Crystals of 4-diphenylcarbamyl-N-methylpiperidine methobromide contain 2 conformers, one with the ester group equatorial and the other with the ester group axial to the piperidine ring. 2. In both conformers and diphenylcarbamyl nitrogen is trigonally substituted and flat compared with the tetrahedral substitution of the corresponding carbon atom in 4-diphenylacetoxy-N-methylpiperidine (4-DAMP) methiodide. 3. The low activity and selectivity of the carbamate at muscarinic receptors is comparable with that of compounds containing only one phenyl ring, e.g. phenylacetyl-N-methyl piperidine methiodide or phenylacetylcholine. It is suggested that the high affinity of 4-DAMP metho-salts and their selectivity depend upon interactions with groups arranged in three dimensions and that the trigonal arrangement about the nitrogen atom in the carbamate makes it impossible for both benzene rings to interact at once.
摘要
4 - 二苯基甲氨甲酰基 - N - 甲基哌啶甲溴化物晶体含有两种构象异构体,一种构象异构体中酯基处于平伏键,另一种构象异构体中酯基处于与哌啶环相连的直立键。2. 在两种构象异构体中,二苯基甲氨甲酰基氮原子呈三角取代且呈平面结构,与之相比,4 - 二苯基乙酰氧基 - N - 甲基哌啶(4 - DAMP)甲碘化物中相应碳原子呈四面体取代。3. 氨基甲酸酯在毒蕈碱受体处的低活性和选择性与仅含一个苯环的化合物相当,例如苯乙酰基 - N - 甲基哌啶甲碘化物或苯乙酰胆碱。有人提出,4 - DAMP甲盐的高亲和力及其选择性取决于与三维排列基团的相互作用,并且氨基甲酸酯中氮原子周围的三角排列使得两个苯环无法同时相互作用。