GR 94800

发表于由

GR 94800;

GR 94800 是有效的、选择性的神经激肽 2 (NK2) 受体的肽类拮抗剂，其对 NK2、NK1 和 NK3 受体的 pKB 值分别为 9.6、6.4 和 6.0。

GR 94800amp;;

GR 94800 Chemical Structure

CAS No. : 141636-65-9

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生物活性

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].

体外研究
(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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

904.06

Formula

C49H61N9O8
CAS 号

141636-65-9
Sequence Shortening

Bz-AA-{D-Trp}-F-{D-Pro}-P-{Nle}-NH2
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [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.