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Chemical Compound Review

SureCN2141823     (2S)-N-[(1S)-1-[[(1S)-1- aminocarbonyl-3...

Synonyms: GR-73632, LS-91361, AC1L3P3N, GR 73632, 133156-06-6
 
 
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Disease relevance of GR-73632

  • Injections of the selective neurokinin-1 (NK-1) receptor agonist drug GR-73632 also caused bradycardia, however the rapid onset of agonist induced desensitization prevented an evaluation of potential effects on AV conduction in the iNA-VL [1].
 

High impact information on GR-73632

  • Ava[L-Pro9,N-MeLeu10] substance P(7-11) (GR 73632) and Sar9, Met(O2)11 increase distention-induced peristalsis through activation of neurokinin-1 receptors on smooth muscle and interstitial cells of cajal [2].
  • Activation of NK1 receptors by Ava[l-Pro(9),N-MeLeu10] substance P(7-11) (GR 73632) and Sar(9), Met(O(2))(11) on smooth muscle cells resulted in prolongation of the activity periods and increased action potential generation occurring superimposed on the intestinal slow wave activity [2].
  • In vivo central administration of HK-1 to gerbils and mice induced foot-tapping and scratching behaviors, respectively, similar to those observed following central administration of SP or the NK1 receptor agonist, GR-73632 [3].
  • In the prostatic urethra the rank order of agonist potency was GR 64349 > NKA-(4-10) > SP > GR 73632, whereas in the prostate it was: GR 64349 >> [beta Ala8 (NKA-(4-10)] > NKA-(4-10) > SP; GR 73632 was ineffective up to 30 microM [4].
  • Only the hyperpolarizing effects, which were in contrast mimicked by the specific NK1 receptor agonists GR 73632 and [Sar9, Met (O2)11]-SP, would be mediated by the few typical NK1 receptors which have been demonstrated in the medial vestibular nucleus [5].
 

Biological context of GR-73632

 

Anatomical context of GR-73632

  • Moreover, TAK-637 reduced the TTX-resistant component of the response to GR-73632 suggesting that NK(1) receptors expressed by epithelial cells are inhibited by TAK-637 [7].
  • ICV administration of 4.2 pmol of GR-73632 produced a rapid onset and sustained rCBV increase in several brain structures, such as the amygdala, the caudate putamen and the cortex [8].
 

Associations of GR-73632 with other chemical compounds

  • The other NK1 receptor agonists used, GR 73632, [Pro9]SP and septide, which did not interfere with the RIA, increased SP-LI basal outflow by 1807 +/- 713% (n = 3), 1259 +/- 160% (n = 3) and 620 +/- 69% (n = 3) at 10 nM, 1 nM and 1 microM, respectively.(ABSTRACT TRUNCATED AT 250 WORDS)[9]
  • Furthermore, GR 73632-induced hind paw tapping was significantly attenuated by co-administration of the peptide tachykinin NK1 receptor antagonist, GR 82334, or intravenous injection of CP-99,994 [10].
 

Gene context of GR-73632

  • The in vivo pharmacological profiles of the selective tachykinin NK1 receptor agonists, [Sar9,Met(O2)11]substance P and GR 73632, were examined in gerbils [10].
  • Moreover, GR 73632 increased the efflus of SP to a greater extent in the absence of peptidase inhibitors [11].
 

Analytical, diagnostic and therapeutic context of GR-73632

References

  1. What are the roles of substance P and neurokinin-1 receptors in the control of negative chronotropic or negative dromotropic vagal motoneurons? A physiological and ultrastructural analysis. Massari, V.J., Johnson, T.A., Gillis, R.A., Gatti, P.J. Brain Res. (1996) [Pubmed]
  2. Ava[L-Pro9,N-MeLeu10] substance P(7-11) (GR 73632) and Sar9, Met(O2)11 increase distention-induced peristalsis through activation of neurokinin-1 receptors on smooth muscle and interstitial cells of cajal. Nieuwmeyer, F., Ye, J., Huizinga, J.D. J. Pharmacol. Exp. Ther. (2006) [Pubmed]
  3. Centrally administered hemokinin-1 (HK-1), a neurokinin NK1 receptor agonist, produces substance P-like behavioral effects in mice and gerbils. Duffy, R.A., Hedrick, J.A., Randolph, G., Morgan, C.A., Cohen-Williams, M.E., Vassileva, G., Lachowicz, J.E., Laverty, M., Maguire, M., Shan, L.S., Gustafson, E., Varty, G.B. Neuropharmacology (2003) [Pubmed]
  4. Pharmacological characterization of tachykinin NK2 receptors on isolated human urinary bladder, prostatic urethra and prostate. Palea, S., Corsi, M., Artibani, W., Ostardo, E., Pietra, C. J. Pharmacol. Exp. Ther. (1996) [Pubmed]
  5. Effects of substance P on medial vestibular nucleus neurons in guinea-pig brainstem slices. Vibert, N., Serafin, M., Vidal, P.P., Muhlethaler, M. Eur. J. Neurosci. (1996) [Pubmed]
  6. Increased ganglionic responses to substance P in hypertensive rats due to upregulation of NK(1) receptors. Schoborg, R.V., Hoover, D.B., Tompkins, J.D., Hancock, J.C. Am. J. Physiol. Regul. Integr. Comp. Physiol. (2000) [Pubmed]
  7. Effects of TAK-637 on NK(1) receptor-mediated mechanisms regulating colonic secretion. Venkova, K., Greenwood-Van Meerveld, B. Toxicol. Appl. Pharmacol. (2004) [Pubmed]
  8. Functional magnetic resonance mapping of intracerebroventricular infusion of a neuroactive peptide in the anaesthetised rat. Gozzi, A., Schwarz, A.J., Reese, T., Crestan, V., Bertani, S., Turrini, G., Corsi, M., Bifone, A. J. Neurosci. Methods (2005) [Pubmed]
  9. Effect of the tachykinin NK1 receptor antagonists, RP 67580 and SR 140333, on electrically-evoked substance P release from rat spinal cord. Malcangio, M., Bowery, N.G. Br. J. Pharmacol. (1994) [Pubmed]
  10. Chromodacryorrhea and repetitive hind paw tapping: models of peripheral and central tachykinin NK1 receptor activation in gerbils. Bristow, L.J., Young, L. Eur. J. Pharmacol. (1994) [Pubmed]
  11. Characterization of substance P release from the intermediate area of rat thoracic spinal cord. Yang, L., Thomas, N.D., Helke, C.J. Synapse (1996) [Pubmed]
  12. NK1 receptors in the medial hypothalamus potentiate defensive rage behavior elicited from the midbrain periaqueductal gray of the cat. Bhatt, S., Gregg, T.R., Siegel, A. Brain Res. (2003) [Pubmed]
 
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