An α-AR antagonist and vasoactive compound; binds to rat α1A- and α1B-ARs (Kis = 4.06 and 6.84 µM

Buflomedil (hydrochloride) – 5 g

Brand:
Cayman
CAS:
35543-24-9
Storage:
-20
UN-No:
Non-Hazardous - /

Buflomedil is a non-selective antagonist of α-adrenergic receptors (α-ARs) and vasoactive compound.{58021,58022,58023,58024} It binds to rat α1A- and α1B-ARs (Kis = 4.06 and 6.84 µM, respectively) and human platelet α2-ARs (IC50 = 1 µM) in radioligand binding assays.{58021,58022} Buflomedil (0.06-60 µM) inhibits contraction of isolated canine saphenous veins induced by phenylephrine, clonidine (Item No. 15949), sympathetic nerve stimulation, or norepinephrine.{58023} It inhibits ADP-, collagen-, or epinephrine-induced aggregation of isolated human platelets when used at a concentration of 100 µM.{58022} Buflomedil (10 mg/kg) reduces hippocampal neuronal cell death in a rat model of carotid clamping-induced ischemia-reperfusion injury.{58024}  

 

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Description

An α-AR antagonist and vasoactive compound; binds to rat α1A- and α1B-ARs (Kis = 4.06 and 6.84 µM, respectively) and human platelet α2-ARs (IC50 = 1 µM); inhibits phenylephrine-, clonidine-, sypathetic nerve stimulation-, or norepinephrine-induced contration of isolated canine saphenous veins from 0.06-60 µM; inhibits ADP-, collagen-, or epinephrine-induced aggregation of isolated human platelets at 100 µM; reduces hippocampal neuronal cell death in a rat model of carotid clamping-induced ischemia-reperfusion injury at 10 mg/kg

Formal name: 4-(1-pyrrolidinyl)-1-(2,4,6-trimethoxyphenyl)-1-butanone, monohydrochloride

Synonyms:  LL-1656

Molecular weight: 343.9

CAS: 35543-24-9

Purity: ≥95%

Formulation: A solid

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