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3-甲基-2-苯基-N-((1S)-1-苯基丙基)喹啉-4-甲酰胺

用途

SB 222200是可逆的竞争性人NK受体抑制剂,对hNK-3受体的Ki为4.4 nM,能透过血脑屏障。

名称

[ CAS 号 ]:
174635-69-9

[ 中文名 ]:
3-甲基-2-苯基-N-((1S)-1-苯基丙基)喹啉-4-甲酰胺

[ 英文名 ]:
SB-222200

[英文别名 ]:

Lopac-S-5192
Tocris-1393
SB-222200

生物活性

[ 描述 ]:

SB 222200是可逆的竞争性人NK受体抑制剂,对hNK-3受体的Ki为4.4 nM,能透过血脑屏障。

[ 相关类别 ]:

信号通路 >> G 蛋白偶联受体/G 蛋白 >> 神经激肽受体

信号通路 >> 神经信号通路 >> 神经激肽受体

研究领域 >> 神经疾病

[参考文献]

[1]. Sarau HM, et al. Nonpeptide tachykinin receptor antagonists. II. Pharmacological and pharmacokinetic profile of SB-222200, a central nervous system penetrant, potent and selective NK-3 receptor antagonist. J Pharmacol Exp Ther. 2000 Oct;295(1):373-81.

[相关活性小分子]

物理化学性质

[ 密度 ]:
1.142g/cm3

[ 沸点 ]:
553.5ºC at 760 mmHg

[ 分子式 ]:
C₂₆H₂₄N₂O

[ 分子量 ]:
380.48200

[ 闪点 ]:
288.6ºC

[ 精确质量 ]:
380.18900

[ PSA ]:
41.99000

[ LogP ]:
6.48220

[ 蒸汽压 ]:
2.7E-12mmHg at 25°C

[ 折射率 ]:
1.633

[ 储存条件 ]:
2-8℃

MSDS

详细MSDS(安全技术说明书)

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

Nonpeptide tachykinin receptor antagonists. II. Pharmacological and pharmacokinetic profile of SB-222200, a central nervous system penetrant, potent and selective NK-3 receptor antagonist.

J. Pharmacol. Exp. Ther. 295(1) , 373-81, (2000)

The pharmacological and pharmacokinetic profile of SB-222200 [(S)-(-)-N-(alpha-ethylbenzyl)-3-methyl-2-phenylquinoline-4-car boxami de], a human NK-3 receptor (hNK-3R) antagonist, was determined. SB-2...

In vitro and in vivo characterization of NK3 receptors in the rabbit eye by use of selective non-peptide NK3 receptor antagonists.

Br. J. Pharmacol. 122 , 469-476, (1997)

1. Inhibition of NK3 receptor agonist-induced contraction in the rabbit isolated iris sphincter muscle was used to assess the in vitro functional activity of three 2-phenyl-4-quinolinecarboxamides, me...

Expression of neurokinin B/NK3 receptor and kisspeptin/KISS1 receptor in human granulosa cells.

Hum. Reprod. 29(12) , 2736-46, (2014)

Are neurokinin B (NKB), NK3 receptor (NK3R), kisspeptin (KISS1) and kisspeptin receptor (KISS1R) expressed in human ovarian granulosa cells?The NKB/NK3R and kisspeptin/KISS1R systems are co-expressed ...

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