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Prucalopride succinate

Chemical Structure : Prucalopride succinate

CAS No.: 179474-85-2

Prucalopride succinate (R-108512;R108512)

Catalog No.: PC-43156Not For Human Use, Lab Use Only.

Prucalopride succinate (R-108512) is a potent, selective 5-HT4 receptor agonist with pKi of 8.6 and 8.1 for 5-HT4a and 5-HT4b, >290-fold higher affinity for 5-HT4 receptors than for other receptors.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

Prucalopride succinate (R-108512) is a potent, selective 5-HT4 receptor agonist with pKi of 8.6 and 8.1 for 5-HT4a and 5-HT4b, >290-fold higher affinity for 5-HT4 receptors than for other receptors; targets the impaired motility associated with chronic constipation, thus normalizing bowel movements; induces contractions (pEC50=7.48) in the guinea-pig colon, demonstrates anti-cholinergic, anticholinesterase or nonspecific inhibitory activity and does not antagonise 5-HT2A, 5-HT2B and 5-HT3 receptors or motilin, CCK1 receptors.

Physicochemical Properties

M.Wt 485.9584
Formula C22H32ClN3O7
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

DMSO: ≥ 36 mg/mL

Chemical Name/SMILES

Butanedioic acid, compd. with 4-amino-5-chloro-2,3-dihydro-N-[1-(3-methoxypropyl)-4-piperidinyl]-7-benzofurancarboxamide (1:1)

References

1. Prins NH, et al. Br J Pharmacol. 1999 Jul;127(6):1431-7.

2. Poen AC, et al. Aliment Pharmacol Ther. 1999 Nov;13(11):1493-7.

3. Bouras EP, et al. Gut. 1999 May;44(5):682-6.

4. Briejer MR, et al. Eur J Pharmacol. 2001 Jun 29;423(1):71-83.

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