离子对RP—HPLC法测定平消胶囊中士的宁的含量

目的:建立平消胶囊中士的宁的质量控制方法。方法:采用高效液相色谱法。色谱条件为 C(18)柱(250 mm×4.6 mm,5μm),乙腈-0.02 mol·L~(-1)十二烷基硫酸钠溶液(用磷酸调节 pH 至3.0)(30∶70)为流动相,流速1.0 mL·min~(-1),检测波长254 nm,柱温35℃。结果:士的宁峰与其他峰分离良好,阴性样品亦无干扰。以峰面积积分值为纵坐标,以进样量为横坐标,绘制标准曲线,结果士的宁进样量在0.1004～0.502μg范围内呈良好的线性关系,加样回收率为98.1%,RSD=0.95%(n=5)。结论:通过在流动相中加入十二烷基硫酸钠作为离子对试剂,可以使平消胶囊中士的宁通过 C_(18)柱得到良好的分离。本文方法的灵敏度、精密度和重复性均良好,能有效控制平消胶囊的质量。     

士的宁敏感的甘氨酸受体对吸入麻醉药催眠和镇痛作用的影响

目的探讨士的宁(strychnine,Stry)敏感的甘氨酸受体(strychnine-sensitive glycine receptor,GlyR)与吸入麻醉药异氟烷、恩氟烷、七氟烷和乙醚催眠、镇痛作用的关系。方法建立小鼠腹腔注射吸入麻醉药催眠、镇痛模型,在催醒和热板实验中分别观察侧脑室(intracerebroventricular,icv)或鞘内(intrathecal,it)注射不同剂量士的宁对小鼠睡眠时间(sleeping time,ST)和热板疼痛指数(pain index in hot-platetest,HPPI)的影响。结果催醒实验中,士的宁1、2、4μg icv对上述4种吸入麻醉药的ST均无影响(P>0.05);热板实验中,士的宁0.1、0.2、0.4μg it能够剂量依赖性地减少吸入麻醉药恩氟烷、七氟烷和乙醚镇痛小鼠的HPPI(P<0.05,P<0.01);士的宁0.1μg it对异氟烷镇痛小鼠的HPPI没有影响(P>0.05),0.2、0.4μg it可减少异氟烷镇痛小鼠的HPPI(P<0.05,P<0.01)。结论士的宁敏感的甘氨酸受体是吸入麻醉药异氟烷、恩氟烷、七氟烷和乙醚镇痛作用的重要靶位,但与其催眠作用关系不大。     

GC-MS法测定疏风活络丸中伪麻黄碱、麻黄碱、士的宁和马钱子碱的含量

目的:建立疏风活络丸中伪麻黄碱、麻黄碱、士的宁和马钱子碱含量的GC-MS测定方法.方法:采用 Variancp-sil 8CB Low bleed/MS毛细管柱(30mx250μm,O.25μm)分离,升温程序:起始温度50℃,保持1min,以25℃/min升至135℃,保持6min,以30℃/min升至300℃,保持22min.进样口温度为280 ℃;载气为He,恒流方式,柱流量为1mL/min,不分流进样1μL.MS采用EI离子源,离子源温度230℃;电子能量70eV,传榆管温度300℃,全扫描方式采集定性,质量范围40-450m/z;伪麻黄碱、麻黄碱采用总离子定量,士的宁和马钱子碱采用选择离子定量.结果:4种生物碱达到良好分离.方法平均回收率分别为伪麻黄碱97.82%(RSD 2.70%)、麻黄碱98.76%(RSD 3.23%)、士的宁98.00%(RSD 2.18%)和马钱子碱98.19%(RSD 1.89%)(n=6).结论:所建立的方法可靠,能准确测定疏风活络丸中4种生物碱类的含量.     

Evidence in favor of a neurotransmitter role of glycine in the rat cerebral cortex

In the present study we analyze whether glycine satisfies some electrophysiological and biochemical criteria to consider it as a putative transmitter in the rat cerebral cortex. Intracellular recordings from rat sensory-motor cortex showed that in 15-20% of the tested neurons glycine hyperpolarized the cell membrane, decreased the firing rate and flattened the evoked EPSP-IPSP sequence by increasing the membrane conductance. The iontophoretic application of strychnine antagonized the block of 'spontaneous' firing and the membrane hyperpolarization induced by glycine. Moreover, in a group of neurons, strychnine decreased the amplitude and duration of the IPSP and brought back the membrane potential to resting values. Previously accumulated [3H]glycine and endogenous glycine were released from cortical synaptosomal preparations by depolarizing stimuli in a Ca2+-dependent way. The release pattern of glycine was qualitatively similar in cortical and in spinal synaptosomes. [14C]Glycine was rapidly synthetized from [14C]serine in cortical synaptosomal preparations, and the newly formed [14C]glycine was released by depolarizing stimuli in a Ca2+-dependent way. It is concluded that glycine, which is generally considered as an inhibitory neurotransmitter in the spinal cord, medulla and pons, may also have a transmitter role in a discrete number of cortical neurons of some mammalian species.U     

Functional interaction between determinant and other foci of epileptiform activity created bilaterally in the cortex

Experiments on cats anesthetized with pentobarbital showed that on the creation of a hyperactive focus with a high level of excitation in the orbital or coronary cortex and a series of foci in the opposite neocortex a functional complex is formed, which works to the same program determined by the activity of the hyperactive focus. The latter plays the role of a determinant structure. Depression of activity of the determinant focus by pentobarbital leads to disinte-gration of the epileptic complex. Division of the rostral portion of the corpus callosum led to disturbance of synchronized operation of the determinant and other foci of epileptic activity. The results confirm the general concept of the role of determinant structures in the activity of the nervous system.Department of Pathological Physiology, N. I. Pirogov Doessa Medical Institute. (Presented by Academecian of the Academy of Medical Sciences of the USSR A. M. Chernukh.) Translated from Byulleten' Éksperimental'noi Biologii i Meditsiny, Vol. 86, No. 8, pp. 142–146, August, 1978.     

Anticonvulsant activity of muscimol against seizures induced by impairment of GABA-mediated neurotransmission

Muscimol is a potent in vivo agonist of gamma-aminobutyric acid (GABA) when tested iontophoretically and binds to GABA receptors in vitro. A study of muscimol effects on seizures induced by agents which impair GABA-mediated neurotransmission was performed in the rat. Muscimol delayed the onset of isoniazid-and picrotoxin-induced convulsions. The tonic forelimb extension component of bicuculline and metrazole seizures was abolished by muscimol. Inhibition of forelimb extension was chosen as an endpoint for comparison of clinically effective antiepileptics with muscimol. The order of potency was diazepam > muscimol > phénobarbital > phenytoin. Muscimol had no effect on strych-nine-induced convulsions. It is concluded that muscimol penetrates rat brain and specifically antagonizes seizures caused by GABA receptor blockade or depletion of brain GABA.     

麝香海马追风膏的质量标准研究

目的建立麝香海马追风膏的质量标准。方法用TLC或HPLC对处方中的药材进行了鉴别；用薄层扫描法测定士的宁的含量。结果在TLC图谱中可检出水杨酸甲酯、冰片、防风、川芎、当归、杜仲、没药的特征色谱；在HPLC图谱中可检出麝香酮的特征色谱；士的宁在0．2～1．0μg线性关系良好，r=0．998，平均回收率为87．2％。结论所建方法可行，重现性较好，可用于本品的质量控制。     

中药马钱子中毒死亡检验方法的研究

 目的建立人体生物检材中的士的宁和马钱子碱的检测方法。方法用GC/NPD及GC/MS检测马钱子药渣,喝剩的马钱子药液及人体肝脏中士的宁和马钱子碱。结果建立了多种样品中士的宁和马钱子碱的定性、定量分析方法。结论本方法操作简便,定性定量准确,可靠。用此方法可以准确测定生物检材(肝脏等)的士的宁和马钱子碱含量。     

正交试验法优选九分散中马钱子、麻黄提取工艺的研究

目的：采用正交试验法筛选九分散中马钱子和麻黄最佳提取工艺。方法：用薄层扫描法同时测定提取液中士的宁、马钱子碱和麻黄碱的含量。结果：溶剂量和提取次数对提取有显著性影响。最佳提取条件为药材量10倍量的水,提取3次,每次1h。