Baldauf J, Wilbert H, Büch H P
Arzneimittelforschung. 1982;32(10):1281-6.
The (-)-enantiomers of 1-methyl-5-phenyl-5-propyl barbituric acid (MPPB) and 1-methyl-5-phenyl-5-butyl barbituric acid (MPBB) injected i.v. depress blood pressure and heart rate of rats to a fourfold higher degree than the (+)-enantiomers. These stereoselectively different actions on blood pressure and heart rate are abolished after pretreatment with reserpine. Stereoselective differences are not existent with regard of the negative inotropic action (isolated left atrium and papillary muscle), the negative chronotropic action (isolated right atrium) and the blockade of tension development induced by noradrenaline at the isolated ductus deferens. The enantiomers of MPPB and MPBB exhibit stereoselectively different influence on the sympathetic outflow of intact rats during barbiturate-induced hypotension and bradycardia: 1 min after injection the efferent activity of neck sympathetic nerve is increased only if the (+)-enantiomers are given (twofold of the control). 5 min after application only in the presence of the (-)-enantiomers a slight increase of the efferent activity is observed.
静脉注射1-甲基-5-苯基-5-丙基巴比妥酸(MPPB)和1-甲基-5-苯基-5-丁基巴比妥酸(MPBB)的(-)-对映体对大鼠血压和心率的抑制程度比对映体(+)-对映体高四倍。用利血平预处理后,这些对血压和心率的立体选择性不同作用被消除。在负性肌力作用(离体左心房和乳头肌)、负性变时作用(离体右心房)以及去甲肾上腺素对离体输精管张力发展的阻断方面不存在立体选择性差异。在巴比妥酸盐诱导的低血压和心动过缓期间,MPPB和MPBB的对映体对完整大鼠的交感神经传出表现出立体选择性不同的影响:注射后1分钟,仅给予(+)-对映体时颈部交感神经的传出活动增加(为对照的两倍)。给药5分钟后,仅在存在(-)-对映体的情况下观察到传出活动略有增加。