卤代苄基异喹啉类化合物的合成

卤代苄基异喹啉类化合物的合成伍家泉，陈虹，王火，庞开圻，陈琪瑞（开平彼迪药业有限公司，开平５２９３３１）（天津武警医学院，天津３００１６２）苄基异喹啉类生物碱广泛存在于天然植物中，其中许多具有重要的生理活性，尤其在心血管方面的作用引人注目。曾证明唐松...     

婴幼儿腹腔镜手术中二氧化碳气腹对米库氯铵 作用时间的影响

目的 探讨小儿腹腔镜手术二氧化碳CO2 气腹对米库氯铵作用时间的影响。方法 选取全身 麻醉气管插管下行择期腹股沟疝修补术的61 例患儿，随机分为腹腔镜组（31 例）和开腹组（30 例）。静脉 给予丙泊酚2.5 mg/kg、芬太尼2 μg/kg 及米库氯铵0.2 mg/kg 进行麻醉诱导，术中吸入50% 一氧化二氮 N2O+50% 氧气O2+ 七氟醚维持麻醉，麻醉深度维持在1.2 ～ 1.4 MAC。使用肌松监测仪记录4 个成串刺激（TOF）； 分别记录T1 完全消失时间（Ta）（即肌松药完全起效时间）；T1 消失至T1 恢复到对照值25% 的时间（Tb）（即 肌松药有效作用时间）。检测手术前后24 h 血浆胆碱酯酶（CHE）、谷丙转氨酶（ALT）、谷草转氨酶（AST） 及总胆红素（TBIL）浓度。结果 两组米库氯铵Ta、Tb 比较，差异无统计学意义（P >0.05）；两组术前、术 后24 h 的CHE、ALT、AST 及TBIL 浓度比较，差异无统计学意义（P >0.05）。结论 婴幼儿CO2 气腹米库氯 铵的完全起效时间和有效作用时间无影响。     

Cardiovascular effects of plant secondary metabolites norarmepavine,coclaurine and norcoclaurine

The cardiovascular effects of (±)-norarmepavine, a benzylisoquinoline alkaloid of natural origin, have been determined on anaesthetized rats in vivo, on spontaneously beating atria and on aortic smooth muscle. In aorta, the effects of (±)-coclaurine and (±)-norcoclaurine, benzylisoquinolines with a related structure, were also compared. (±)-Norarmepavine (10 mg/kg i.v.) decreased the mean arterial pressure and heart rate by 45% and 21%, respectively. (±)-Norarmepavine (10⁻⁵–10⁻³ M ) showed a negative chronotropic effect on rat-isolated atria, decreasing the spontaneous frequency by about 54%. Aortic rings contracted with KCl 70 mM were relaxed in a concentration-dependent manner by (±)-norarmepavine, (±)-coclaurine and (±)-norcoclaurine (10⁻⁶–10⁻³ M ). The two earlier alkaloids exhibited an efficacy similar to verapamil, relaxing the aortic rings by 100%. (±)-Norcoclaurine exhibited a lower efficacy. These results point to the importance of methylation of these compounds. The rank order of potency was: (±)-verapamil > (±)-norarmepavine > (±)-norcoclaurine > (±)-coclaurine. The alkaloids shifted to the right the calcium-dependent contraction curves, denoting a calcium antagonist-like effect; however, only a 10-fold increment of (±)-norcoclaurine concentration produced an equivalent effect. Our results demonstrate the hypotensive and bradycardic properties of (±)-norarmepavine. It is proposed that this alkaloid could somehow modulate calcium entry, its intracellular release or the calcium sensitivity of the cell contractile-machinery, previously postulated for coclaurine. (±)-Norcoclaurine effects reported here are not in agreement with the proposal of (±)-norcoclaurine as a calcium channel activator or β₁-adrenoceptor agonist. © 1998 John Wiley & Sons, Ltd.