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首页-小分子抑制剂&激动剂-GPCR-5-HT Receptor-SB-656104A
SB-656104A

Chemical Structure : SB-656104A

CAS No.: 527750-76-1

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SB-656104A (SB-656104-A, SB-656104, SB656104)

货号: PC-26609Not For Human Use, Lab Use Only.

SB-656104A (SB-656104-A) is a potent, selective 5-HT7 receptor antagonist, potently inhibits [3H]-SB-269970 binding to the human cloned 5-HT7(a) (pKi=8.7) and 5-HT7(b) (pKi=8.5) receptor variants and the rat native receptor (pKi=8.8).

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

SB-656104A (SB-656104-A) is a potent, selective 5-HT7 receptor antagonist, potently inhibits [3H]-SB-269970 binding to the human cloned 5-HT7(a) (pKi=8.7) and 5-HT7(b) (pKi=8.5) receptor variants and the rat native receptor (pKi=8.8).
SB-656104A (SB-656104-A) displays at least 30-fold selectivity for the human 5-HT7(a) receptor versus other human cloned 5-HT receptors apart from the 5-HT1D receptor (∼10-fold selective).
SB-656104-A antagonised competitively the 5-carboxamidotryptamine (5-CT)-induced accumulation of cyclic AMP in h5-HT7(a)/HEK293 cells with a pA2 of 8.5.
SB-656104-A produced a significant reversal of the 5-CT-induced hypothermic effect in guinea pigs, a pharmacodynamic model of 5-HT7 receptor interaction in vivo (ED50 2 mg kg−1).
SB-656104A (SB-656104-A) significantly increased the latency to onset of rapid eye movement (REM) sleep at 30 mg kg−1 i.p. (+93%) and reduced the total amount of REM sleep at 10 and 30 mg kg−1 i.p.

物理化学性质&存储条件

分子量 524.50
分子式 C25H31Cl2N3O3S
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

(6-((R)-2-{2-[4-(4-Chloro-phenoxy)-piperidin-1-yl]-ethyl}-pyrrolidine-1-sulphonyl)-1H-indole hydrochloride)

参考文献

1. Thomas DR, et al. Br J Pharmacol. 2003 Jun;139(4):705-14.

2. Forbes IT, et al. Bioorg Med Chem Lett. 2002 Nov 18;12(22):3341-4.

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