141636-65-9

141636-65-9 structure

Name: GR 94800 TFA
Chemical Name: (2S)-N-[(2S)-1-amino-1-oxohexan-2-yl]-1-[(2R)-1-[(2S)-2-[[(2R)-2-[[(2S)-2-[[(2S)-2-benzamidopropanoyl]amino]propanoyl]amino]-3-(1H-indol-3-yl)propanoyl]amino]-3-phenylpropanoyl]pyrrolidine-2-carbonyl]pyrrolidine-2-carboxamide
CAS Number: 141636-65-9
Molecular Formula: C₄₉H₆₁N₉O₈
Molecular Weight: 904.06400
Catalog: Signaling Pathways GPCR/G Protein Neurokinin Receptor
Create Date: 2017-10-14 01:33:27
Modify Date: 2024-01-16 14:14:14
GR 94800 is a potent and selective NK2 receptor peptide antagonist, with pKB values of 9.6, 6.4 and 6.0 for NK2, NK1 and NK3 receptors, respectively[1][2].

Name	(2S)-N-[(2S)-1-amino-1-oxohexan-2-yl]-1-[(2R)-1-[(2S)-2-[[(2R)-2-[[(2S)-2-[[(2S)-2-benzamidopropanoyl]amino]propanoyl]amino]-3-(1H-indol-3-yl)propanoyl]amino]-3-phenylpropanoyl]pyrrolidine-2-carbonyl]pyrrolidine-2-carboxamide
Synonyms	Chlor-essigsaeure-phenylester Acetic acid,chloro-,phenyl este chloro-aceticaciphenylester chloroacetic acid phenyl ester Phenyl-chloracetat Chloracetoxy-benzol Acetic acid,chloro-,phenyl ester Phenyl-CO-Ala-Ala-D-Trp-Phe-D-Pro-Pro-Nle-NH2 Phenylchloroacetate PhCO-Ala-Ala-D-Trp-Phe-D-Pro-Pro-NleNH2 Phenyl cholroacetate

Description	GR 94800 is a potent and selective NK2 receptor peptide antagonist, with pKB values of 9.6, 6.4 and 6.0 for NK2, NK1 and NK3 receptors, respectively[1][2].
Related Catalog	Signaling Pathways >> Neuronal Signaling >> Neurokinin Receptor Research Areas >> Neurological Disease Signaling Pathways >> GPCR/G Protein >> Neurokinin Receptor
In Vitro	Responses to EFS (15 Hz) were significantly reduced by the NK2 receptor antagonist GR 94800 (1 μM) either alone or in combination with the NK1 antagonist (1 μM)[3].
References	[1]. A B McElroy, et al. Highly potent and selective heptapeptide antagonists of the neurokinin NK-2 receptor. J Med Chem. 1992 Jul 10;35(14):2582-91. [2]. M A Matuszek, et al. An investigation of tachykinin NK2 receptor subtypes in the rat. Eur J Pharmacol. 1998 Jul 3;352(1):103-9. [3]. Stephen D Tichenor, et al. Excitatory motor innervation in the canine rectoanal region: role of changing receptor populations. Br J Pharmacol. 2002 Dec;137(8):1321-9.