琥珀酸普芦卡必利 T6958

Product Introduction
Bioactivity


英文名: Prucalopride Succinate

描述: Prucalopride Succinate (Resolor Succinate) 是5-HT4受体选择高亲和性激动剂，对5-HT4a 和5-HT4b 的 Ki 值分别为 2.5 和 8 nM。

体外活性: Prucalopride induces contractions in a concentration-dependent manner with pEC50 of 7.5. Prucalopride (1 mM) significantly amplifies the rebound contraction of the guinea-pig proximal colon after electrical field stimulation. Prucalopride induces relaxation of the rat oesophagus preparation of rat oesophagus tunica muscularis mucosae with pEC50 of 7.8, yielding a monophasic concentration–response curve. [1] Prucalopride (0.1 μM) concentration-dependently increases the amplitude of submaximal cholinergic contractions and of acetylcholine release induced by electrical field stimulation in pig gastric circular muscle, and the effect is induced and enhanced IBMX (10 μM). [2] Prucalopride (1 μM) significantly enhances the electrically induced cholinergic contractions in pig descending colon, and the facilitating effect is significantly enhanced by Rolipram. [3]

体内活性: Prucalopride alters colonic contractile motility patterns in a dose-dependent fashion by stimulating high-amplitude clustered contractions in the proximal colon and by inhibiting contractile activity in the distal colon of fasted dogs. Prucalopride also causes a dose-dependent decrease in the time to the first giant migrating contraction (GMC); at higher doses of prucalopride, the first GMC generally occurres within the first half-hour after treatment. [4]

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

溶解度: Ethanol : < 1 mg/mL (insoluble or slightly soluble)
H2O : 89 mg/mL (183.1 mM)
DMSO : 90 mg/mL (185.2 mM)


关键字: inhibit | 5-HT Receptor | Inhibitor | Serotonin Receptor | Prucalopride Succinate | 5-hydroxytryptamine Receptor | R108512 | Prucalopride | R 108512

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相关库: Anti-Neurodegenerative Disease Compound Library | Drug Repurposing Compound Library | Anti-Cancer Drug Library | Membrane Protein-targeted Compound Library | Anti-Cancer Clinical Compound Library | GPCR Compound Library | Anti-Cancer Approved Drug Library | EMA Approved Drug Library | NO PAINS Compound Library | Bioactive Compound Library

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