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GR 203040

GR 203040用途

GR203040 是一种具有口服活性的 NK1 受体拮抗剂,pKi 为 10.3。GR203040 显示出有效的止吐活性。

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GR 203040名称

[ CAS 号 ]:
168398-02-5

[ 英文名 ]:
GR 203040

[英文别名 ]:

GR 203040生物活性

[ 描述 ]:

GR203040 是一种具有口服活性的 NK1 受体拮抗剂,pKi 为 10.3。GR203040 显示出有效的止吐活性。

[ 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 ]

pKi: 10.3 (NK1 receptor)[1]

[参考文献]

[1]. Ward P, et al. Discovery of an orally bioavailable NK1 receptor antagonist, (2S,3S)-(2-methoxy-5-tetrazol-1-ylbenzyl)(2-phenylpiperidin-3-yl)amine (GR203040), with potent antiemetic activity. J Med Chem. 1995 Dec 22;38(26):4985-92.

GR 203040物理化学性质

[ 沸点 ]:
560.4ºC at 760mmHg

[ 分子式 ]:
C₂₀H₂₆Cl₂N₆O

[ 分子量 ]:
437.37

[ 闪点 ]:
292.7ºC

[ 精确质量 ]:
364.20100

[ PSA ]:
76.89000

[ LogP ]:
2.97350

[ 蒸汽压 ]:
1.37E-12mmHg at 25°C

GR 203040安全信息

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

GR 203040文献

Attenuation of the gerbil writhing response by mu-, kappa- and delta-opioids, and NK-1, -2 and -3 receptor antagonists.

Pharmacol. Biochem. Behav. 79(1) , 125-35, (2004)

Mu-, kappa- and delta-opioid receptor agonists are reported to attenuate the acetic-acid-induced abdominal constriction response in mice. NK-1, -2 and -3 receptor antagonists also display activity in ...

Brain uptake and receptor binding of two [11C]labelled selective high affinity NK1-antagonists, GR203040 and GR205171--PET studies in rhesus monkey.

Neuropharmacology 39(4) , 664-70, (2000)

Two high affinity and selective NK1-receptor antagonists, GR203040 and GR205171, were labelled with 11C and used in a series of experiments in rhesus monkeys. The purpose of these studies was to evalu...

The broad-spectrum anti-emetic activity of the novel non-peptide tachykinin NK1 receptor antagonist GR203040.

Br. J. Pharmacol. 116(8) , 3158-63, (1995)

1. Following our earlier observations that the tachykinin NK1 receptor antagonist CP-99,994 is an effective anti-emetic in ferrets, we have examined the anti-emetic effects of a more potent and novel ...

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