A β3-AR antagonist in animal models; less selective for human β-AR subtypes (Kis = 16.4

SR 59230A (hydrochloride) – 5 mg

Brand:
Cayman
CAS:
1135278-41-9
Storage:
22
UN-No:
Non-Hazardous - /

SR 59230A (hydrochloride) is a β3-adrenergic receptor (β3-AR) antagonist (pA2s = 8.76, 7.31, and 6.63 in rat proximal colon, guinea pig atrium, and guinea pig trachea, respectively).{34206} It is less selective for β3-AR in cells transfected with the human β-AR subtypes (Kis = 16.4, 61.9, and 122 nM for β1-, β2-, and β3-AR, respectively).{34205} At low concentrations, SR 59230A blocks MDMA-induced hyperthermia, while at high concentrations it blocks hyperthermia but also increases heat loss through an α1-AR antagonistic mechanism.{34203} In adipocytes, it induces phosphorylation of p38 MAPK via the Gs pathway.{34207} It has also been used in studies of heart failure to elucidate the role of the β3-ARs.{34204}  

 

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Description

A β3-AR antagonist in animal models; less selective for human β-AR subtypes (Kis = 16.4, 61.9, and 122 nM for β1-, β2-, and β3-AR, respectively); blocks MDMA-induced hyperthermia at low and high concentrations with some α1-AR antagonist properties

Formal name: (2S)-1-(2-ethylphenoxy)-3-[[(1S)-1,2,3,4-tetrahydro-1-naphthalenyl]amino]-2-propanol, monohydrochloride

Synonyms: 

Molecular weight: 361.9

CAS: 1135278-41-9

Purity: ≥99%

Formulation: A solid

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

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