DL-四氢巴马汀对大鼠单胺的排空作用

DL-四氢巴马汀(THP)是中药延胡索的有效成分,具有镇静、安定、镇痛和温和降压等作用。本文用高压色谱并用电化学检测器法研究了THP对大鼠单胺代谢的影响。THP60mg/kg能降低三种单胺介质的含量:DA(-70%),NA(-50%),5-HT(-30%)。它们的酸性或中性代谢物HVA,DOPAC,MHPG-SO₄和5-HIAA含量显著升高(+200～300%)。而DA的甲基化代谢物3-甲氧基酪胺(3-MT)含量明显减少。DA酸性代谢物的升高和DA被COMT甲基化的代谢物3-MT的降低,皆表示DA被排空和导致DA能系统功能的低落。可以得出结论,THP是一个短效单胺排空剂。     

优降宁对四氢巴马汀排空大鼠脑内儿茶酚胺作用的影响

dl-四氢巴马汀(dl-Tetrahydropalmatine,THP)是中药延胡索(Corydalis ambigua)的有效成分之一,有镇静、安定和镇痛作用。本文作者曾报道,THP有利血平样作用,能排空动物脑内多巴胺(DA)、去甲肾上腺素(NA)和5-羟色胺及心脏内的NA,提出THP为一短效单胺排空剂。众所周知,利血平类化合物的作用可为单胺氧化酶抑制剂(MAOI)所翻转。如在利血平以前给予MAOI,则前者的镇静作用翻转为兴奋,对单胺的排空作用亦被     

优降宁对四氢巴马汀排空大鼠脑内儿茶酚胺作用的影响

DL-Tetrahydropalmatine (THP) is an active principle found in the Chinese herb Corydalis ambigua. It possesses sedative and analgesic activities. THP had been reported to deplete dopamine (DA), noradrenaline (NA) and serotonin in rat brain. The effect of reserpine in reducing the transmitters and its sedative action could be reversed by MAOI i. e. reserpine-reversal. In order to investigate the influence of pargyline on THP induced depletion of catecholamines, NA, DA and their metabolites were measured by high performance liquid chromatography coupled with electrochemical detection. It was shown that the decrease of NA and DA concentrations in the limbic area was reversed by pretreatment with pargyline, whereas that in the striatal area returned to normal. From this study further evidence was obtained to support the hypothesis that THP is a monoamine depletor with reserpine-like action.     

四氢巴马汀对大鼠伏核单位放电的影响

用清醒制动大鼠记录了前脑伏核神经元的自发放电。伏核单位放电率为4.9次/s。四氢巴马汀(THP)明显抑制伏核单位放电。抑制效应在给药后10 min开始,30 min时最明显。单胺氧化酶抑制剂优降宁对伏核放电无明显影响,但能消除THP对伏核放电的抑制作用。本研究结果和THP排空单胺介质的生化资料结果一致,可以认为THP为利血平样作用的单胺排空剂。     

DL-四氢巴马汀对犬心脏血流动力学作用

消旋体四氢巴马汀(dl-tetrahydropalmatine,THP),是从罂栗科紫堇属植物延胡索中提取的一种生物碱,有镇痛、镇静、催眠、舒张平滑肌、降压等作用。近来发现,THP还有广泛的抗心律失常作用,其作用机理相当于Ⅳ类抗心律失常药,为一类似戊脉安的钙通道阻滞剂。本文观察了THP对麻醉开胸犬的血流动力学作用,为探索THP的作用机理及今后临床用药提供一定的参考。     

左旋四氢巴马汀与左旋千金藤啶碱的单胺受体结合特性与单胺排空作用的关系

本文报道了四氢异喹啉生物碱(TIQ):左旋千金藤啶碱(1—SPD),左旋及消旋四氢巴马汀(THP)及小檗胺(BBM)对大鼠脑内DA_2,5-HT_2及β—肾上腺素受体的结合特性。 所测的四种TIQ对β-肾上腺素受体的亲和力均很低(IC_(50)大于10~(-4)M)。结果表明,THP对单胺能神经递质受体亲和力远小于经典的单胺受体阻断剂,从而提示单胺受体阻断可能并非THP影响单胺能神经传递的主要机制。作者认为THP一类的TIQ,生物碱至少可以通过两种机制发挥作用:单胺受体阻断及利血平样“颗粒效应”。而对于THP,起主要作用的是引起单胺排空的“颗粒效应”。此外,实验中发现1-SPD与DA_2受体结合并不是简单的双分子反应,表现为1-SPD/[~3H]螺环哌啶酮抑制曲线的Hill系数远小于1。这一受体结合特点可能与其在动物行为实验中表现出的部分激动剂性质有关。     

阿米替林增强左旋四氢巴马汀的镇痛作用

目的 探讨阿米替林增强左旋四氢巴马汀(L-THP)的镇痛作用。方法 采用热板法和化学刺激法进行镇痛实验。结果 阿米替林两组剂量(4．2mg／kg，8．3mg／kg)均加强了L-THP的镇痛作用，镇痛作用时间持续4h。结论 阿米替林可增强L-THP的镇痛作用。     

L-四氢巴马汀对羟考酮依赖大鼠不同脑区单胺递质水平的影响

目的：观察L-四氢巴马汀（L-THP）对羟考酮依赖大鼠不同脑区单胺递质含量的影响，探讨L—THP对抗羟考酮依赖的机制。方法：以连续递增给药建立羟考酮依赖大鼠模型，L—THP伴随给药，采用HPLC—ECD法测定大鼠前皮层、海马、纹状体和伏隔核内多巴胺（DA）和5-羟色胺（5-HT）含量的变化。结果：与空白对照组相比，羟考酮依赖的大鼠纳络酮催促戒断后前皮层内DA、高香草酸（HVA）和5-HT含量明显降低，伏隔核内DA、3，4-二羟基苯醋酸（DOPAC）、HVA和5-HT含量明显降低，海马内DA、DOPAC、5-HT含量没有明显变化，而5-吲哚乙酸（5-HIAA）明显升高，纹状体内DA及其代谢产物DOPAC、HVA以及5-HT、5-HIAA含量明显降低；L—THP（10，20，30mg·kg^-1，ig）伴随给药，能不同程度抑制上述变化。结论：L—THP可抑制羟考酮依赖引起的不同脑区内单胺类递质含量的变化，提示LTHP对抗羟考酮依赖可能与调节多巴胺和5-HT系统相关。     

左旋四氢巴马汀及其同类物的心血管药理作用

<正> 左旋四氢巴马汀(L-tetrahydropalmatjne.L—THP)又称颅痛定.为中药延胡索的主要有效成分—延胡索乙素(dl—THP)的左旋物,已作为镇痛药广泛用于临床。1—THP与左旋千金藤立定(1—stepholi—dine.l—SPD)、四氢小檗碱(tetrahydroberberine,THB)同属四氢原小檗碱类(THPB).有相同的化学结构母核(附图)早年发现THPB类化合物具有多种相似的中枢药理作用.如镇痛、镇静、安定、催眠等。近来研究证明它们还有多种相近的心血管效应。本文拟从以下几方面对其作用及其临床研究作一综述。     

吡喹酮对大鼠单胺介质的影响

吡喹酮是一种新型广谱抗寄生虫药。本文报道用高效液相色谱-电化学检测器联用的方法,测定单胺类神经介质及其代谢物的含量,研究吡喹酮对大鼠单胺类介质的影响。结果表明:吡喹酮(250 mg/kg使脑DA的酸性代谢产物DOPAC,HVA和5-HT的代谢物5-HIAA的含量明显升高,而对DA和NA含量无明显影响。DA酸性代谢物和5-HIAA升高表明吡喹酮能增加DA和5-HT的转换率     

吡喹酮对大鼠单胺介质的影响

吡喹酮是一种新型广谱抗寄生虫药。本文报道用高效液相色谱-电化学检测器联用的方法,测定单胺类神经介质及其代谢物的含量,研究吡喹酮对大鼠单胺类介质的影响。结果表明:吡喹酮(250 mg/kg使脑DA的酸性代谢产物DOPAC,HVA和5-HT的代谢物5-HIAA的含量明显升高,而对DA和NA含量无明显影响。DA酸性代谢物和5-HIAA升高表明吡喹酮能增加DA和5-HT的转换率。     

加钖果宁的镇痛作用及其作用机制

野花椒系芸香科植物(Zanthoxylum simulans Hance),其根皮有止痛及局麻作用。其水溶性生物碱有肌松作用,曾用于外科手术作为中麻辅助用药。常志青从中分离到加钖果宁[(—)edulinine,简称加钖碱,下同],并发现有镇痛及中枢抑制作用。本文进一步证明其镇痛作用及其作用机制与阿片受体有关。     

利血平与优降宁对动物痛阈和吗啡镇痛作用影响因素探讨

采用三种测痛方法,观察了利血平、优降宁对小鼠、大鼠正常痛阈和吗啡镇痛作用的影响,结果表明:ip利血平2 mg/kg,优降宁100 mg/kg均能明显抑制小鼠扭体反应;ip利血平1 mg/kg能明显提高小鼠热板反应时间,但ip优降宁75 mg/kg无明显影响;ip利血平6 mg/kg,优降宁75 mg/kg对大鼠甩尾反应时间均无明显影响;利血平(小鼠0.5～1.0 mg/kg,大鼠2 mg/kg ip)能明显对抗吗啡镇痛作用;优降宁(小鼠35 mg/kg,大鼠50 mg/kg ip)能明显增强吗啡镇痛作用,并能“逆转”利血平对抗吗啡镇痛作用。其“逆转”作用的强弱取决于利血平、优降宁给药的先后次序。     

利血平与优降宁对动物痛阈和吗啡镇痛作用影响因素探讨

采用三种测痛方法,观察了利血平、优降宁对小鼠、大鼠正常痛阈和吗啡镇痛作用的影响,结果表明:ip利血平2 mg/kg,优降宁100 mg/kg均能明显抑制小鼠扭体反应;ip利血平1 mg/kg能明显提高小鼠热板反应时间,但ip优降宁75 mg/kg无明显影响;ip利血平6 mg/kg,优降宁75 mg/kg对大鼠甩尾反应时间均无明显影响;利血平(小鼠0.5～1.0 mg/kg,大鼠2 mg/kg ip)能明显对抗吗啡镇痛作用;优降宁(小鼠35 mg/kg,大鼠50 mg/kg ip)能明显增强吗啡镇痛作用,并能“逆转”利血平对抗吗啡镇痛作用。其“逆转”作用的强弱取决于利血平、优降宁给药的先后次序。     

肼类和非肼类化合物抑制单胺氧化酶作用的研究

本文除报导了筛选单胺氧化酶抑制剂(MAOI)的常规。并讨论了非肼类和肼类化合物(包括吲哚类、氨基酸类、胍类、石蒜生物碱、及酰肼类)等49种药物的初筛结果。经体外、体内筛选和毒性试验,发现4-硫杂庚二酰(2-异丙基)肼,简称硫双肼(CH-6),具有较强的抑制单胺氧化酶的作用,作用强度与苯乙肼相似。毒性较低,仅为苯乙肼的1/50。     

EFFECTS OF RESERPINE ON THE CONTENT AND UPTAKE OF DOPAMINE AND NORADRENALINE IN RABBIT ARTERIES

1. Change with time of the content and uptake of dopamine (DA) and noradrenaline (NA) in the renal, superior mesenteric and femoral arteries and abdominal aorta of rabbit after reserpine administration was examined. Endogenous DA and NA were measured by high performance liquid chromatography coupled with electrochemical detector. 2. A single dose of reserpine (3 mg/kg, i.p.) maximally depleted the endogenous DA and NA contents in the four blood vessels 24 h after the administration; the ratios of reductions were 70–90% and approximately 90% of the normal levels, respectively. The DA contents in all four vessels recovered to the normal level within 4 days after reserpine. However, NA content did not recover to the normal levels within 30 days after reserpine except in the mesenteric artery. 3. The activity of dopamine β-hydroxylase (DBH) significantly increased in all four blood vessels 1 h after reserpine. Although the DBH activity returned to the normal level after 3 days in the mesenteric artery, it returned within 24 h in the other three vessels. 4. [³H]-Dopamine and [³H]-NA uptake were almost completely depressed 1 h after reserpine. The [³H]-NA uptake in four vessels recovered to the normal level 2–14 days after reserpine, and [³H]-DA uptake recovered after 30–45 days. Thus, the endogenous DA content in blood vessels was completely restored although DA uptake and NA content were still affected. 5. These results suggested that the recovery of stored DA after reserpine was faster than that of stored NA and the recovery of DA uptake after reserpine was slower than NA uptake. This indicates a possibility that a part of DA pool may be different from NA pool in adrenergic nerve terminals in the blood vessels.     

LETHAL EFFECTS OF RESERPINE PLUS PHYSOSTIGMINE AND NEOSTIGMINE IN MICE

1. The interaction between the reversible cholinesterase inhibitors, physostigmine and neostigmine and reserpine was studied. 2. A combination of reserpine plus a cholinesterase inhibitor significantly increased lethality in adult male Swiss-Webster mice above that caused by either neostigmine, physostigmine, or reserpine alone. 3. Methscopolamine completely reversed this effect. 4. It would appear that the presence of the antiadrenergic agent, reserpine, increases the toxicity of cholinomimetic agents. 5. The above results may have clinical significance, since reserpine and cholinesterase inhibitors are used in the practice of medicine.     

中国人参与西洋参皂甙抗热应激作用的比较

中国红参根皂甙、中国人参茎叶皂甙和西洋参根皂甙在热应激的警觉期能抑制小鼠直肠温度的升高。用回归直线方程法比较了三种皂甙的抗热应激作用的半数致死时间(LT_(50)),中国红参根皂甙及茎叶皂甙的 LT_(50)均显著长于对照组,故能延长动物在热环境中的存活时间,而西洋参则无此作用。