Boc-Ala-Ala-D-Trp-Phe-D-Pro-Pro-NleNH2

Names

[ Name ]:
Boc-Ala-Ala-D-Trp-Phe-D-Pro-Pro-NleNH2

[Synonym ]:
boc-ala-ala-d-trp-phe-d-pro-pro-nle-nh2

Biological Activity

[Description]:

GR 87389 is a potent NK2 receptor antagonist. GR 87389 antagonized GA 64349-induced smooth muscle strips contractions in a competitive manner in the human detrusor, prostate and prostatic urethra[1][2].

[Related Catalog]:

Signaling Pathways >> Neuronal Signaling >> Neurokinin Receptor

Research Areas >> Neurological Disease

Signaling Pathways >> GPCR/G Protein >> Neurokinin Receptor

[Target]

NK2

[In Vitro]

GR 87389 是一种非肽和肽速激肽拮抗剂，对海马、膀胱和十二指肠的 Ki 值分别为 4.0、5.2 和 14 nM[1]。 GR 87389 (30-300 nM) 拮抗 GA 64349 诱导的人类逼尿肌、前列腺和前列腺尿道平滑肌条收缩[2]。

[References]

[1]. Saffroy M, et, al. Presence of NK2 binding sites in the rat brain. J Neurochem. 2001 Dec;79(5):985-96.

[2]. Palea S, et, al. Pharmacological characterization of tachykinin NK2 receptors on isolated human urinary bladder, prostatic urethra and prostate. J Pharmacol Exp Ther. 1996 May;277(2):700-5.

Chemical & Physical Properties

[ Molecular Formula ]:
C₄₇H₆₅N₉O₉

[ Molecular Weight ]:
900.07400

[ Exact Mass ]:
899.49100

[ PSA ]:
254.23000

[ LogP ]:
5.01350

Related Compounds

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