科研之友
微信
新浪微博
Facebook
分享链接
摘要
Two novel opioid analogues have been designed by substituting the native d-Ala residues in position 2,2' of biphalin with two residues of d-penicillamine or l-penicillamine and by forming a disulfide bond between the thiol groups. The so-obtained compound <bold>9</bold> containing d-penicillamines showed excellent mu/delta mixed receptor affinities (K-i(delta) = 5.2 nM; K-i mu = 1.9 nM), together with an efficacious capacity to trigger the second messenger and a very good in vivo antinociceptive activity, whereas product <bold>10</bold> was scarcely active. An explanation of the two different pharmacological behaviors of products <bold>9</bold> and <bold>10</bold> was found by studying their conformational properties.
- 出版日期2014-9
