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编 号：F401663
分子式：C18H22ClNO
分子量：303.83
分子式：C18H22ClNO
分子量：303.83
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CAS No: 59-96-1
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生物活性：
Phenoxybenzamine is a nonselective, irreversible, orally active α-adrenoceptor antagonist that is commonly used for the research of hypertension, specifically caused by pheochromocytoma. Phenoxybenzamine also shows antitumor activity.
体内研究：
Phenoxybenzamine hydrochloride (20 nM; s.c.; 2-day interval for 26 days) shows anti-tumorigenic effect in mice.Phenoxybenzamine (1.0 mg/kg; i.v.; daily for 30 days) is neuroprotective in a rat model of severe traumatic brain injury.Animal Model:Nude mice, U87MG tumor model
Dosage:20 nM
Administration:Subcutaneous injection, 2-day interval for 26 days
Result:Reduced the tumor cells.
Animal Model:Male Wistar rats (350–500 g), traumatic brain injury (TBI) model
Dosage:1.0 mg/kg
Administration:Intravenous injection, daily for 30 days
Result:Showed significant improvements in neurological severity score (NSS) and foot fault scoring on days 14, 21, and 30. Reduced cognitive impairment associated with severe TBI and reduced the expression of pro-inflammatory genes.
体外研究：
Phenoxybenzamine hydrochloride (0-100 μM; 96 h) markedly inhibits U251 and U87MG cells proliferation.Phenoxybenzamine hydrochloride (10 μM; 24 h or 72 h) inhibits migration and invasion of U251 and U87MG cells.Phenoxybenzamine hydrochloride (10 μM; 12 h) activates LINGO-1 and inhibits the TrkB-Akt pathway.Phenoxybenzamine (0.1 μM-1 mM; 0-16 h) prevents hippocampal cell death after oxygen glucose deprivation.
Phenoxybenzamine is a nonselective, irreversible, orally active α-adrenoceptor antagonist that is commonly used for the research of hypertension, specifically caused by pheochromocytoma. Phenoxybenzamine also shows antitumor activity.
体内研究：
Phenoxybenzamine hydrochloride (20 nM; s.c.; 2-day interval for 26 days) shows anti-tumorigenic effect in mice.Phenoxybenzamine (1.0 mg/kg; i.v.; daily for 30 days) is neuroprotective in a rat model of severe traumatic brain injury.Animal Model:Nude mice, U87MG tumor model
Dosage:20 nM
Administration:Subcutaneous injection, 2-day interval for 26 days
Result:Reduced the tumor cells.
Animal Model:Male Wistar rats (350–500 g), traumatic brain injury (TBI) model
Dosage:1.0 mg/kg
Administration:Intravenous injection, daily for 30 days
Result:Showed significant improvements in neurological severity score (NSS) and foot fault scoring on days 14, 21, and 30. Reduced cognitive impairment associated with severe TBI and reduced the expression of pro-inflammatory genes.
体外研究：
Phenoxybenzamine hydrochloride (0-100 μM; 96 h) markedly inhibits U251 and U87MG cells proliferation.Phenoxybenzamine hydrochloride (10 μM; 24 h or 72 h) inhibits migration and invasion of U251 and U87MG cells.Phenoxybenzamine hydrochloride (10 μM; 12 h) activates LINGO-1 and inhibits the TrkB-Akt pathway.Phenoxybenzamine (0.1 μM-1 mM; 0-16 h) prevents hippocampal cell death after oxygen glucose deprivation.
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