胃肠宁对利血平所致大鼠脾虚模型的影响

目的 观察胃肠宁对大鼠脾虚证模型的影响.方法 36只大鼠随机分为正常对照组、脾虚模型组、四君子汤组和胃肠宁组,每组9只.采用利血平复制大鼠脾虚模型,连续灌胃14 d后,处死大鼠,分离肝、十二指肠和血清,测定各组大鼠血浆LDH、AKP、AchE、CK和肝组织匀浆中SOD、MDA、GSH-Px、NOS含量变化,并观察各组大鼠肝和十二指肠病理变化.结果 与正常对照组相比,脾虚模型组大鼠LDH、AchE、CK、SOD、GSH-Px、NOS含量明显降低,而AKP、MDA含量明显升高;与脾虚模型组相比,胃肠宁组LDH、AchE、CK、SOD、GSH-Px、NOS含量显著升高,而AKP、MDA含量显著降低;脾虚模型组大鼠肝组织发生广泛性颗粒变性和空泡变性;十二指肠上皮及绒毛明显脱落,大量炎性细胞浸润,杯状细胞数量明显减少,胃肠宁组与脾虚组相比,肝和十二指肠病理变化明显减轻.结论 胃肠宁对利血平所致大鼠脾虚具有较好的治疗作用.     

Centrally-administered glycine antagonists increase locomotion in monoamine-depleted mice

Summary It was shown in the present study that several structurally diverse antagonists of the glycine site of the NMDA receptor, including (R)-HA-966, L 689,560, 5,7-dichlorokynurenic acid, 7-chlorokynurenic acid, and two of ZENECA's novel pyridazinoindole glycine antagonists, caused marked reversal of akinesia when administered intrastriatally to monoamine depleted mice. Coinjection of the glycine agonist D-serine antagonized this locomotor stimulation. In addition, all glycine antagonists tested did not cause significant locomotor stimulation when intrastriatally administered to normal mice. These data suggest that glycine antagonists may offer therapeutic utility in the treatment of idiopathic Parkinson's disease.     

社区复方制剂抗高血压治疗研究:2年干预效果分析

目的:观察复方利血平氨苯喋啶片(北京降压0号)和复方利血平片(复方降压片)长期治疗轻、中度高血压的效果、安全性和依从性。方法 :选取2008-10至2009-01北京7个农村社区的轻、中度原发性高血压患者766例,年龄45~75岁,随机分成2组,分别服用北京降压0号(降压0号组,393例)和复方降压片(复降片组,373例),北京降压0号的剂量为0.5~1片/次,1次/d,复方降压片的剂量为1~2片/次,3次/d,观察时间为24个月。结果 :共710例患者完成试验,降压0号组与复降片组患者收缩压/舒张压下降幅度[(24.7±13.9/13.2±8.8)mm Hg vs(23.0±14.2/11.9±9.5)mm Hg,1 mm Hg=0.133 k Pa]、总有效率(89.0%vs 84.5%)、不良反应发生率(0.5%vs 1.34%)差异均无统计学意义(P0.05)。对于2级高血压患者,服药后1、6、12、24个月降压0号组舒张压的下降幅度均高于复降片组,差异有统计学意义(P0.05);降压0号组患者在服药24个月末依从性高于复降片组[(99.2±4.8)%vs(98.2±6.5)%],差异有统计学意义(P0.05)。结论 :北京降压0号依从性和对2级高血压的降压幅度高于复方降压片。两组不良反应差异不明显,均未见明显的不良作用。     

Regional uptake of iodine-125-metaiodobenzylguanidine in the rat heart

Regional uptake of iodine- 125-metaiodobenzylguanidine ([¹²⁵I]MIBG) was evaluated in normal (n=12) and reserpinized (n=12) rat hearts. At 15 min and 1, 3 and 6 h after injection of [¹²⁵I]MIBG, tissue activities were calculated for the right ventricular myocardium (RV), the whole left ventricular myocardium (whole LV), the epicardial layer of the left ventricular myocardium (Ep LV), the endocardial layer of the left ventricular myocardium (En LV), the basal segment of the left ventricular myocardium and the apical segment of the left ventricular myocardium. The uptake of [¹²⁵I]MIBG at 6 h after injection in the normal rat heart was higher in RV than in whole LV (0.45 ± 0.09% vs 0.30 ± 0.06% kg dose/g), and in Ep LV than in En LV (0.32 ± 0.07% vs 0.25 ± 0.05%). In the reserpinized rat heart, the difference in the uptake between Ep LV and En LV was smaller. This suggests that the difference in the regional [¹²⁵I] MIBG uptake might reflect different intravesicular uptake in the layers of the heart. To our knowledge, the low uptake in the endocardial layer was a new finding which seems to indicate a difference in innervation between the epicardial and endocardial layers of the left ventricle in the rat heart. Autoradiographic study also showed the low uptake of [¹²⁵I] MIBG in the endocardial layer, while homogeneous perfusion was observed with thallium-201, supporting the tissue uptake study. Thus, the endocardial and epicardial layers of the left ventricle in the rat heart were considered to be differently innervated.     

3,15-二乙酰苯甲酰乌头宁镇痛作用与中枢去甲肾上腺素能系统的关系

大鼠电刺激法及小鼠醋酸扭体法测痛表明,利血平,二乙基二硫代氨基甲酸钠(DDC),酚苄明和育亨宾均可使3,15-二乙酰苯甲酰乌头宁(DABA)镇痛作用减弱或消失,哌唑嗪及普萘洛尔对其作用无明显影响,结果提示DABA的镇痛作用可能与中枢去甲肾上腺素能系统的α_2受体有关.     

Influence of eicosanoids on serotonin release in the rat brain: inhibition by prostaglandins E1 and E2

Summary Cardiac alpha- and beta-adrenoceptor sensitivities were examined after chronic pretreatment of rats with reserpine. Increases in sensitivity would indicate that the receptor is under the influence of the sympathetic innervation, removal by catecholamine depletion with reserpine of the tonic effect of neurotransmitter release would permit receptor upregulation. The positive inotropic responses of paced left atria and papillary muscles and the positive chronotropic responses of spontaneously beating right atria were recorded. A concentration-response curve to isoprenaline (beta-adrenoceptor-mediated) was followed, in the presence of beta-blockade, by one to methoxamine (alpha-adrenoceptor-mediated). Methoxamine exerted positive inotropy of left atria and papillary muscles, the maxima being 43.2 ± 2.7 and 26.8 ± 4.4% of the isoprenaline maxima. A small positive chronotropy (16.5 ± 5.6% maximum) of right atria occurred. After pretreatment with reserpine (1.0 mg kg^–1 i.p. daily) for 7 days, the three preparations displayed supersensitivity to isoprenaline, revealed as a significant displacement (P < 0.05) of the concentration-response curves to the left of those for control rats. Reserpine pretreatment, however, had no effect on the sensitivity to methoxamine. The increase in beta-adrenoceptor sensitivity to isoprenaline after reserpine pretreatment was accompanied by a significant 41.3% increase (P < 0.05) in the number of [³H]-dihydroalprenolol ([³H]-DHA) binding sites (B _max) in ventricular membranes, although the dissociation constant (_{K D}) was unaffected. There were more alpha-adrenoceptor [³H]-prazosin binding sites in ventricular than atrial membranes. However, there was no difference in K _D or B _max between reserpine-pretreated and control tissues. It is proposed that the increase in beta-adrenoceptor sensitivity and binding sites arises from the depletion-induced loss of neuronal noradrenaline release onto the beta-adrenoceptors which are therefore directly under the influence of the neurotransmitter. The failure of cardiac alpha-adrenoceptors to exhibit supersensitivity and increased numbers suggests that they are not directly affected by the sympathetic innervation. Send offprint requests to K. J. Broadley at the above address     

一种白僵菌代谢产物提取物对利血平拮抗实验的影响

目的研究一种白僵菌代谢产物提取物 (BCEF)对利血平拮抗实验的影响。方法采用预防性一次灌胃给药、预防性连续灌胃给药、治疗性连续灌胃给药观察BCEF对利血平拮抗实验的影响。结果皮下注射 (sc)利血平后动物呈现利血平化 :出现眼睑下垂、体温下降及活动抑制。小鼠、大鼠BCEF2 5、5 0、10 0mg·kg-1预防性一次灌胃对利血平 (sc ,2、2 .5mg·kg-1,qd× 1d)、大鼠BCEF2 5、5 0、10 0mg·kg-1预防性连续灌胃 14d ,对利血平 (sc ,2 .5mg·kg-1,qd× 1d)致上睑下垂及活动抑制均无明显改变 ;小鼠BCEF5 0、10 0mg·kg-1治疗性连续灌胃 14天 ,可明显改善利血平 (sc ,0 .2mg·kg-1,qd× 14d)化小鼠的眼睑下垂及活动抑制。结论BCEF对利血平拮抗实验具有一定的改善作用。提示BCEF具有部分增强单胺递质系统的作用。     

丁螺环酮加强戊四氮致小鼠惊厥作用

新型非苯二氮(艹卓)类抗焦虑剂丁螺环酮(Bus)(1～10 mg·kg~1)使戊四氮(PTZ)致惊厥作用的CD_(50)下降12～37％,具有剂量依赖性和时间效应关系.色氨酸羟化酶抑制剂对氯苯丙氨酸(250 mg·kg~1)和单胺耗竭剂利血平(2mg·kg~1)均可增强PTZ致惊厥作用,但同时减弱Bus的增强作用.而α_2受体激动剂可乐定和赛拉嗪以及DA受体激动剂阿朴吗啡,拮抗剂氟哌啶醇均不影响Bus的增强作用.结果表明,Bus的增强作用有5-HT能神经元的参与.     

Effects of extended periods of reserpine and α-methyl-p-tyrosine treatment on the development of the putamen in fetal rabbits

Developing nigrostriatal neuroblasts exhibit catecholamine-induced fluorescence before their axons have left the vicinity of the cell bodies. To evaluate possible developmental effects of dopamine, we have used reserpine and α-methyl-p-tyrosine to deplete dopamine chronically during the development of these axons. We found that dopamine-induced fluorescence was either absent or markedly decreased in the fetal putamens. To determine whether the absence of fluorescence was due to a reduction of dopamine terminals, the uptake of tritium-labeled dopamine was measured in the putamen. Uptake of labeled dopamine was significantly depressed in reserpine-treated fetuses to 70% of that of controls; however, no depression of labeled dopamine was found in the α-methyl-p-tyrosine-treated fetuses. After both drug treatments, the striatal perikarya were less mature than those of controls. Although we cannot rule out possible non-specific or toxic effects of the drugs, these observations support the conclusion that presynaptic dopamine may be important for development of target neurons in the neostriatum.     

The effect of immunosympathectomy on the responses of the mouse to reserpine and various

The technique of immunosympathectomy was used to investigate the relative importance of sympathetically mediated processes in the body temperature responses of mice to reserpine treatment and the thermogenic effects of subsequently administered anti-depressant and CNS stimulant drugs.It was found that immunosympathectomized mice were less sensitive to the temperature lowering effects of reserpine but exhibited, unexpectedly, an enhanced thermogenic response to each of the representative antidepressant and stimulant drugs tested.These findings appear to exclude the sympathetic division of the autonomic nervous system as an essential prerequisite for the thermogenic effects of anti-depressant and stimulant drugs in reserpine treated mice. It is suggested that the observed effects could be accounted for in terms of a possible hyperfunctional adrenal gland.The findings reported above were presented, in part, at the 7th International Congress of C.I.N.P., Prague, Czechoslovakia, August 1970.