GR 203040

更新时间:2024-02-05 19:27:28

GR 203040结构式
GR 203040结构式
品牌特惠专场
常用名 GR 203040 英文名 GR 203040
CAS号 168398-02-5 分子量 437.37
密度 N/A 沸点 560.4ºC at 760mmHg
分子式 C20H26Cl2N6O 熔点 N/A
MSDS 美版 闪点 292.7ºC

 GR 203040用途

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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。

 GR 203040名称

英文名 N-[[2-methoxy-5-(tetrazol-1-yl)phenyl]methyl]-2-phenylpiperidin-3-amine
英文别名 更多

 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
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6

更多文献
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 ...

 GR 203040英文别名

3-Piperidinamine,N-[[2-methoxy-5-(1H-tetrazol-1-yl)phenyl]methyl]-2-phenyl-,hydrochloride(1:2),(2S,3S)
3-Piperidinamine,N-[[2-methoxy-5-(1H-tetrazol-1-yl)phenyl]methyl]-2-phenyl-,dihydrochloride,(2S-cis)
3-Piperidinamine,N-[[2-methoxy-5-(1H-tetrazol-1-yl)phenyl]methyl]-2-phenyl-,dihydrochloride,(2S,3S)-(9CI)
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