N-benzyl-N-(2-chloroethyl)-1-(2,3,4,5,6-pentadeuteriophenoxy)propan-2-amine:hydrochloride Chemische Eigenschaften,Einsatz,Produktion Methoden
Beschreibung
Phenoxybenzamine-d
5 is intended for use as an internal standard for the quantification of phenoxybenzamine by GC- or LC-MS. Phenoxybenzamine is an antagonist of α-adrenergic receptors (α-ARs). It inhibits norepinephrine-induced inositol phosphate formation in HEK293 cells expressing α
1-ARs (EC
50s = 125.9-316.2 nM), as well as radioligand binding to α
2A-, α
2B-, and α
2C-ARs in CHO cell membranes (K
is = 60, 10, and 60 nM, respectively). Phenoxybenzamine (0.5-5 μM) decreases norepinephrine-, histamine-, and calcium-induced contractions in isolated rabbit aortic strips. It also inhibits proliferation of nine cancer cell lines, including lymphoma, breast, and lung cancer cells, with IC
50 values ranging from 29.5 to 99.8 μM. Phenoxybenzamine (3-1,000 μg/kg) reduces increases in diastolic blood pressure induced by the α-AR agonists cirazoline , St-587, Sgd 101/75, and B-HT 920 in pithed rats. 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). Formulations containing phenoxybenzamine have been used in the treatment of hypertension and hyperhidrosis associated with pheochromocytomas, an adrenal medullary neuroendocrine tumor.
Verwenden
An irreversible α-antagonist. Used in the treatment of hypertension, it has a relatively slow onset and prolonged effect when compared to alternative α-blockers.
N-benzyl-N-(2-chloroethyl)-1-(2,3,4,5,6-pentadeuteriophenoxy)propan-2-amine:hydrochloride Upstream-Materialien And Downstream Produkte
Upstream-Materialien
Downstream Produkte
