摘要
5-HT重摄取抑制/5-HT1A受体拮抗双重作用抗抑郁药是在单胺递质学说的基础上研发的新一代抗抑郁药,此类药物研发的策略主要是通过分子拼合原理,在单一分子中引入2种药效团在体内共同发挥抗抑郁作用。文中对该类药物中几种典型的结构构效关系及生物活性评价结果进行综述,以期为抗抑郁药物的研发提供参考。新型化合物在有效性、安全耐受性及起效时间等方面表现出很多优势,但是目前还没有相关的临床报道数据。
Based on monoamine hypothesis, new antidepressants with serotonergic activity at both the 5- HT1A receptor and 5-HT transporter have been developed. The generic strategy in designing target molecules uses the termed “overlapping type approach”. Both pharmacophores in single target molecule exert the antidepressive effect together. As a clue to antidepressant research, the current knowledge concerning several kinds of new antidepressants about bioactivity and structure-effect relations was summarized in this paper. The dual acting antidepressants possess some superiorities in respects of efficacy, safety, tolerance and onset of action, but there are till no clinical data to support the superiorities.
出处
《中国新药杂志》
CAS
CSCD
北大核心
2008年第16期1381-1384,1394,共5页
Chinese Journal of New Drugs
