Description: |
Prucalopride succinate is a selective, high affinity 5-HT4 receptor agonist with pKi of 8.6/8.1 for 5-HT4a/4b.in 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.
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. For the detailed information of Prucalopride succinate, the solubility of Prucalopride succinate in water, the solubility of Prucalopride succinate in DMSO, the solubility of Prucalopride succinate in PBS buffer, the animal experiment (test) of Prucalopride succinate, the cell expriment (test) of Prucalopride succinate, the in vivo, in vitro and clinical trial test of Prucalopride succinate, the EC50, IC50,and affinity,of Prucalopride succinate, For the detailed information of Prucalopride succinate, the solubility of Prucalopride succinate in water, the solubility of Prucalopride succinate in DMSO, the solubility of Prucalopride succinate in PBS buffer, the animal experiment (test) of Prucalopride succinate, the cell expriment (test) of Prucalopride succinate, the in vivo, in vitro and clinical trial test of Prucalopride succinate, the EC50, IC50,and affinity,of Prucalopride succinate, Please contact DC Chemicals. |