Dimmock J R, Hamon N W, De Gooijer C A, Grant G F, Jonnalagadda S S, Hancock D S
College of Pharmacy, University of Saskatchewan, Saskatoon, Canada.
Pharmazie. 1989 Aug;44(8):560-2.
5-Dimethylamino-1-phenyl-1-penten-3-one hydrochloride (1a) has high inhibiting properties in mitochondria isolated from mice liver. Substitution at the 4-methylene group of 1a by different alkyl substituents lead to compounds with wide variation in respiration-inhibiting properties. No correlations were found between either the Charton steric parameter (v), Taft inductive value (f*) or fragmental constant (f) of the substituents at position 4 of the Mannich bases with inhibition of respiration. However the biological results suggested two receptor sites were present in the mitochondria which may interact with the Mannich bases namely a common receptor for all compounds and in addition a narrow hydrophobic binding area which can accommodate a n-butyl or higher alkyl groups which are present in some of the compounds.
5-二甲基氨基-1-苯基-1-戊烯-3-酮盐酸盐（1a）对从小鼠肝脏分离出的线粒体具有高度抑制特性。在1a的4-亚甲基上用不同的烷基取代基进行取代，会得到呼吸抑制特性差异很大的化合物。在曼尼希碱4位取代基的查顿立体参数（v）、塔夫脱诱导值（f*）或碎片常数（f）与呼吸抑制之间均未发现相关性。然而，生物学结果表明线粒体中存在两个可能与曼尼希碱相互作用的受体位点，即所有化合物的共同受体，此外还有一个狭窄的疏水结合区域，它可以容纳某些化合物中存在的正丁基或更高的烷基。
