Mantegani S, Brambilla E, Caccia C, Chiodini L, Ruggieri D, Lamberti E, Di Salle E, Salvati P
Pharmacia and Upjohn, Nerviano, Milan, Italy.
Farmaco. 1998 Apr;53(4):293-304. doi: 10.1016/s0014-827x(98)00023-8.
The synthesis and antihypertensive activity of a series of 2,4-dioxoimidazolidin-1-yl and perhydro-2,4-dioxopyrimidin-1-yl ergoline derivatives are reported. The oral antihypertensive activity was studied in spontaneously hypertensive rats (SHRs) by measuring systolic blood pressure by an indirect tail-cuff method at different times after treatment. The prolactin lowering activity (indirectly measured by the nidation test) in rats and the oral acute toxicity in mice were also studied. The results of this study revealed potent antihypertensive ergoline derivatives devoid of side-effects related to the dopaminergic stimulation and the importance of the delta 9,10 double bond for conferring high potency within these compounds.
报道了一系列2,4-二氧代咪唑烷-1-基和全氢-2,4-二氧代嘧啶-1-基麦角灵衍生物的合成及其降压活性。通过间接尾套法在治疗后的不同时间测量自发性高血压大鼠（SHR）的收缩压，研究其口服降压活性。还研究了大鼠的催乳素降低活性（通过着床试验间接测量）和小鼠的口服急性毒性。该研究结果揭示了有效的降压麦角灵衍生物，其没有与多巴胺能刺激相关的副作用，以及δ9,10双键对于赋予这些化合物高效能的重要性。
