粉防己碱有较好的钙拮抗作用,临床上已试用于治疗高血压,为简化结构,将粉防己碱还原裂解,以裂解产物为先导物,设计合成了一系列取代的四氢异喹啉衍生物,其中86040经药效学研究表明,静注或口服给药,对正常和高血压大鼠都有降压作用,本文还探讨了86040构象对活性的可能影响。 Tetrandrine has a good calcium antagonism, has been clinically tested for the treatment of high blood pressure, in order to simplify the structure, the tetrandrine tetrahedron reduction and lysis, the cleavage products as lead, designed and synthesized a series of tetrahydroisoquinoline Derivatives, of which 86040 pharmacodynamics studies have shown that intravenous or oral administration, both normal and hypertensive rats have antihypertensive effect, the paper also explored the possible impact of the 86040 conformation on the activity.