3,4—二氯苯丙烯酰另丁胺抗抑郁作用的药理研究

研究一种新的胡椒碱衍化物:3,4—二氯苯丙烯酰另丁胺(7903)对五种抑郁动物模型的影响。7903在小于TD_(50)剂量下,对所用动物模型均显示出抗抑郁效应,即在不增加动物的自主活动情况下,急性ip 7903可明显缩短小鼠及大鼠强迫游泳不动状态时间;急性ip或po明显缩短小鼠悬尾不动时间;慢性(二周)ip可明显缩短电刺激小鼠角膜引起的最长持续不动状态时间;急性ip可明显改善利血平引起的小鼠体温下降。     

非甾体抗炎药酮咯酸的脊髓镇痛作用

采用小鼠温浴法研究非甾体抗炎药（ＮＳＡＩＤ）酮咯酸氨了三醇的脊髓镇痛作用及其机制，发现脊髓内注射酮咯酸氨了三醇０．４ｍｇ·ｋｇ－１有明显镇痛作用，但全身给药（ｉｐ）需８ｍｇ·ｋｇ－１才能达到同样镇痛效果，脊髓与腹腔注射有效剂量比为１：２０，证实酮咯酸具有脊髓镇痛作用，该作用可被ｓｃ利血平、呱唑嗪或育亨宾取消，表明酮咯酸脊髓镇痛作用机制与内源镇痛系统中的去甲肾上腺素能神经有密切关系。本文研究结果为了解ＮＳＡＩＤｓ的中枢镇痛作用及其机制提供了新资料。     

利血平诱导大鼠肾上腺髓质增生模型的动态观察

目的探讨利血平诱导建立的大鼠肾上腺髓质增生(AMH)模型的最佳期限和肾上腺髓质百分数计算的最佳方法。方法雄性SD大鼠60只,随机分为A、B、C、a、b、c 6组各10只,A、B、C实验组皮下注射利血平0.4 mg/(kg.d)和0.9%生理盐水0.4 mg/(kg.d),a、b、c对照组皮下注射0.9%生理盐水0.8 mg/(kg.d),1次/d,A和a组、B和b组、C和c组分别持续40 d、60 d和80 d后停药,测大鼠血浆儿茶酚胺(CA)水平,称肾上腺重量,光镜下观察并计算肾上腺髓质的长径、短径及总径百分数。结果各阶段实验组CA水平均有显著性升高(P<0.05);实验组与对照组之间肾上腺重量相比无显著性差异(P>0.05);40 d时A和a组的髓质长径、短径及总径百分数及60 d时B和b组的髓质短径百分数相比无显著性差异(P>0.05),60 d时B和b组的髓质长径和总径百分数及80 d时C和c组的各径髓质百分数相比均有显著性差异(P<0.05)。结论利血平0.4 mg/(kg.d)皮下注射建立的大鼠AMH模型研究的最佳期限是60 d,肾上腺髓质百分数计算的最佳方法以髓质的总径计算为佳。肾上腺重量不能反应出肾上腺髓质是否增生。     

理中丸和四君子汤对利血平脾虚大鼠自主活动的影响

目的观察理中丸和四君子汤对利血平脾虚大鼠自主活动度的影响。方法采用中国中医科学院基础所生理室发明的小动物自主活动检测装置对大鼠的自主活动进行观察,并用生理实验信号采集分析系统进行信号的采集和分析。结果正常组、理中丸组和四君子汤组大鼠的自主活动度高于模型组,差异显著。结论四君子汤和理中丸对脾虚大鼠自主活动有显著影响,但两组间无显著性差异。     

Neuropharmacological effects of isomers of hexachlorocyclohexane—3. An account of the convulsant activity of the γ-isomer in rats

A study was made of the somatomotor responses of rats to y-hexachlorocyclohexane, the insecticide lindane, with a view to assessing its properties as a convulsant in mammals. The drug was known to successively elicit a (myo-)clonic and a (myo-)clonic-tonic seizure on slow intravenous infusion as does pentylenetetrazol. The correspondence with pentylenetetrazol is now shown to include, apart from premonitory signs and a certain form of postictal state (1) the ontogenetic development of the two different types of seizure; (2) the antagonistic action of trimethadione and of the α-isomer of hexachlorocyclohexane; (3) a facilitatory action of reserpine. Further, an identical series of locomotor behaviours has been found to be elicited by γ-hexachlorocyclohexane and pentylenetetrazol upon injection into basal strata of allo- and neocortex overlying the tectum or into the superior colliculus none of which, however, constitutes a significant early part of the sequence of effects seen after systemic administration. The implications of this discrepancy are considered with reference to evidence which would seem to indicate that the response obtained by topical application into the tectum might be initiated through interference with GABAergic neurotransmission. Consideration is also given to the pharmacokinetic properties of the insecticide which bear on onset of action and apparent potency in relation to pentylenetetrazol. It is concluded that γ-hexachlorocyclohexane exerts its somatomotor effects in a manner akin to pentylenetetrazol with respect to target sites and modes of excitation.     

Inhibitory effects of reserpine and carbonyl cyanide m-chloro-phenylhydrazone on fluoroquinolone resistance of Acinetobacter baumannii

echanisms of bacterial resistance to fluorogquinolones may be grouped into three principal categories; gene mutations of DNA topoisomerase Ⅱ (GyrA or GyrB), DNA topoisomerase Ⅳ (ParC or ParE), decrease of outer membrane permeation and upregulation of multi-drug efflux pump (active efflux system). Efflux pumps are transport proteins removing toxic substrates (including virtually all classes of clinically relevant antibiotics) from cells to the external environment.     

Evidence for the outward transport of norepinephrine in synaptic vesicles attached to the plasma membrane

In a low-sodium, choline⁺ (Ch⁺) medium, rat heart slices, that were labelled in vivo with [³H]norepinephrine, exhibited a delayed, Ca²⁺-dependent release of radioactivity, these radioactive compounds consisted of both amines and deaminated metabolites. The Ca²⁺-dependent release of radioactivity was largely blocked by cocaine suggesting that the release may represent an outward transport of [³H]amines. Reserpine, which is known to inhibit binding of norepinephrine to synaptic vesicles, stimulated the release of deaminated metabolites and some amines from the slices. Cocaine increased the release of [³H]amines in monoamine oxidase inhibited, reserpinized slices in the control medium. When Ch⁺ -Ca²⁺ and reserpine stimulation were combined, the effects of Ch ⁺ -Ca²⁺ predominated. These effects were blocked by cocaine, which then permitted the response to reserpine to become established. The conclusion derived from the above experiments is that norepinephrine coming from synaptic vesicles brought in close proximity to the plasma membrane by a Ca²⁺-dependent system can be transported outwardly to the extraneuronal space by a cocaine-sensitive mechanism.     

利血平抑郁模型的剂量探讨

目的:建立利血平抑郁模型的合适剂量,观察不同剂量利血平对大鼠自发活动的影响。方法:大鼠随机分为实验组(腹腔注射利血平2、4、6 mg/kg)和对照组(腹腔注射相同体积的溶剂),于注射后1 h通过开场实验评价大鼠自发活动的改变。结果:腹腔注射利血平(2、4、6 mg/kg)可引起大鼠抑郁样行为;4 mg/kg组抑郁样行为与2 mg/kg组比有统计学意义(P<0.05),而与6 mg/kg组比无统计学意义;行为改变(48~72 h)可随利血平剂量的增加而减少,继续增加剂量则呈现出一种平台样变化。结论:利血平能引起大鼠抑郁样行为,4 mg/kg为制造抑郁模型较为合适的剂量。     

Ventricular dysrhythmias following an alfentanil anesthetic in a patient on reserpine for hypertension

The case is presented of a hypertensive patient on reserpine, who developed ventricular irritability after administration of alfentanil, a new ultra-short-acting narcotic used in anesthesia. The dysrhythmias resolved after cessation of the offending agent. There are no reported cases of interaction of reserpine and alfentanil in the literature.     

REPERFUSION ARRHYTHMIAS IN CLOSED-CHEST RATS: THE EFFECT OF MYOCARDIAL NORADRENALINE DEPLETION AND Ca2+-ANTAGONISM

1. The influence of myocardial noradrenaline depletion on the incidence and severity of reperfusion arrhythmias in closed-chest anaesthetized rats was investigated. Five-minute left coronary artery occlusion was carried out via an implanted occluder. Four groups of rats were studied: controls, rats treated with reserpine (5 mg/kg, intraperitoneally) 24 h before occlusion, and rats receiving 0.2 mg/kg gallopamil intravenously 5 min before occlusion either with or without reserpine pretreatment. 2. In the control group all animals had ventricular tachycardia (VT) and fibrillation (VF) immediately after reperfusion. Gallopamil reduced VT to 50% and VF to 25% (P less than 0.05 versus control). In the reserpine group all had VT, and 67% had VF, this being not significantly different from controls. Additional treatment with gallopamil markedly reduced VT and totally prevented VF (P less than 0.05 versus control). 3. Thus, total depletion of myocardial noradrenaline stores neither prevented the occurrence nor reduced the severity of reperfusion arrhythmia in rats, while gallopamil treatment was effective.