prucalopride

Modify Date: 2025-08-23 17:59:02

prucalopride structure	Common Name	prucalopride
	CAS Number	179474-81-8	Molecular Weight	367.870
	Density	1.3±0.1 g/cm3	Boiling Point	481.4±45.0 °C at 760 mmHg
	Molecular Formula	C₁₈H₂₆ClN₃O₃	Melting Point	90.7°
	MSDS	Chinese USA	Flash Point	244.9±28.7 °C
	Symbol	GHS07, GHS09	Signal Word	Warning

Use of prucalopride

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.IC50 value: 8.6/8.1 for 5-HT4a/4b(pKi)Target: 5-HT4 receptorPrucalopride 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].

Name	Prucalopride
Synonym	More Synonyms

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.IC50 value: 8.6/8.1 for 5-HT4a/4b(pKi)Target: 5-HT4 receptorPrucalopride 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].
Related Catalog	Signaling Pathways >> GPCR/G Protein >> 5-HT Receptor Signaling Pathways >> Neuronal Signaling >> 5-HT Receptor Research Areas >> Neurological Disease
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.

Description

Related Catalog

Signaling Pathways >> GPCR/G Protein >> 5-HT Receptor

Signaling Pathways >> Neuronal Signaling >> 5-HT Receptor

Research Areas >> Neurological Disease

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.

Density	1.3±0.1 g/cm3
Boiling Point	481.4±45.0 °C at 760 mmHg
Melting Point	90.7°
Molecular Formula	C₁₈H₂₆ClN₃O₃
Molecular Weight	367.870
Flash Point	244.9±28.7 °C
Exact Mass	367.166260
PSA	76.82000
LogP	1.44
Vapour Pressure	0.0±1.2 mmHg at 25°C
Index of Refraction	1.599

Symbol	GHS07, GHS09
Signal Word	Warning
Hazard Statements	H315-H319-H335-H400
Precautionary Statements	P305 + P351 + P338
Hazard Codes	Xi
RIDADR	UN 3077 9 / PGIII

4-Amino-5-chloro-N-[1-(3-methoxypropyl)-4-piperidinyl]-2,3-dihydro-1-benzofuran-7-carboxamide

prucalopride

4-Amino-5-chloro-2,3-dihydro-N-[1-(3-methoxypropyl)-4-piperidinyl]-7-benzofurancarboxamide

Resolor

7-Benzofurancarboxamide, 4-amino-5-chloro-2,3-dihydro-N-[1-(3-methoxypropyl)-4-piperidinyl]-

4-Amino-5-chloro-N-[1-(3-methoxypropyl)piperidin-4-yl]-2,3-dihydro-1-benzofuran-7-carboxamide

Unii-0A09iuw5tp

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prucalopride

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