货号 | 16211-5g |
描述 | Phenoxybenzamine is a noncompetitive, irreversible α-adrenergic receptor antagonist (IC50 = 34.2 nM for α1; Kis = 0.06, 0.01, and 0.06 µM for α2A, α2B, and α2C, respectively) with antihypertensive activity.1,2 It forms a covalent bond with the adrenergic receptor, resulting in a slow onset and highly prolonged duration (2-8 days) of the blockade that subsides upon the synthesis of new adrenergic receptors.3 Due to its ability to selectively block longitudinal but not circular muscle contraction in human vas deferens, phenoxybenzamine has been explored as a form of male contraception to prevent sperm emission.4 The ability of phenoxybenzamine to block sympathetic signal transduction has also been explored in the context of complex regional pain syndrome.5 |
别名 | Dibenzyline™;NSC 37448; |
供应商 | Cayman |
应用文献 | |
1.Frang, H.,Cockcroft, V.,Karskela, T., et al. Phenoxybenzamine binding reveals the helical orientation of the third transmembrane domain of adrenergic receptors. The Journal of Biological Chemisty 276(33), 31279-31284 (2014). 2.Nagatomo, T.,Tsuchihashi, H.,Sasaki, S., et al. Displacement by α-adrenergic agonists and antagonists of 3H-prazosin bound to the α-adrenoceptors of the dog aorta and the rat brain. Japan J.Pharmacol. 37, 181-187 (1985). 3.Guzzetta, N.A. Phenoxybenzamine in the treatment of hypoplastic left heart syndrome: A core review. Anesthesia and Analgesia 105(2), 312-315 (2007). 4.Amobi, N.I.B. and Smith, I.C.H. Differential inhibition in the human vas deferens by phenoxybenzamine: a possible mechanism for its contraceptive action. Journal of Reproduction and Fertility 103(2), 215-221 (1995). 5.Inchlosa, M.A., Jr. Phenoxybenzamine in complex regional pain syndrome: potential role and novel mechanisms. Anesthesiol.Res.Pract. 2013, 1-7 (2013). | |
运输条件 | Room temperature in continental US; may vary elsewhere |
存放说明 | -20 |
纯度 | ≥98% |
计算分子量 | 340.3 |
分子式 | C18H22ClNO • HCl |
CAS号 | 63-92-3 |
稳定性 | ≥ 2 years |
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