A potent and selective 5-HT4 agonist (Ki = 2.5 and 8 nM for 5-HT4A and 5-HT4B

Prucalopride – 50 mg

Brand:
Cayman
CAS:
179474-81-8
Storage:
-20
UN-No:
De Minimis - 3077 / 9

Prucalopride is a potent and selective agonist of the serotonin (5-HT) receptor subtype 5-HT4 (Kis = 2.5 and 8 nM for human 5-HT4A and 5-HT4B, respectively).{38962} Prucalopride is greater than 250-fold selective for 5-HT4 over a panel of 53 overexpressed receptors, including 5-HT subtypes, but does bind to human dopamine D4 and sigma-1 (σ1) receptors and mouse 5-HT3 receptors (Kis = 2.3, 3.7, and 3.8 μM, respectively). It induces contractions in guinea pig colon with an EC50 value of 33 nM, an effect that is blocked by the 5-HT4 antagonist GR113808 but not the 5-HT2A and 5-HT3 antagonists ketanserin (Item No. 22058) and granisetron (Item No. 21239), respectively.{38963} It also facilitates non-cholinergic contractions induced by electrical stimulation. In fasted dogs, oral administration of prucalopride increases colonic motility by inhibiting distal colon contractions (ED50 = 0.04 mg/kg), an effect that is blocked by pretreatment with the 5-HT4 antagonist GR125487. Prucalopride (5-10 mg/kg, s.c.) increases acetylcholine and histamine levels in the rat prefrontal cortex by 2.4-fold and 3-fold, respectively, and increases the power of hippocampal theta oscillations.{38964} Formulations containing prucalopride have been used in the treatment of chronic idiopathic constipation.  

 

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Description

A potent and selective 5-HT4 agonist (Ki = 2.5 and 8 nM for 5-HT4A and 5-HT4B, respectively); greater than 250-fold selective for 5-HT4 over a panel of 53 overexpressed receptors, including 5-HT subtypes, but does bind to human D4 and σ1 receptors and mouse 5-HT3 receptors (Kis = 2.3, 3.7, and 3.8 μM respectively); induces 5-HT4-dependent contractions in guinea pig colon (EC50 = 33 nM) and facilitates non-cholinergic contractions induced by electrical stimulation; increases colonic motility by inhibiting distal colon contractions in dogs (ED50 = 0.04 mg/kg, p.o.); increases acetylcholine and histamine levels in the rat prefrontal cortex and the power of hippocampal theta oscillations (5-10 mg/kg, s.c.)

Formal name: 4-amino-5-chloro-2,3-dihydro-N-[1-(3-methoxypropyl)-4-piperidinyl]-7-benzofurancarboxamide

Synonyms: 

Molecular weight: 367.9

CAS: 179474-81-8

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Receptor Pharmacology|Agonists||Research Area|Neuroscience

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