Greenslade F C, Scott C K, Newquist K L, Krider K M, Chasin M
J Pharm Sci. 1982 Jan;71(1):94-100. doi: 10.1002/jps.2600710123.
Thirty-four vasodilators were screened in several in vitro biochemical assays related to smooth muscle excitation-contraction coupling, binding to beta 1-,beta 2-, and alpha-adrenergic receptors, inhibition of phosphodiesterase activity, and antagonism of calcium accumulation. Isoproterenol and perhexiline only exhibited binding to beta-adrenergic sites. Ergocryptine, tolazoline, and amotriphene only bound to alpha-adrenergic receptors. Leniquinsin, papaverine, proquazone, dioxyline, hoquizil, quazodine, and theophylline were active only as phosphodiesterase inhibitors. Isoxsuprine, nylidrin, and bencyclane bound to alpha- and beta-receptors. Pentoxifylline bound to beta 1-sites and inhibited phosphodiesterase. Cyclandelate bound to beta 2-sites and blocked calcium accumulation. Cinnarizine and flunarizine antagonized calcium accumulation and bound to alpha-sites. Prazosin bound to alpha-sites and inhibited phosphodiesterase. Ethaverine and dipyridamole were inhibitors of phosphodiesterase and calcium accumulation. Nafronyl bound to beta 2- and alpha-sites and antagonized calcium accumulation. Mebeverine bound to beta 2- and alpha-receptors and inhibited phosphodiesterase activity and calcium accumulation. Verapamil bound to alpha-sites, and blocked phosphodiesterase and calcium accumulation. Quinazosin bound to beta 2- and alpha-receptors and antagonized both phosphodiesterase activity and calcium accumulation. Vasodilators that were inactive in all assays included niacin, nicotinyl alcohol, inositol nicotinate, amyl nitrite, sodium nitroprusside, diazoxide, hydralazine, and protoveratrine. Vasodilators should not be considered as a single drug class since they act on various mechanisms related to coupling of neuronal excitation to muscular contractility.
在与平滑肌兴奋 - 收缩偶联、与β1 -、β2 - 和α - 肾上腺素能受体结合、抑制磷酸二酯酶活性以及拮抗钙蓄积相关的多种体外生化试验中，对34种血管扩张剂进行了筛选。异丙肾上腺素和哌克昔林仅表现出与β - 肾上腺素能位点结合。麦角隐亭、妥拉唑啉和阿莫曲芬仅与α - 肾上腺素能受体结合。雷诺辛、罂粟碱、丙磺舒、双氧嗪、霍喹嗪、夸唑定和茶碱仅作为磷酸二酯酶抑制剂有活性。异克舒令、尼立替林和苄环烷与α - 和β - 受体结合。己酮可可碱与β1 - 位点结合并抑制磷酸二酯酶。环扁桃酯与β2 - 位点结合并阻止钙蓄积。桂利嗪和氟桂利嗪拮抗钙蓄积并与α - 位点结合。哌唑嗪与α - 位点结合并抑制磷酸二酯酶。乙罂粟碱和双嘧达莫是磷酸二酯酶和钙蓄积的抑制剂。萘呋胺与β2 - 和α - 位点结合并拮抗钙蓄积。美贝维林与β2 - 和α - 受体结合并抑制磷酸二酯酶活性和钙蓄积。维拉帕米与α - 位点结合，并阻断磷酸二酯酶和钙蓄积。喹唑嗪与β2 - 和α - 受体结合并拮抗磷酸二酯酶活性和钙蓄积。在所有试验中均无活性的血管扩张剂包括烟酸、烟醇、烟酸肌醇酯、亚硝酸异戊酯、硝普钠、二氮嗪、肼屈嗪和原藜芦碱。血管扩张剂不应被视为单一的药物类别，因为它们作用于与神经元兴奋与肌肉收缩偶联相关的多种机制。
