prucalopride

Modify Date: 2024-01-02 14:51:00

prucalopride Structure
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
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].

 Names

Name Prucalopride
Synonym More Synonyms

 prucalopride Biological Activity

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
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.

 Chemical & Physical Properties

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

 Safety Information

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

 Synonyms

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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