|(R)-3-((2-(2-(4-甲基哌嗪-1-基)乙基)吡咯烷-1-基)磺酰基)苯酚盐酸盐|CsnPharm

CAS No.: 261901-57-9

SB-269970 HCl/SB269970 盐酸盐 Catalog No. CSN13121

Synonyms: SB-269970A;SB-269970 (hydrochloride);SB-269970

SB-269970 HCl is a HCl salt form of SB-269970, which is a 5-HT7 receptor antagonist with pKi of 8.3 and exhibits > 50-fold selectivity against other receptors.

规格	价格	促销价格	库存	数量

400-920-2911

sales@csnpharm.cn

tech@csnpharm.cn

加入购物车大规格询价

加入收藏

产品咨询

400-920-2911

sales@csnpharm.cn

tech@csnpharm.cn

纯度 & 质量文件批次:

靶点选择性

生物活性

实验方案

技术信息

生物活性

描述SB269970 hydrochloride (SB-269970A) is a hydrochloride salt form of SB-269970, which is a 5-HT7 receptor antagonist with the pKi of 8.3, exhibits >50-fold selectivity against other receptors. The pA2 (8.5 ± 0.2) for SB-269970-A agreed well with the pKi determined from [(3)H]-5-CT binding studies. 5-CT-stimulated adenylyl cyclase activity in guinea-pig hippocampal membranes (pEC50 of 8.4 ± 0.2) was inhibited by SB-269970-A (0.3 μM) with a pKB (8.3 ± 0.1) in good agreement with its antagonist potency at the human cloned 5-HT7a receptor and its binding affinity at guinea-pig cortical membranes. 5-CT (0.3 mg/kg, i.p.) induced hypothermia in guinea-pigs was blocked by SB-269970-A (ED50 = 2.96 mg/kg, i.p.) and the non-selective 5-HT7 receptor antagonist metergoline (0.3 - 3 mg/kg, s.c.). SB-269970-A (30 mg/kg) administered at the start of the sleep period, significantly reduced time spent in Paradoxical Sleep (PS) during the first 3 h of EEG recording in conscious rats^[2]. Elevated corticosterone level reduces DRN (dorsal raphe nucleus) 5HT7 receptor reactivity and decreases GABAergic transmission within the DRN (dorsal raphe nucleus), which can be reversed by SB 269970^[3]. In the fibrogenic phase, both SB-269970 and terguride reduced the serotonin concentrations in lung homogenates and significantly protected against IPF fibrogenic phase by attenuating collagen deposition and mRNA expression of both transforming growth factor-β1 (TGF-β1), and procollagen type Ӏ (PINP)^[4].
参考文献

[1] Roberts C, Allen L, 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.
[2] Hagan JJ, Price GW, Jeffrey P, et al. Characterization of SB-269970-A, a selective 5-HT(7) receptor antagonist. Br J Pharmacol. 2000;130(3):539-548
[3] Sowa J, Kusek M, Siwiec M, et al. The 5-HT7 receptor antagonist SB 269970 ameliorates corticosterone-induced alterations in 5-HT7 receptor-mediated modulation of GABAergic transmission in the rat dorsal raphe nucleus. Psychopharmacology (Berl). 2018;235(12):3381-3390
[4] Tawfik MK, Makary S. 5-HT7 receptor antagonism (SB-269970) attenuates bleomycin-induced pulmonary fibrosis in rats via downregulating oxidative burden and inflammatory cascades and ameliorating collagen deposition: Comparison to terguride. Eur J Pharmacol. 2017;814:114-123

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.5710 mL
- 12.8550 mL
- 25.7101 mL
- 5 mM
- 0.5142 mL
- 2.5710 mL
- 5.1420 mL
- 10 mM
- 0.2571 mL
- 1.2855 mL
- 2.5710 mL

技术信息

CAS号

261901-57-9

储存条件

粉末: Inert atmosphere,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C18H29ClN2O3S

运输

蓝冰

分子量

388.95

别名

SB-269970A;SB-269970 (hydrochloride);SB-269970;GR-125743;SB269970 HCl

溶解度

DMSO	11.0 mg/mL (28.3 mM)
Water	Insoluble
Ethanol	Insoluble

动物实验配方

大规格询价

号为必填项

姓名: 邮箱: 手机号:

留言:

提交

SB-269970 HCl/SB269970 盐酸盐 Catalog No. CSN13121

靶点选择性

请登录您的专属账户

确认信息