  • The effects of intracerebroventricular injections of the neurokinin-2 (NK-2) receptor agonist neurokinin A and the neurokinin-3 (NK-3) receptor agonist senktide on scopolamine (sc)-induced amnesia were investigated based on spontaneous alternation performance in mice [7].

High impact information on Senktide


Chemical compound and disease context of Senktide


Biological context of Senktide


Anatomical context of Senktide


Associations of Senktide with other chemical compounds

  • The rank order of tachykinin peptides competing for [3H]senktide binding at the NK-3 receptor homolog was [MePhe7]neurokinin B > senktide > substance P = neurokinin A > neurokinin B [9].
  • These compounds, namely septide [( pGlu6, Pro9]substance P6-11 hexapeptide), which preferentially acts on the NK-1 (SP-P) receptor, and senktide (succinyl-[Asp6,Me-Phe8] substance P (6-11) hexapeptide), which selectively acts on the NK-3 (or SP-N) receptor, were now used to identify the tachykinin receptors present in several smooth muscle systems [20].
  • 5. MEN 10,627 inhibited the response to [beta-Ala8]NKA 4-10 but not to SP, SPME, NKA, NKB or senktide [21].
  • Septide as well as senktide were found to be devoid of activity in the electrically stimulated rat vas deferens, showing that, in this preparation, which is the prototype NK-2 (or SP-E) system, tachykinin-induced contraction is not mediated via NK-1 or NK-3 receptors [20].
  • The NK-3 tachykinin receptor agonist senktide elicits 5-HT-mediated behaviour following central or peripheral administration in mice and rats [22].

Gene context of Senktide

  • GR64349 and senktide (agonists at NK2 and NK3 receptors respectively) also inhibited K+ currents, but only at concentrations which were several orders of magnitude greater than GR73632, suggesting that current inhibition was mediated via NK1 receptors [23].
  • Both NK-1 (GR73632) and NK-3 (senktide) agonists induced a variety of behavioural effects which appeared to compete with the drinking response [24].
  • Neurokinin A (0.1-3 micrograms) or senktide (0.0003-0.03 microgram) alone did not influence either spontaneous alternation performance or total arm entries [7].
  • 4. The NK3 tachykinin receptor agonist, senktide, contrasts with the NK1 receptor agonists in that it elicited only wet-dog shakes, at doses ranging from 0.32 to 1.25 micrograms [25].
  • In contrast, the NK3-selective hexapeptide, senktide, was recognized only when transmembrane segment III and IV from the NK3 receptor were incorporated into the chimeric constructs [26].

Analytical, diagnostic and therapeutic context of Senktide


  1. Spinal neurokinin3 receptors mediate thermal but not mechanical hyperalgesia via nitric oxide. Linden, D.R., Seybold, V.S. Pain (1999) [Pubmed]
  2. Pharmacological profile of (2R-trans)-4-[1-[3,5-bis(trifluoromethyl)benzoyl]-2-(phenylmethyl)-4-piperidinyl]-N-(2,6-dimethylphenyl)-1-acetamide (S)-Hydroxybutanedioate (R116301), an orally and centrally active neurokinin-1 receptor antagonist. Megens, A.A., Ashton, D., Vermeire, J.C., Vermote, P.C., Hens, K.A., Hillen, L.C., Fransen, J.F., Mahieu, M., Heylen, L., Leysen, J.E., Jurzak, M.R., Janssens, F. J. Pharmacol. Exp. Ther. (2002) [Pubmed]
  3. Implication of nigral tachykinin NK3 receptors in the maintenance of hypertension in spontaneously hypertensive rats: a pharmacologic and autoradiographic study. Lessard, A., Campos, M.M., Neugebauer, W., Couture, R. Br. J. Pharmacol. (2003) [Pubmed]
  4. Receptor subtypes involved in tachykinin-mediated edema formation. Alves, R.V., Campos, M.M., Santos, A.R., Calixto, J.B. Peptides (1999) [Pubmed]
  5. Cardiovascular roles of tachykinin peptides in the nucleus tractus solitarii of rats. Nagashima, A., Takano, Y., Tateishi, K., Matsuoka, Y., Hamaoka, T., Kamiya, H. Brain Res. (1989) [Pubmed]
  6. Localization of Fos-like immunoreactivity induced by the NK3 tachykinin receptor agonist, senktide, in the guinea-pig brain. Yip, J., Chahl, L.A. Br. J. Pharmacol. (1997) [Pubmed]
  7. Neurokinin A and senktide attenuate scopolamine-induced impairment of spontaneous alternation performance in mice. Ukai, M., Shinkai, N., Kameyama, T. Nihon shinkei seishin yakurigaku zasshi = Japanese journal of psychopharmacology. (1996) [Pubmed]
  8. Role of neurokinin 3 receptors on responses to colorectal distention in the rat: electrophysiological and behavioral studies. Julia, V., Su, X., Buéno, L., Gebhart, G.F. Gastroenterology (1999) [Pubmed]
  9. Functional expression of a novel human neurokinin-3 receptor homolog that binds [3H]senktide and [125I-MePhe7]neurokinin B, and is responsive to tachykinin peptide agonists. Krause, J.E., Staveteig, P.T., Mentzer, J.N., Schmidt, S.K., Tucker, J.B., Brodbeck, R.M., Bu, J.Y., Karpitskiy, V.V. Proc. Natl. Acad. Sci. U.S.A. (1997) [Pubmed]
  10. High affinity binding of [3H]propionyl-[Met(O2)11]substance P(7-11), a tritiated septide-like peptide, in Chinese hamster ovary cells expressing human neurokinin-1 receptors and in rat submandibular glands. Sagan, S., Beaujouan, J.C., Torrens, Y., Saffroy, M., Chassaing, G., Glowinski, J., Lavielle, S. Mol. Pharmacol. (1997) [Pubmed]
  11. Priming effects of substance P on calcium changes evoked by interleukin-8 in human neutrophils. Dianzani, C., Lombardi, G., Collino, M., Ferrara, C., Cassone, M.C., Fantozzi, R. J. Leukoc. Biol. (2001) [Pubmed]
  12. Interaction of the tachykinin NK3 receptor agonist senktide with behavioral effects of cocaine in marmosets (Callithrix penicillata). de Souza Silva, M.A., Mello, E.L., Müller, C.P., Jocham, G., Maior, R.S., Huston, J.P., Tomaz, C., Barros, M. Peptides (2006) [Pubmed]
  13. Different subtypes of tachykinin NK(1) receptor binding sites are present in the rat brain. Beaujouan, J.C., Saffroy, M., Torrens, Y., Glowinski, J. J. Neurochem. (2000) [Pubmed]
  14. Electrophysiological effects of tachykinins and capsaicin on guinea-pig bronchial parasympathetic ganglion neurones. Myers, A.C., Undem, B.J. J. Physiol. (Lond.) (1993) [Pubmed]
  15. Spinal neurokin3 receptors facilitate the nociceptive flexor reflex via a pathway involving nitric oxide. Linden, D.R., Jia, Y.P., Seybold, V.S. Pain (1999) [Pubmed]
  16. Use of a dipeptide chemical library in the development of non-peptide tachykinin NK3 receptor selective antagonists. Boden, P., Eden, J.M., Hodgson, J., Horwell, D.C., Hughes, J., McKnight, A.T., Lewthwaite, R.A., Pritchard, M.C., Raphy, J., Meecham, K., Ratcliffe, G.S., Suman-Chauhan, N., Woodruff, G.N. J. Med. Chem. (1996) [Pubmed]
  17. Pharmacological characterization of ZD6021: a novel, orally active antagonist of the tachykinin receptors. Rumsey, W.L., Aharony, D., Bialecki, R.A., Abbott, B.M., Barthlow, H.G., Caccese, R., Ghanekar, S., Lengel, D., McCarthy, M., Wenrich, B., Undem, B., Ohnmacht, C., Shenvi, A., Albert, J.S., Brown, F., Bernstein, P.R., Russell, K. J. Pharmacol. Exp. Ther. (2001) [Pubmed]
  18. Distribution of Fos-like immunoreactivity within the rat brain following intraventricular injection of the selective NK(3) receptor agonist senktide. Smith, M.E., Flynn, F.W. J. Comp. Neurol. (2000) [Pubmed]
  19. Pharmacological examination of receptors mediating contractile responses to tachykinins in airways isolated from human, guinea pig and hamster. Ellis, J.L., Undem, B.J., Kays, J.S., Ghanekar, S.V., Barthlow, H.G., Buckner, C.K. J. Pharmacol. Exp. Ther. (1993) [Pubmed]
  20. Desensitization with a selective agonist discriminates between multiple tachykinin receptors. Laufer, R., Gilon, C., Chorev, M., Selinger, Z. J. Pharmacol. Exp. Ther. (1988) [Pubmed]
  21. Mediation of irregular spiking activity by multiple neurokinin-receptors in the small intestine of the rat. Lördal, M., Bränström, R., Hellström, P.M. Br. J. Pharmacol. (1998) [Pubmed]
  22. The NK-3 tachykinin receptor agonist senktide elicits 5-HT-mediated behaviour following central or peripheral administration in mice and rats. Stoessl, A.J., Dourish, C.T., Iversen, S.D. Br. J. Pharmacol. (1988) [Pubmed]
  23. Inhibition of Ca(2+)-sensitive K+ currents in NG 108-15 cells by substance P and related tachykinins. Phenna, S., Carpenter, E., Peers, C., Maudsley, S., Gent, J.P. Br. J. Pharmacol. (1996) [Pubmed]
  24. 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]
  25. Comparative behavioural profile of centrally administered tachykinin NK1, NK2 and NK3 receptor agonists in the guinea-pig. Piot, O., Betschart, J., Grall, I., Ravard, S., Garret, C., Blanchard, J.C. Br. J. Pharmacol. (1995) [Pubmed]
  26. Chimeric NK1 (substance P)/NK3 (neurokinin B) receptors. Identification of domains determining the binding specificity of tachykinin agonists. Gether, U., Johansen, T.E., Schwartz, T.W. J. Biol. Chem. (1993) [Pubmed]
  27. Intraventricular injections of tachykinin NK3 receptor agonist reduce the gain of the baroreflex in unrestrained rats. Flynn, F.W. Exp. Neurol. (2005) [Pubmed]
  28. Substance P in the dorsal motor nucleus of the vagus evokes gastric motor inhibition via neurokinin 1 receptor in rat. Krowicki, Z.K., Hornby, P.J. J. Pharmacol. Exp. Ther. (2000) [Pubmed]
  29. Neurokinin-1 and -3 receptor blockade inhibits slow excitatory synaptic transmission in myenteric neurons and reveals slow inhibitory input. Johnson, P.J., Bornstein, J.C. Neuroscience (2004) [Pubmed]
  30. Neurochemical mediators of the behavioural effects of receptor-selective substance P agonists administered intrathecally in the rat. Papir-Kricheli, D., Gilon, C., Chorev, M., Selinger, Z., Devor, M. Neuropharmacology (1990) [Pubmed]
  31. Central neurokinin 3 receptors increase systemic oxytocin release: interaction with norepinephrine. Bealer, S.L., Flynn, F.W. Exp. Neurol. (2003) [Pubmed]
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