Székely J I
Gyógyszerkutató Intézet Kft., 1045 Budapest, Berlini-út 47-49.
Acta Pharm Hung. 2001;71(1):25-39.
The contribution of the research workers of the Institute for Drug Research to some early discoveries in the field of endorphins is reviewed. The author takes pride in the fact the analgesic action of beta-endorphin was described in his laboratory concurrently with an American and a British group, respectively. The other main findings of his laboratory include demonstration of the cross-tolerance between beta-endorphin and morphine, description of the elevation of the pain threshold upon inhibition of the breakdown endogenous opioids by intracerebroventricular administration of bacitracin, attenuation of morphine tolerance by alpha-MSH and Met-enkephalin, pharmacological development and clinical examination of a highly potent enkephalin analogue, (D-Met2,Pro5)-enkephalinamide, coded as GYKI 14,238.
本文回顾了药物研究所研究人员在脑啡肽领域的一些早期发现所做出的贡献。作者对以下事实感到自豪:在他的实验室中,β-内啡肽的镇痛作用分别与一个美国小组和一个英国小组同时被描述。他的实验室的其他主要发现包括证明β-内啡肽与吗啡之间的交叉耐受性;描述通过脑室内注射杆菌肽抑制内源性阿片类物质分解后疼痛阈值的升高;α-促黑素和甲硫氨酸脑啡肽对吗啡耐受性的减弱;一种高效脑啡肽类似物(D-蛋氨酸²,脯氨酸⁵)-脑啡肽酰胺(编码为GYKI 14,238)的药理学开发和临床研究。