Walton K G, Liepmann P, Baldessarini R J
Eur J Pharmacol. 1978 Nov 15;52(2):231-4. doi: 10.1016/0014-2999(78)90211-x.
Phenoxybenzamine at a concentration of 2 X 10(-6 M) produced half-maximal inhibition of dopamine-stimulated adenylate cyclase activity in homogenates of rat striatum. Inhibition was sharply dependent on time and temperature of preincubation with the inhibitor. When included in the preincubation medium, dopamine was nearly 8 times more effective than norepinephrine at protecting against this inhibition, whereas neither isoproterenol nor methoxamine appeared to protect at all. These results suggest a direct, and possibly irreversible, interaction of phenoxybenzamine with the dopamine-binding component of the adenylate cyclase.
浓度为2×10⁻⁶M的酚苄明对大鼠纹状体匀浆中多巴胺刺激的腺苷酸环化酶活性产生半数最大抑制作用。抑制作用强烈依赖于与抑制剂预孵育的时间和温度。当多巴胺包含在预孵育培养基中时,其在防止这种抑制方面的效力比去甲肾上腺素高近8倍,而异丙肾上腺素和甲氧明似乎根本没有保护作用。这些结果表明酚苄明与腺苷酸环化酶的多巴胺结合成分存在直接且可能不可逆的相互作用。