GR 203040

更新时间：2024-02-05 19:27:28

GR 203040结构式	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

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。

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

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.

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

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

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 ...

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)