A β-adrenergic and 5-HT1A receptor antagonist (IC50s = 2.8 and 9.9 nM

Penbutolol (hemisulfate) – 100 mg

Brand:
Cayman
CAS:
38363-32-5
Storage:
-20
UN-No:
Non-Hazardous - /

Penbutolol is an antagonist of β-adrenergic receptors (β-ARs; IC50 = 2.8 nM) and the serotonin (5-HT) receptor subtype 5-HT1A (IC50 = 9.9 nM).{53262} It inhibits adenylate cyclase activity induced by the β-AR agonist isoprenaline (isoproterenol; Item No. 15592) in guinea pig myocardial membranes with a Ki value of 2.4 nM.{53263} Penbutolol reduces basal renin activity and blood pressure in spontaneously hypertonic rats.{53264} It decreases isolation-induced aggressive behavior in mice (ED50 = 56 µmol/kg) and reverses reductions in aggression induced by 8-hydroxy-DPAT (Item No. 22608) and TFMPP with ED50 values of 8.1 and 2.1 µmol/kg, respectively.{53262} Formulations containing penbutolol were previously used in the treatment of arterial hypertension.  

 

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SKU: 29524 - 100 mg Category:

Description

A β-adrenergic and 5-HT1A receptor antagonist (IC50s = 2.8 and 9.9 nM, respectively); inhibits isoprenaline-induced adenylate cyclase activity in guinea pig myocardial membranes (Ki = 2.4 nM); reduces basal renin activity and blood pressure in spontaneously hypertonic rats; decreases isolation-induced aggressive behavior in mice (ED50 = 56 µmol/kg) and reverses 8-hydroxy-DPAT- and TFMPP-induced reductions in aggression (ED50s = 8.1 and 2.1 µmol/kg, respectively)

Formal name: (2S)-1-(2-cyclopentylphenoxy)-3-[(1,1-dimethylethyl)amino]-2-propanol, hemisulfate

Synonyms:  HOE 39-893d

Molecular weight: 340.5

CAS: 38363-32-5

Purity: ≥95%

Formulation: A solid

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