An α-AR antagonist; inhibits norepinephrine-induced inositol phosphate formation in HEK293 cells expressing α1-ARs (EC50s = 125.9-316.2 nM)

Phenoxybenzamine (hydrochloride) – 5 g

Brand:
Cayman
CAS:
63-92-3
Storage:
-20
UN-No:
Non-Hazardous - /

Phenoxybenzamine is an antagonist of α-adrenergic receptors (α-ARs).{53203,26625} It inhibits norepinephrine-induced inositol phosphate formation in HEK293 cells expressing α1-ARs (EC50s = 125.9-316.2 nM), as well as radioligand binding to α2A-, α2B-, and α2C-ARs in CHO cell membranes (Kis = 60, 10, and 60 nM, respectively). Phenoxybenzamine (0.5-5 µM) decreases norepinephrine-, histamine-, and calcium-induced contractions in isolated rabbit aortic strips.{53204} It also inhibits proliferation of nine cancer cell lines, including lymphoma, breast, and lung cancer cells, with IC50 values ranging from 29.5 to 99.8 µM.{53205} Phenoxybenzamine (3-1,000 µg/kg) reduces increases in diastolic blood pressure induced by the α-AR agonists cirazoline (Item No. 21791), St-587, Sgd 101/75, and B-HT 920 (Item No. 14177) in pithed rats.{53206} It also decreases the time to find the platform in the Morris water maze, indicating restored spatial memory, in a rat model of fluid percussion-induced traumatic brain injury (TBI).{53207} Formulations containing phenoxybenzamine have been used in the treatment of hypertension and hyperhidrosis associated with pheochromocytomas, an adrenal medullary neuroendocrine tumor.  

 

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Description

An α-AR antagonist; inhibits norepinephrine-induced inositol phosphate formation in HEK293 cells expressing α1-ARs (EC50s = 125.9-316.2 nM), as well as radioligand binding to α2A-, α2B-, and α2C-ARs in CHO cell membranes (Kis = 60, 10, and 60 nM, respectively); decreases norepinephrine-, histamine-, and calcium-induced contractions in isolated rabbit aortic strips from 0.5-5 µM; inhibits proliferation of a variety of cancer cell lines (IC50s = 29.5-99.8 µM); reduces cirazoline-, St-587-, Sgd 101/75-, and B-HT 920-induced increases in diastolic blood pressure in pithed rats; decreases the time to find the platform in the Morris water maze, indicating restored spatial memory, in a rat model of fluid percussion-induced TBI

Formal name: N-(2-chloroethyl)-N-(1-methyl-2-phenoxyethyl)-benzenemethanamine, monohydrochloride

Synonyms:  NSC 37448

Molecular weight: 340.3

CAS: 63-92-3

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Receptor Pharmacology|Antagonists||Research Area|Cardiovascular System|Cardiovascular Diseases|Hypertension||Research Area|Cardiovascular System|Vasculature|Vasodilation||Research Area|Neuroscience|Behavioral Neuroscience|Learning & Memory

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