A selective

SB-207266 – 1 mg

Brand:
Cayman
CAS:
152811-62-6
Storage:
-20
UN-No:
De Minimis - 2811 / 6.1

The indole derivative SB-207266 is a selective and potent antagonist of the serotonin (5-HT) receptor 5-HT4 with a pA2 value of 10.6 ± 0.1.{34073, 34070} In COS7 cells, 100 nM SB-207266 inhibited 5-HT4 responses to 5-HT and reduced basal agonist-independent cAMP production.{34070} In several animal models, low concentrations of SB-207266 blocked exogenous 5-HT-mediated sensitization of intestinal peristalsis.{34073, 34072, 34071} In a dog model, SB-207266 (0.1–100 pg/kg) dose-dependently reduced responses to 5-HT, with an ID50 value of 1.3 pg/kg.{34073} SB-206226 (0.5 mg/kg/24 h) improved cardiac function in a rat model of congestive heart failure.{34069}  

 

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Description

A selective, potent antagonist of the 5-HT4 receptor (pA2 value = 10.6 + 0.1; ID50 value = 1.3 pg/kg); inhibits responses to 5-HT and reduces basal agonist-independent cAMP production in COS7 cells; reduces gastrointestinal 5-HT4 receptor activity in animal models

Formal name: N-[(1-butyl-4-piperidinyl)methyl]-3,4-dihydro-2H-[1,3]oxazino[3,2-a]indole-10-carboxamide

Synonyms:  Piboserod

Molecular weight: 369.5

CAS: 152811-62-6

Purity: ≥95%

Formulation: A crystalline solid

Product Type|Biochemicals|Receptor Pharmacology|Antagonists||Research Area|Cardiovascular System|Cardiovascular Diseases|Heart Failure||Research Area|Neuroscience

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