Coppi G
Forschungszentrum, Poli Industria Chimica S.p.A., Rozzano, Mailand, Italien.
Arzneimittelforschung. 1992 Nov;42(11A):1381-90.
A pharmacological and toxicological review of dihydroergocristine (DHEC, CAS 17479-19-5) is reported. Dihydroergocristine exercises a double agonistic/antagonistic activity on dopaminergic and adrenergic receptors; it also shows a non competitive antagonistic effect on serotonin receptors. The central effects of DHEC depend on the initial cerebrovascular resistance. DHEC exercises an inhibiting effect on the anaerobic glycolysis and on aerobic oxidation processes. It increases the cerebral blood flow and the oxygen consumption of the brain. Dihydroergocristine protects the brain against the metabolic effects of ischaemia by acting at a cellular level. In age-related modifications of the cerebral enzymatic antioxidant system DHEC increases the reduced glutathione. DHEC exercises a vasoregulating amphoteric action which depends on the initial tonus: it is hypotensive in hypertensive and normotensive animals but it is hypertensive in hypotensive animals. The results of acute and chronic toxicity in rats, dogs and monkeys, of teratogenesis and fertility in rats and rabbits and of mutagenic tests show that DHEC is a non toxic and well tolerated drug.
本文报道了双氢麦角克碱(DHEC,化学物质登记号17479 - 19 - 5)的药理学和毒理学综述。双氢麦角克碱对多巴胺能和肾上腺素能受体具有双重激动/拮抗活性;它对血清素受体也表现出非竞争性拮抗作用。双氢麦角克碱的中枢作用取决于初始脑血管阻力。双氢麦角克碱对无氧糖酵解和有氧氧化过程具有抑制作用。它增加脑血流量和脑氧耗。双氢麦角克碱通过在细胞水平发挥作用,保护大脑免受缺血的代谢影响。在与年龄相关的脑酶抗氧化系统改变中,双氢麦角克碱增加还原型谷胱甘肽。双氢麦角克碱发挥血管调节两性作用,这取决于初始张力:在高血压和血压正常的动物中它是降压的,但在低血压动物中它是升压的。大鼠、狗和猴子的急性和慢性毒性试验结果,大鼠和兔子的致畸性和生育力试验结果以及致突变试验结果表明,双氢麦角克碱是一种无毒且耐受性良好的药物。