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Chemical Compound Review

Septide     (2S)-N-[(1S)-1-[[(2S)-1- [(2S)-2-[[(1S)-1...

Synonyms: LS-91363, CTK8D4751, DNC001128, DNC001321, AR-1G9331, ...
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Disease relevance of Septide

  • SPOME (100-300 nM) inhibited peristalsis by a rise of the pressure threshold at which peristaltic waves were triggered, whereas septide and GR-73 632 (30-300 nM) interrupted peristalsis by causing circular muscle spasms [1].
  • Binding experiments performed with [(125)I]-NKA allowed us to demonstrate the presence of "septide-sensitive" specific binding sites on membranes from rat CHO cells transfected with the NK(1) receptor cDNA (CHO-rat-NK1 cells), human astrocytoma U373 MG, or mouse cortical astrocytes, cells which express NK(1) but neither NK(2) nor NK(3) receptors [2].
  • The selectivity of this compound for the latter receptor was confirmed by its failure to affect SP- or septide-induced hypotension in either guinea pigs or rats [3].
  • Intravenous administration of the undecapeptide [Sar9]substance P (SP) sulfone (1.5 nmol/kg) and the hexapeptide [Glp6,Pro9]SP(6-11) (septide; 0.4 nmol/kg) produced a comparable (about 30-40% of maximal effect) increase of insufflation pressure (bronchospasm) in anesthetized guinea-pigs [4].
  • These findings confirm that tachykinins mediate edema formation via the NK(1) receptor and provide direct evidence that the septide-sensitive binding site is on the NK(1) receptor [5].

High impact information on Septide


Biological context of Septide

  • However, ALIE-124 stimulated phosphatidylinositol hydrolysis, as previously shown for septide-like peptides [8].
  • SR 140333 blocked the stimulatory effect of this agonist (10(-7) M) with an IC50 of 1.6 x 10(-9) M, whereas the effect of another NK1 agonist, septide (EC50 = 1.5 x 10(-8) M) was antagonized with an IC50 of 2.1 x 10(-10) M [9].
  • Dose-response curves showed that septide was a more potent bronchoconstrictor than [Sar(9),Met(O(2))(11)]SP to cause bronchoconstriction [10].
  • 4. All antagonists except LY303241 blocked dose-dependently the increases in vascular permeability to equipotent doses of [Sar9, Met(O2)11]SP and septide [11].
  • 4. The NK1r antagonists, CP-99994 (2S,3S)-3-(2-methoxybenzyl)amino-2-phenylpiperidine dihydrochloride and MEN-10581, cyclo(Leu,[CH2NH]Lys(benzyloxycarbonyl)-Gln-Trp-Phe-betaAla) were both more potent in inhibiting endocytosis (50 x and 8 x greater respectively) against septide than against SP [12].

Anatomical context of Septide

  • The hexapeptide [pGlu6,Pro9]substance P (SP)6-11, septide, has been shown to be an agonist as potent as SP in eliciting smooth muscle contraction in several in vitro preparations, while being a poor competitor of labeled SP binding [13].
  • Septide was a weak competitor of [3H]SP binding, with dissociation constants (Ki) of 2.9 +/- 0.6 microM and 3.7 +/- 0.9 microM for membranes and intact transfected cells, respectively [13].
  • Our data indicate that in rat parotid gland, the existence of a specific "septide-sensitive" receptor can be ruled out and that only the NK1 receptor is present and mediates cellular responses [14].
  • 6. The NK2 receptor antagonists, GR 94,800 and SR 48,968 selectively antagonized the response to [beta Ala8]NKA(4-10) without affecting that to [Sar9]SP sulphone or septide in the ileum and colon [15].
  • 3. In a number of spinal cord neurones (n = 17) only septide induced a membrane depolarization while DiMe-C7 elicited no response [16].

Associations of Septide with other chemical compounds

  • RP67580 is apparently as potent at antagonizing septide, SP, or SP(4-11) (in all cases KB = 3 nM) [14].
  • Increasing the dose of RP 67,580 3 fold resulted in inhibition of the response to SP (0.2 nmol) and [Sar9]SP sulphone (0.002 nmol) by approximately 66% and 64% respectively with the response to septide being inhibited by approximately 70%.(ABSTRACT TRUNCATED AT 250 WORDS)[17]
  • In contrast, (D-Arg1, D-Pro2,4, D-Phe7, D-His9)-SP (0.5-1.0 nmol) and (D-Phe7, D-His9)-SP (6-11) (0.5-2.0 nmol) inhibited only SP-induced behavioral response, but not physalaemin- or septide-induced response [18].
  • The tachykinin NK1 and NK3 receptor agonists septide and senktide, respectively, were ineffective [19].
  • The analog [pGlu6,Pro9] SP(6-11) (septide) may also act on atypical NK-1 receptors in guinea pig ileum [20].

Gene context of Septide

  • 2. The synthetic tachykinin receptor agonists, septide (pD2 7.87) and [Sar9]substance P (SP) sulphone (pD2 7.64) produced concentration-dependent contractions of the rat isolated urinary bladder [21].
  • 1. The NK1 tachykinin receptor agonists, septide, [Sar9,Met(O2)11]SP and [Pro9]SP produced locomotor hyperactivity (10-20 min) when injected intracerebroventricularly (i.c.v.) in the guinea-pig [22].
  • When administered simultaneously with NK-1 receptor agonists, a putative SP antagonist, spantide inhibited SP-, physalaemin- and septide-induced behavioral response in a dose-dependent manner with ED50 values of 1.0, 0.65 and 1.3 nmol/mouse, respectively [18].
  • 1. Following the recent proposal that the selective agonist septide, ([pGlu6,Pro9]SP(6-11)), acts on a novel tachykinin receptor distinct from the 'classical' NK1 receptor, the aim of the study was to investigate the possible heterogeneity of tachykinin NK1 receptors in the rat urinary bladder [21].
  • Septide, an agonist with a low affinity for NK-1 binding sites, [Sar9, Met(O2)11]SP and to a lesser extent [Pro9]SP, two potent and selective NK-1 agonists were the most effective drugs in stimulating these behaviours [23].

Analytical, diagnostic and therapeutic context of Septide

  • Therefore, following the blockade of tachykinin NK1, NK2 and septide-sensitive receptors, the accumulation of inositol monophosphate appears to be a valuable, rapid and sensitive bioassay for determining the activity of NK3 receptor agonists and putative NK3 receptor antagonists [24].


  1. Differences in circular muscle contraction and peristaltic motor inhibition caused by tachykinin NK1 receptor agonists in the guinea-pig small intestine. Shahbazian, A., Holzer, P. Neurogastroenterol. Motil. (2000) [Pubmed]
  2. Further evidence for the presence of "septide-sensitive" tachykinin binding sites in tissues possessing solely NK(1) tachykinin receptors. Torrens, Y., Beaujouan, J.C., Saffroy, M., Glowinski, J. Biochem. Biophys. Res. Commun. (2000) [Pubmed]
  3. Pharmacological evidence that NK-2 tachykinin receptors mediate hypotension in the guinea pig but not in the rat. Floch, A., Thiry, C., Cavero, I. Fundamental & clinical pharmacology. (1996) [Pubmed]
  4. In vivo evidence for the activation of a septide-sensitive tachykinin receptor in guinea pig bronchoconstriction. Boni, P., Maggi, C.A., Evangelista, S. Life Sci. (1994) [Pubmed]
  5. Use of NK(1) knockout mice to analyze substance P-induced edema formation. Cao, T., Gerard, N.P., Brain, S.D. Am. J. Physiol. (1999) [Pubmed]
  6. The 'septide-sensitive' tachykinin receptor: still an enigma. Glowinski, J. Trends Pharmacol. Sci. (1995) [Pubmed]
  7. Neurokinin receptors differentially mediate endogenous acetylcholine release evoked by tachykinins in the neostriatum. Arenas, E., Alberch, J., Perez-Navarro, E., Solsona, C., Marsal, J. J. Neurosci. (1991) [Pubmed]
  8. 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]
  9. SR 140333, a novel, selective, and potent nonpeptide antagonist of the NK1 tachykinin receptor: characterization on the U373MG cell line. Oury-Donat, F., Lefevre, I.A., Thurneyssen, O., Gauthier, T., Bordey, A., Feltz, P., Emonds-Alt, X., Le Fur, G., Soubrie, P. J. Neurochem. (1994) [Pubmed]
  10. Role of nitric oxide and septide-insensitive NK(1) receptors in bronchoconstriction induced by aerosolised neurokinin A in guinea-pigs. Ricciardolo, F.L., Trevisani, M., Geppetti, P., Nadel, J.A., Amadesi, S., Bertrand, C. Br. J. Pharmacol. (2000) [Pubmed]
  11. Characterization of central and peripheral effects of septide with the use of five tachykinin NK1 receptor antagonists in the rat. Cellier, E., Barbot, L., Iyengar, S., Couture, R. Br. J. Pharmacol. (1999) [Pubmed]
  12. Two affinities for a single antagonist at the neuronal NK1 tachykinin receptor: evidence from quantitation of receptor endocytosis. Jenkinson, K.M., Southwell, B.R., Furness, J.B. Br. J. Pharmacol. (1999) [Pubmed]
  13. Septide: an agonist for the NK1 receptor acting at a site distinct from substance P. Pradier, L., Ménager, J., Le Guern, J., Bock, M.D., Heuillet, E., Fardin, V., Garret, C., Doble, A., Mayaux, J.F. Mol. Pharmacol. (1994) [Pubmed]
  14. A "septide-sensitive" receptor is not involved in tachykinin-mediated secretory and inositol phosphate responses in rat parotid gland: are several transduction pathways involved after the stimulation of the NK1 receptor? Huleux, C., Berthier, A., Rossignol, B., Dreux, C. J. Neurochem. (1998) [Pubmed]
  15. Comparison of tachykinin NK1 and NK2 receptors in the circular muscle of the guinea-pig ileum and proximal colon. Maggi, C.A., Patacchini, R., Meini, S., Quartara, L., Sisto, A., Potier, E., Giuliani, S., Giachetti, A. Br. J. Pharmacol. (1994) [Pubmed]
  16. Effects of receptor-selective neurokinin agonists and a neurokinin antagonist on the electrical activity of spinal cord neurones in culture. Wienrich, M., Reuss, K., Harting, J. Br. J. Pharmacol. (1989) [Pubmed]
  17. Demonstration of a 'septide-sensitive' inflammatory response in rat skin. Ahluwalia, A., Giuliani, S., Maggi, C.A. Br. J. Pharmacol. (1995) [Pubmed]
  18. Differential effects of substance P analogs on neurokinin 1 receptor agonists in the mouse spinal cord. Sakurada, T., Yamada, T., Tan-no, K., Manome, Y., Sakurada, S., Kisara, K., Ohba, M. J. Pharmacol. Exp. Ther. (1991) [Pubmed]
  19. Excitatory motor and electrical effects produced by tachykinins in the human and guinea-pig isolated ureter and guinea-pig renal pelvis. Patacchini, R., Santicioli, P., Zagorodnyuk, V., Lazzeri, M., Turini, D., Maggi, C.A. Br. J. Pharmacol. (1998) [Pubmed]
  20. Use of selective antagonists for further characterization of tachykinin NK-2, NK-1 and possible "septide-selective" receptors in guinea pig bronchus. Zeng, X.P., Burcher, E. J. Pharmacol. Exp. Ther. (1994) [Pubmed]
  21. Tachykinin NK1 receptor subtypes in the rat urinary bladder. Meini, S., Patacchini, R., Maggi, C.A. Br. J. Pharmacol. (1994) [Pubmed]
  22. 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]
  23. Differential ability of tachykinin NK-1 and NK-2 agonists to produce scratching and grooming behaviours in mice. Ravard, S., Betschart, J., Fardin, V., Flamand, O., Blanchard, J.C. Brain Res. (1994) [Pubmed]
  24. A new selective bioassay for tachykinin NK3 receptors based on inositol monophosphate accumulation in the guinea pig ileum. Petitet, F., Saffroy, M., Torrens, Y., Glowinski, J., Beaujouan, J.C. Eur. J. Pharmacol. (1993) [Pubmed]
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