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SB-269970盐酸盐

SB-269970盐酸盐用途

SB269970盐酸盐是5-HT7受体拮抗剂,pKi为8.3,比对其它受体的抑制性高50倍以上。

SB-269970盐酸盐名称

[ CAS 号 ]:
261901-57-9

[ 中文名 ]:
(R)-3-((2-(2-(4-甲基哌啶-1-基)乙基)吡咯烷-1-基)磺酰基)苯酚盐酸盐

[ 英文名 ]:
SB269970 HCl

[英文别名 ]:

SB-269970 (hydrochloride)

SB-269970盐酸盐生物活性

[ 描述 ]:

SB269970盐酸盐是5-HT7受体拮抗剂,pKi为8.3,比对其它受体的抑制性高50倍以上。

[ 相关类别 ]:

信号通路 >> G 蛋白偶联受体/G 蛋白 >> 5-HT受体

信号通路 >> 神经信号通路 >> 5-HT受体

研究领域 >> 神经疾病

[参考文献]

[1]. http://www.ncbi.nlm.nih.gov/pubmed/10821781

[2]. Roberts C, et al. The effect of SB-269970, a 5-HT(7) receptor antagonist, on 5-HT release from serotonergic terminals and cell bodies. Br J Pharmacol. 2001 Apr;132(7):1574-80.

[3]. Monti JM, et al. The serotonin 5-HT7 receptor agonist LP-44 microinjected into the dorsal raphe nucleus suppresses REM sleep in the rat. Behav Brain Res. 2008 Aug 22;191(2):184-9.

[相关活性小分子]

SB-269970盐酸盐物理化学性质

[ 分子式 ]:
C₁₈H₂₉ClN₂O₃S

[ 分子量 ]:
388.95200

[ 精确质量 ]:
388.15900

[ PSA ]:
69.23000

[ LogP ]:
4.42590

[ 储存条件 ]:
2-8°C

[ 水溶解性 ]:
H2O: soluble10mg/mL, clear (warmed to 60 °C)

SB-269970盐酸盐MSDS

详细MSDS(安全技术说明书)

SB-269970盐酸盐安全信息

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

[ 危害码 (欧洲) ]:
Xi

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

[ 海关编码 ]:
2935009090

SB-269970盐酸盐海关

[ 海关编码 ]: 2935009090

[ 中文概述 ]:
2935009090 其他磺（酰）胺. 增值税率:17.0% 退税率:9.0% 监管条件:无最惠国关税:6.5% 普通关税:35.0%

[ 申报要素 ]: 品名, 成分含量, 用途

[ Summary ]:
2935009090 other sulphonamides VAT:17.0% Tax rebate rate:9.0% Supervision conditions:none MFN tariff:6.5% General tariff:35.0%

SB-269970盐酸盐文献

A novel, potent, and selective 5-HT(7) antagonist: (R)-3-(2-(2-(4-methylpiperidin-1-yl)ethyl)pyrrolidine-1-sulfonyl) phen ol (SB-269970).

J. Med. Chem. 43(3) , 342-345, (2000)

Characterization of SB-269970-A, a selective 5-HT(7) receptor antagonist.

Br. J. Pharmacol. 130(3) , 539-48, (2000)

The novel 5-HT(7) receptor antagonist, SB-269970-A, potently displaced [(3)H]-5-CT from human 5-HT(7(a)) (pK(i) 8.9+/-0.1) and 5-HT(7) receptors in guinea-pig cortex (pK(i) 8.3+/-0.2). 5-CT stimulated...

[(3)H]-SB-269970--A selective antagonist radioligand for 5-HT(7) receptors.

Br. J. Pharmacol. 130(2) , 409-17, (2000)

Binding of the 5-HT(7) receptor antagonist radioligand [(3)H]-SB-269970 to human 5-HT(7(a)) receptors expressed in HEK293 cell membranes (h5-HT(7(a))/293) and to guinea-pig cerebral cortex membranes, ...

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