Name | 4-amino-5-chloro-N-[1-(3-methoxypropyl)piperidin-4-yl]-2,3-dihydro-1-benzofuran-7-carboxamide,butanedioic acid |
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Synonyms |
Resolor
Prucalopride succinate BUTANEDIOIC ACID 4-AMINO-5-CHLORO-2,3-DIHYDRO-N-[1-(3-METHOXYPROPYL)-4-PIPERIDINYL]-7-BENZOFURANCARBOXAMIDE Prucalopride succinate (USAN) Resolor (TN) 7-Benzofurancarboxamide, 4-amino-5-chloro-2,3-dihydro-N-[1-(3-methoxypropyl)-4-piperidinyl]-, butanedioate (1:1) Prucalopride Succinat Succinic acid - 4-amino-5-chloro-N-[1-(3-methoxypropyl)-4-piperidinyl]-2,3-dihydro-1-benzofuran-7-carboxamide (1:1) Prucalopride (succinate) |
Description | Prucalopride succinate is a selective, high affinity 5-HT4 receptor agonist with pKi of 8.6/8.1 for 5-HT4a/4b.IC50 value:Target: 5-HT4 agonistin vitro: Prucalopride was a 5-HT(4) receptor agonist in the guinea-pig colon, as it induced contractions (pEC(50)=7.48+/-0.06; insensitive to a 5-HT(2A) or 5-HT(3) receptor antagonist, but inhibited by a 5-HT(4) receptor antagonist) as well as the facilitation of electrical stimulation-induced noncholinergic contractions (blocked by a 5-HT(4) receptor antagonist). Prucalopride did not cause relevant inhibition of 5-HT(2A), 5-HT(2B), or 5-HT(3), motilin or cholecystokinin (CCK(1)) receptor-mediated contractions, nor nicotinic or muscarinic acetylcholine receptor-mediated contractions, up to 10 microM [1].in vivo: Rat microdialysis studies revealed that prucalopride maximally increased ACh and histamine levels in the prefrontal cortex at 5 and 10 mg/kg, whereas PRX-03140 significantly increased cortical histamine levels at 50 mg/kg, failing to affect ACh release at doses lower than 150 mg/kg [2]. |
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References |
Molecular Formula | C22H32ClN3O7 |
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Molecular Weight | 485.958 |
Exact Mass | 485.192871 |
PSA | 154.91000 |
LogP | 3.11750 |
Storage condition | -20℃ |