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pGlu-Ala-Asp-Pro-Asn-Lys-Phe-Tyr-Pro(spiro-γ-lactam-Leu-Trp-NH2

用途

GR 82334 是一种有效的、特异性的可逆速激蛋白 NK1 受体 (tachykinin NK1 receptor) 拮抗剂。GR 82334 通过阻断 NK1 受体的作用,抑制大鼠神经肽 P 物质诱导的致敏作用。

名称

[ CAS 号 ]:
129623-01-4

[ 中文名 ]:
pGlu-Ala-Asp-Pro-Asn-Lys-Phe-Tyr-Pro(spiro-γ-lactam-Leu-Trp-NH2

[ 英文名 ]:
GR 82334

生物活性

[ 描述 ]:

[ 相关类别 ]:

信号通路 >> 其他 >> 其他

研究领域 >> 神经疾病

[体内研究]

GR 82334(鞘内给药；0.1 nmol-1 nmol)在1 nmol但不在0.1 nmol时刺激大鼠无名膀胱,并且局部应用辣椒素(4μg/50μl)可降低反射性化学伤害性[1]。GR 82334(10 nM-1µM；在椎骨L4和L5之间注射)在10 nM处对两种动物都没有影响,在剂量>100 nM时增加小鼠热诱导的足部退缩潜伏期,但在裸鼹鼠中没有这种增加,剂量>100 nM引起潜伏期缩短的趋势[2]。动物模型：3-6月龄雄性C57BL/6小鼠和6-18月龄裸鼹鼠[2]剂量：10nm,100nm,1µM给药：L4和L5椎骨间注射。结果：小鼠热诱导的足退缩潜伏期增加。

[参考文献]

[1]. A Lecci,et al.Effect of the NK-1 receptor antagonist GR 82,334 on reflexly-induced bladder contractions. Life Sci

[2]. Antje Brand, et al. Functional neurokinin and NMDA receptor activity in an animal naturally lacking substance P: the naked mole-rat.PLoS One. 2010 Dec 21;5(12):e15162.

物理化学性质

[ 分子式 ]:
C₆₉H₉₁N₁₅O₁₆

[ 分子量 ]:
1386.55000

[ 精确质量 ]:
1385.68000

[ PSA ]:
479.25000

[ LogP ]:
3.53680

安全信息

[ 个人防护装备 ]:
Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter

[ 危险品运输编码 ]:
NONH for all modes of transport

文献

Effect of tachykinins on ascending and descending reflex pathway in rat small intestine.

Acta Pharmacol. Sin. 23(4) , 289-95, (2002)

To examine the effect of tachykinins on the ascending reflex pathway in rat small intestine, we used different selective neurokinin (NK) receptor antagonists (RA): a) NK1-RA: GR-82334 and CP-96.345, b...

Substance P modulates localized calcium transients and membrane current responses in murine colonic myocytes.

Br. J. Pharmacol. 138(7) , 1233-43, (2003)

1. Neurokinins contribute to the neural regulation of gastrointestinal (GI) smooth muscles. We studied responses of murine colonic smooth muscle cells to substance P (SP) and NK(1) and NK(2) agonists ...

Characterization of receptors for two Xenopus gastrointestinal tachykinin peptides in their species of origin.

Naunyn Schmiedebergs Arch. Pharmacol. 370(1) , 35-45, (2004)

Two tachykinin peptides, bufokinin and Xenopus neurokinin A (X-NKA) were recently isolated from Xenopus laevis. In this study we investigated the tachykinin receptors in the Xenopus gastrointestinal t...

更多文献

pGlu-Ala-Asp-Pro-Asn-Lys-Phe-Tyr-Pro(spiro-γ-lactam-Leu-Trp-NH2

用途

名称

生物活性

物理化学性质

安全信息

文献

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