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SHA 68 是一种有效的选择性非肽神经肽 S 受体 (NPSR) 拮抗剂,对 NPSR Asn107 和 NPSR Ile107 的 IC50 分别为 22.0 和 23.8 nM。SHA 68 具有有限的血脑屏障 (BBB) 渗透能力和用于神经痛的活性。
[1]. Okamura N, et al. Synthesis and pharmacological in vitro and in vivo profile of 3-oxo-1,1-diphenyl-tetrahydro-oxazolo[3,4-a]pyrazine-7-carboxylic acid 4-fluoro-benzylamide (SHA 68), a selective antagonist of the neuropeptide S receptor.J Pharmacol Exp Ther. 2008 Jun;325(3):893-901.
[2]. Ensho T, et al. Neuropeptide S increases motor activity and thermogenesis in the rat through sympathetic activation.Neuropeptides. 2017 Oct;65:21-27.
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