Gero A
Life Sci. 1985 Mar 18;36(11):1021-4. doi: 10.1016/0024-3205(85)90486-2.
The history of models for opioid drug receptors is traced and two currently proposed models are compared, the first envisaging two rigid receptors, one for agonists and one for antagonists, while the second model postulates one single flexible receptor which in its native conformation fits opioid antagonists but is distorted when it binds to agonists. Important recent experiments are satisfactorily interpreted by both models but the flexible one-receptor model requires fewer assumptions and explains more facts.
追溯了阿片类药物受体模型的历史，并比较了目前提出的两种模型。第一种模型设想有两种刚性受体，一种用于激动剂，一种用于拮抗剂；而第二种模型假定有一个单一的柔性受体，其天然构象适合阿片类拮抗剂，但在与激动剂结合时会发生扭曲。近期的重要实验两种模型都能给出令人满意的解释，但柔性单受体模型所需的假设更少，能解释更多事实。
