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SB271046
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
SB271046图片
CAS NO:209481-20-9
规格:98%
分子量:451.99
包装与价格:
包装价格(元)
10mg电议
50mg电议

产品介绍
5-HT6 receptor antagonist, orally active
CAS:209481-20-9
分子式:C20H22ClN3O3S2
分子量:451.99
纯度:98%
存储:Store at -20°C

Background:

SB-271046 is a selective and orally active 5-HT6 receptor antagonist.


5-HT6 belongs to GPCR which stimulates adenylate cyclase via Gs, which cloned from rat striatum.


SB-271046 substituted [125I]-SB-258585 and [3H]-LSD from human 5-HT6 receptors which recombinantly expressed in HeLa cells in vitro (pKi 8.92 and 9.09 respectively). SB-271046 also transfered [125I]-SB-258585 from human caudate putamen and rat and pig striatum membranes (pKi 8.81, 9.02 and 8.55 respectively). By 5-HT alone or after increasing concentrations of SB-271046 (10, 30, 100 and 300 nM) stimulates adenylyl cyclase activity in HeLa cells stably expressing human 5-HT6 receptors. [1]


The affinities of SB-271046 in human (pKi 8.81), pig (pKi 8.55) and rat (pKi 9.02) were similar suggesting a lack of species differences in 5-HT6 receptor for this given ligand. SB-271046 has greater than 200 fold selectivity over 69 other receptor, enzyme and binding sites, containing all other 5-HT receptor subtypes tested. SB-271046 did not alter basal levels of 5-HT, DA and NA in either brain region. In contrast, administration of SB-271046 (10mg.kg-1s.c.) produced an important and tetrodotoxin-dependent acceleration in extracellular levels of both glutamate and aspartate within the frontal cortex, reaching maximum values of 375.482.3 and 215.362.1% of preinjection values, respectively. [2]


参考文献:
1.  Characterization of SB-271046: a potent, selective and orally active 5-HT(6) receptor antagonist. Br J Pharmacol. 2000 Aug;130(7):1606-12.
2.  In vivo effects of the 5-HT(6) antagonist SB-271046 on striatal and frontal cortex extracellular concentrations of noradrenaline, dopamine, 5-HT, glutamate and aspartate. Br J Pharmacol. 2000 May;130(1):23-6.