Prucalopride

製品コードS2875 バッチS287501

印刷

化学情報

Chemical Structure Synonyms R-93877 Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C18H26ClN3O3
分子量 367.87 CAS No. 179474-81-8
Solubility (25°C)* 体外 DMSO 60 mg/mL (163.1 mM)
Ethanol 38 mg/mL (103.29 mM)
Water Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 Prucalopride (R-93877) is a selective, high affinity 5-HT receptor agonist for 5-HT4A and 5-HT4B receptor with Ki of 2.5 nM and 8 nM, respectively, exhibits >290-fold selectivity against other 5-HT receptor subtypes.
in vitro 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]
in vivo Complete bowel movements per week is 30.9% of those receiving 2 mg of Prucalopride and 28.4% of those receiving 4 mg of Prucalopride, as compared with 12.0% in the placebo group. 47.3% of patients receiving 2 mg of Prucalopride and 46.6% of those receiving 4 mg of Prucalopride has an increase in the number of spontaneous, complete bowel movements of one or more per week, on average, as compared with 25.8% in the placebo group. Prucalopride (2 mg or 4 mg) significantly improves all other secondary efficacy end points, including patients' satisfaction with their bowel function and treatment and their perception of the severity of their constipation symptoms. [2] Prucalopride (4 mg daily) accelerates overall gastric emptying and small bowel transit in patients with constipation without a rectal evacuation disorder. Prucalopride (4 mg daily) tends to accelerate overall colonic transit with significantly faster overall colonic transit and ascending colon emptying. [3] Higher proportions of patients on prucalopride 2 mg (19.5%), 4 mg (23.6%) has three or more spontaneous complete bowel movements(SCBM)/week compared with placebo (9.6%). Prucalopride also significantly improves secondary efficacy and quality of life endpoints, including the proportion of patients with an increase of one or more SCBM/week, evacuation completeness, perceived disease severity and treatment effectiveness and quality of life. [4] 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. [5]

プロトコル(参考用のみ)

キナーゼアッセイ Binding assay
Membrane fractions from cells or from tissue homogenates are incubated with a radioactively labelled ligand with high affinity for a particular receptor. Specific receptor binding of the radioligand is distinguished from the nonspecific labelling by addition of an excess of an unlabelled compound, known to compete with the radioligand for binding to the receptor sites. The remaining nonspecific labelling is subtracted from total binding values obtained without the competitor. To determine the receptor binding affinity of unlabelled prucalopride, the ligand is added at various concentrations to the incubation mixture. Following an incubation period necessary to reach equilibrium at a given temperature, the membranes are harvested by rapid filtration and filters are placed in counting vials, 2 mL of Ultima Gold MV are added and filter-bound radioactivity is counted after shaking and resting in a Packard liquid scintillation counter.

カスタマーフィードバック

, , Neurogastroenterol Motil, 2017, doi: 10.1111/nmo.13064

Data from [Data independently produced by , , Neurogastroenterol Motil, 2016, 28(8):1241-51.]

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Preoperative administration of the 5-HT4 receptor agonist prucalopride reduces intestinal inflammation and shortens postoperative ileus via cholinergic enteric neurons. [ Gut, 2019, 68(8):1406-1416] PubMed: 30472681
Modulation of Cytokine-Induced Astrocytic Endothelin-1 Production as a Possible New Approach to the Treatment of Multiple Sclerosis [ Front Pharmacol, 2019, 10:1491] PubMed: 31969819
Gastric Emptying and Gastrointestinal Transit Compared among Native and Hydrolyzed Whey and Casein Milk Proteins in an Aged Rat Model. [ Nutrients, 2017, 9(12)] PubMed: 29236034
5-HT4 receptors facilitate cholinergic neurotransmission throughout the murine gastrointestinal tract. [Pauwelyn V, et al. Neurogastroenterol Motil, 2017, 10.1111/nmo.13064] PubMed: 28332745
Tracking gastrointestinal transit of solids in aged rats as pharmacological models of chronic dysmotility. [Dalziel JE, et al. Neurogastroenterol Motil, 2016, 28(8):1241-51] PubMed: 27028044

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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