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GR-73632

GR-73632用途

GR-73632 是新型速激肽神经激肽1 (NK-1) 受体激动剂。GR-73632 通过传递瘙痒信号的 NK1 受体直接作用于初级感觉神经元的外周末端。

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GR-73632名称

[ CAS 号 ]:
133156-06-6

[ 英文名 ]:
GR 73632

[英文别名 ]:

GR-73632

GR-73632生物活性

[ 描述 ]:

GR-73632 是新型速激肽神经激肽1 (NK-1) 受体激动剂。GR-73632 通过传递瘙痒信号的 NK1 受体直接作用于初级感觉神经元的外周末端。

[ 相关类别 ]:

信号通路 >> 神经信号通路 >> 神经激肽受体

研究领域 >> 神经疾病

信号通路 >> G 蛋白偶联受体/G 蛋白 >> 神经激肽受体

[ 靶点 ]

IC50: NK-1 receptor[1]

[参考文献]

[1]. Sakurada C, et al. Spinal actions of GR73632, a novel tachykinin NK1 receptor agonist. Peptides. 1999;20(2):301-4.

[2]. Costantini VJ, et al. The NK1 receptor antagonist aprepitant attenuates NK1 agonist-induced scratching behaviour in the gerbil after intra-dermal, topical or oral administration. Exp Dermatol. 2015 Apr;24(4):312-4.

GR-73632物理化学性质

[ 密度 ]:
1.198g/cm3

[ 沸点 ]:
1082.2ºC at 760mmHg

[ 分子式 ]:
C₄₀H₅₉N₇O₆S

[ 分子量 ]:
766.00500

[ 闪点 ]:
608.3ºC

[ 精确质量 ]:
765.42500

[ PSA ]:
222.33000

[ LogP ]:
4.66890

[ 蒸汽压 ]:
0mmHg at 25°C

[ 折射率 ]:
1.576

[ 储存条件 ]:
-20°C，密封，干燥

GR-73632安全信息

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

[ 安全声明 (欧洲) ]:
S22

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

GR-73632文献

Neurokinin receptor modulation of respiratory activity in the rabbit.

Eur. J. Neurosci. 27(12) , 3233-43, (2008)

The respiratory role of neurokinin (NK) receptors was investigated in alpha-chloralose-urethane-anaesthetized, vagotomized, paralysed and artificially ventilated rabbits by using bilateral microinject...

Phosphorylation of TRPV1 by neurokinin-1 receptor agonist exaggerates the capsaicin-mediated substance P release from cultured rat dorsal root ganglion neurons.

Neuropharmacology 55(8) , 1405-11, (2008)

The present study was conducted to determine whether the activation of neurokinin-1 receptor (NK-1R) by its agonist (GR73632) enhances the capsaicin-evoked substance P (SP) release using a radioimmuno...

Calcitonin gene-related peptide and substance P regulate the intestinal radiation response.

Clin. Cancer Res. 12(13) , 4112-8, (2006)

Intestinal toxicity is important in the therapeutic use of radiation as well as in nontherapeutic radiation exposure scenarios. Enteric sensory nerves are critical for mucosal homeostasis and for an a...

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