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SB-222200

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Chemical Structure| 174635-69-9 同义名 : -
CAS号 : 174635-69-9
货号 : A875802
分子式 : C26H24N2O
纯度 : 99%+
分子量 : 380.482
MDL号 : MFCD00944072
存储条件：

粉末 Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(275.97 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
动物实验配方：
生物活性
描述 NK-3 receptors are G-protein coupled receptors activated by mammalian tachykinins, which can modulate dopaminergic neurotransmission, and thus may play a role in development and expression of behavioral sensitization[3]. SB-222200 is a human NK-3 receptor (hNK-3R) antagonist. SB-222200 inhibited 125I-[MePhe7] neurokinin B (NKB) binding to Chinese hamster ovary (CHO) cell membranes stably expressing the hNK-3 receptor with a Ki of 4.4 nM and antagonized NKB-induced Ca2+ mobilization in HEK 293 cells stably expressing the hNK-3 receptor with an IC50 of 18.4 nM. SB-222200 was selective for hNK-3 receptors compared with hNK-1 (Ki > 100,000 nM) and hNK-2 receptors (Ki = 250 nM). In HEK 293 cells transiently expressing murine NK-3 receptors, SB-222200 inhibited binding of 125I-[MePhe7]NKB (Ki = 174 nM) and antagonized NKB (1 nM)-induced calcium mobilization (IC50 = 265 nM). In mice oral administration of SB-222200 produced dose-dependent inhibition of behavioral responses induced by i.p. or intracerebral ventricular administration of the NK-3 receptor-selective agonist, senktide, with ED50 value of approximately 5 mg/kg. Pharmacokinetic evaluation of SB-222200 in rat after oral administration (8 mg/kg) indicated sustained plasma concentrations (Cmax) = 400 ng/mL) and bioavailability of 46% [2]. Administration of SB-222200 (5 mg/kg, s.c.) prior to repeated cocaine (20 mg/kg, i.p.) prevented the development of sensitized responses after a cocaine challenge.
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.63mL

0.53mL

0.26mL

13.14mL

2.63mL

1.31mL

26.28mL

5.26mL

2.63mL
参考文献

[1]King AG, Sanger GJ. Effect of a selective and potent central nervous system penetrant, neurokinin-3 receptor antagonist (SB-222200), on cisplatin-induced emesis in the ferret. Neurosci Lett. 2005 Mar 7;376(1):5-8.

[2]Sarau HM, Griswold DE, Bush B, et al. Nonpeptide tachykinin receptor antagonists. II. Pharmacological and pharmacokinetic profile of SB-222200, a central nervous system penetrant, potent and selective NK-3 receptor antagonist. J Pharmacol Exp Ther. 2000;295(1):373-381.

[3]Nwaneshiudu CA, Unterwald EM. NK-3 receptor antagonism prevents behavioral sensitization to cocaine: a role of glycogen synthase kinase-3 in the nucleus accumbens. J Neurochem. 2010;115(3):635-642.