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Prucalopride

  Cat. No.:  DC4147   Featured
Chemical Structure
179474-81-8
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Field of application
Prucalopride is a selective, high affinity 5-HT receptor agonistfor 5-HT4a and 5-HT4b with Ki of 2.5 nM and 8 nM, respectively.
Chemicals PropertiesBiological activity COA & MSDSRelated productsDatasheet
Cas No.: 179474-81-8
Chemical Name: 4-amino-5-chloro-N-(1-(3-methoxypropyl)piperidin-4-yl)-2,3-dihydrobenzofuran-7-carboxamide
Synonyms: R-108512; R 108512; R108512; R 093877; R-093877; R093877; R 93877; R-93877; R93877； Prucalopride; Prucalopride free base; Motegrity; Resolor; Resotran;
SMILES: O=C(NC1CCN(CCCOC)CC1)C2=CC(Cl)=C(N)C3=C2OCC3
Formula: C18H26ClN3O3
M.Wt: 367.87
Purity: 99%
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Description: Prucalopride (R093877) is a drug acting as a selective, high affinity 5-HT4 receptor agonist(pKi=8.6/8.1 for 5-HT4a/4b); >150-fold higher affinity for 5-HT4 receptors than for other receptors.Prucalopride is a novel enterokinetic compound and is the first representative of the benzofuran class. Receptor binding data have demonstrated prucalopride's high affinity to both investigated 5-HT(4) receptor isoforms, with mean pK(i) estimates of 8.60 and 8.10 for the human 5-HT(4a) and 5-HT(4b) receptor, respectively. From the 50 other binding assays investigated in this study only the human D(4) receptor (pK(i) 5.63), the mouse 5-HT(3) receptor (pK(i) 5.41) and the human sigma(1) (pK(i) 5.43) have shown measurable affinity, resulting in at least 290-fold selectivity for the 5-HT(4) receptor [1].
Target: IC50 value: 8.6/8.1 for 5-HT4a/4b(pKi) Target: 5-HT4 receptor
References: [1]. Briejer MR, et al. The in vitro pharmacological profile of prucalopride, a novel enterokinetic compound. Eur J Pharmacol. 2001 Jun 29;423(1):71-83. [2]. Emmanuel AV, et al. Randomised clinical trial: the efficacy of prucalopride in patients with chronic intestinal pseudo-obstruction--a double-blind, placebo-controlled, cross-over, multiple n = 1 study. Aliment Pharmacol Ther. 2012 Jan;35(1):48-55. [3]. Bouras EP, et al. Selective stimulation of colonic transit by the benzofuran 5HT4 agonist, prucalopride, in healthy humans. Gut. 1999 May;44(5):682-6.
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
2018-0101
2018-0101
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