Formulation: A crystalline solid
Formal Name: 1-methyl-1H-indole-3-carboxylic acid, [1-[2-[(methylsulfonyl)amino]ethyl]-4-piperidinyl]methyl ester
Purity: ≥98%
Formula Markup: C19H27N3O4S
Formula Weight: 393,5
Shelf life (days): 1460
CAS Number: 144625-51-4
Notes: GR113808 is an antagonist of the serotonin (5-HT) receptor subtype 5-HT4.{42967} It binds to 5-HT4 receptors with an IC50 value of 0.4 nM in COS-7 cells expressing the human recombinant receptor and in guinea pig striatal membranes (IC50 = 0.5 nM).{42968} GR113808 is selective for 5-HT4 receptors over 5-HT1 receptors (Kis = >10 µM in dog saphenous vein and porcine vena cava), as well as 5-HT2 and 5-HT3 receptors (Kis = >10 and 1 μM in rabbit thoracic aorta and rat cerebral cortex, respectively).{42967} It is also selective for 5-HT4 over adenosine, adrenergic, dopamine, GABA, muscarinic, nicotinic, histamine, and NMDA receptors (Kis = >10 μM for all). GR113808 inhibits relaxation induced by 5-HT (Item No. 14332) in rat thoracic esophagus precontracted by carbachol (carbamoylcholine; Item No. 14486; pA2 = 9.3). In vivo, GR113808 inhibits 5-methoxytryptamine-induced tachycardia in anaesthetized piglets.
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