Cinromide is an anticonvulsant agent. Cinromide inhibits epithelial neutral amino acid transporter BAT1 (SLC6A19) with an IC 50 of 0.5 μM.
性状
Solid
体外研究(In Vitro)
Cinromide (10-100 μM) inhibits 5-HT-induced contractions in rat fundus strips by 46%. Cinromide (100 μM) inhibits monoamine oxidase prepared from both liver and brain of rats. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
Cinromide shows electroshock convulsion and leptazol(pentetrazo1)-induced convulsion in mice, with ED 50 s of 60 ± 11 mg/kg, 90 ± 15 mg/kg and 80 ± 15 mg/kg, 300 ± 61 mg/kg for i.p. and oral administrion, respectively. Cinromide produces a dose-related antileptazol activity with an ED 50 value of 58 ± 11 mg/kg by i.p. administration in rats. Furthermore, Cinromide (75 mg/kg) significantly elevates the amount of leptazol needed to induce clonic seizures in the intravenously infused leptazol-threshold test in rats. Cinromide (300 mg/kg, i.p) shows no sifnificant effect on the anaesthetized open-chested dogs after 4 h treatment, neither in conscious dogs after 5-h oral treatment with 300 and 600 mg/kg of Cinromide. Cinromide (40 mg/kg, i.v.) depresses the response of the neuron to the unconditioned maxillary nerve stimulus, increasing the latency and decreasing
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
参考文献
[1]. Chiu P, et al. The effect of cinromide on "kindled" seizures in the rat. Neuropharmacology. 1982;21(3):273-276.[2]. Yadav A, et al. Novel Chemical Scaffolds to Inhibit the Neutral Amino Acid Transporter B0AT1 (SLC6A19), a Potential Target to Treat Metabolic Diseases. Front Pharmacol. 2020;11:140. Published 2020 Feb 28.
溶解度数据
In Vitro: DMSO : 250 mg/mL (983.79 mM; Need ultrasonic)配制储备液