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SB-269970 HCl

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Chemical Structure| 261901-57-9 同义名 : SB-269970A;SB-269970 (hydrochloride);SB-269970 hydrochloride
CAS号 : 261901-57-9
货号 : A584325
分子式 : C18H29ClN2O3S
纯度 : 98+%
分子量 : 388.952
MDL号 : MFCD03788020
存储条件：

粉末 Inert atmosphere,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 30 mg/mL(77.13 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

H2O: 10 mg/mL(25.71 mM)，配合低频超声，并水浴加热至45℃助溶
动物实验配方：
生物活性
靶点

  • 5-HT7

    5-HT7, pKi:8.3
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].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.57mL

0.51mL

0.26mL

12.86mL

2.57mL

1.29mL

25.71mL

5.14mL

2.57mL
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