A 5-HT2B receptor antagonist; binds to 5-HT2B receptors in isolated rat fundus (Kb = 0.177 nM); selective for 5-HT2B receptors over 5-HT2A and 5-HT2C receptors (Kis = 3.54 and 2.1 nM

LY272015 – 1 mg

Brand:
Cayman
CAS:
172895-15-7
Storage:
-20
UN-No:
Non-Hazardous - /

LY272015 is an antagonist of the serotonin (5-HT) receptor subtype 5-HT2B.{49231} It binds to 5-HT2B receptors in isolated rat fundus (Kb = 0.177 nM). LY272015 is selective for 5-HT2B receptors over 5-HT2A and 5-HT2C receptors (Kis = 3.54 and 2.1 nM, respectively), as well as α1-adrenergic receptors.{49231,52703} It reduces 5-HT-induced migration of isolated mouse aortic smooth muscle cells when used at a concentration of 100 nM.{52704} LY272015 (1 and 3 mg/kg) decreases mean arterial pressure in hypertensive DOCA-SALT rats.{52705}  

 

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Description

A 5-HT2B receptor antagonist; binds to 5-HT2B receptors in isolated rat fundus (Kb = 0.177 nM); selective for 5-HT2B receptors over 5-HT2A and 5-HT2C receptors (Kis = 3.54 and 2.1 nM, respectively), as well as α1-adrenergic receptors; reduces 5-HT-induced migration of isolated mouse aortic smooth muscle cells at 100 nM; decreases mean arterial pressure in hypertensive DOCA-SALT rats at 1 and 3 mg/kg

Formal name: 1-[(3,4-dimethoxyphenyl)methyl]-2,3,4,9-tetrahydro-6-methyl-1H-pyrido[3,4-b]indole, monohydrochloride

Synonyms: 

Molecular weight: 372.9

CAS: 172895-15-7

Purity: ≥98%

Formulation: A solid

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