A comparison of solution, solid state and theoretical conformations of morphine.
A comparison of solution, solid state and theoretical conformations of morphine.
复制标题
吗啡溶液、固态和理论构象的比较。
DOI：
10.1016/s0006-291x(81)80189-1
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发表时间：
1981
影响因子：
3.1
通讯作者：
Glasel,JA
中科院分区：
文献类型：
--
作者：
Glasel,JA
利用甚高频1h核磁共振首次证实了融合多环分子中n -取代哌啶环的氮反转。讨论的分子是强效阿片激动剂吗啡，其中哌啶环已知在受体介导的药理作用中至关重要。以往，基于固体构象和理论构象的研究，普遍认为哌啶环的构象仅为N-R、赤道构象。目前的工作表明轴向和赤道形式之间的交换速率相对较慢，因此需要重新评估以前的文献，适用于吗啡的受体活性构象。
Using very high frequency1H nuclear magnetic resonance, nitrogen inversion in the N-substituted piperidine ring of a fused polycyclic molecule is demonstrated for the first time. The molecule discussed is the potent opiate agonist morphine where the piperidine ring is known to be of vital importance in receptor mediated pharmacological action. Previously, it has been accepted that the conformation of the piperidine ring was solely N-R, equatorial, on the basis of solid state and theoretical conformation studies. The present work demonstrates a relatively slow rate of interchange between the axial and equatorial forms and therefore requires a reappraisal of the previous literature as applied to the receptor active conformation of morphine.