SR57227盐酸盐 T23394

Product Introduction
Bioactivity


英文名: SR 57227A

描述: SR 57227A (SR 57227 hydrochloride) 是一种有效的、具有口服活性和选择性的 5-HT3 受体激动剂，具有穿越血脑屏障的能力和抗抑郁作用。它对大鼠皮质膜和整个 NG 108-15 细胞或其膜上的 5-HT3 受体结合位点的亲和力，IC50在 2.8 至 250 nM 之间。

体内活性: Seizure latency was significantly prolonged by a 5-HT3 receptor agonist SR 57227 in a dose-dependent manner.?Seizure score and mortality were also decreased by SR 57227 in PTZ-treated mice.?Furthermore, these anticonvulsant effects of SR 57227 were inhibited by a 5-HT3 receptor antagonist ondansetron.?However, ondansetron alone had no effect on seizure latency, seizure score or mortality at different doses.?Immunohistochemical studies have also shown that c-Fos expression was significantly increased in hippocampus (dentate gyrus, CA1, CA3 and CA4) of PTZ-treated mice.?Furthermore, c-Fos expression was significantly inhibited by ondansetron in mice treated with PTZ and SR 57227.?An ELISA study showed that SR 57227 attenuated the PTZ-induced inhibitory effects of GABA levels in hippocampus and cortex, and the attenuated effects of SR 57227 were antagonized by ondansetron in hippocampus but not cortex.?Activation of 5-HT3 receptor by SR 57227, which plays an important role on the control of seizure induced by PTZ, may be related to GABA activity in hippocampus.?Therefore, 5-HT3 receptor subtype is a potential target for the treatment of epilepsy[1].

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 8.33 mg/mL (33.57 mM)


关键字: SR 57227 Hydrochloride | immobility | barrier | Serotonin Receptor | cell | brain | 5-HT Receptor | SR 57227A | Inhibitor | 5-hydroxytryptamine Receptor | anti-depressant | inhibit | blood | SR57227 Hydrochloride | SR-57227 Hydrochloride | NG 108-15

相关产品: 5-HT1A modulator 2 hydrochloride | Risperidone | Nexopamil | Facinicline hydrochloride | Mirtazapine | Alniditan | Geissoschizine methyl ether | Hesperetin | Nuciferine | PZ-1922

相关库: Anti-Neurodegenerative Disease Compound Library | ReFRAME Related Library | Anti-Cancer Compound Library | Angiogenesis related Compound Library | Membrane Protein-targeted Compound Library | Bioactive Compounds Library Max | Neuronal Signaling Compound Library | GPCR Compound Library | Covalent Inhibitor Library | Bioactive Compound Library

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途