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1.
(—)SPD和(—)THP对蓝斑核去甲肾上腺素能神经元自发放电的影响 总被引:1,自引:0,他引:1
利用在体记录大鼠蓝斑核神经元单位放电,研究了(-)SPD和(-)THP对其放电活动的影响。结果表明:(-)SPD通过去甲肾上腺素a2受体,以剂量依赖方式增强蓝斑核神经元放电,但较大剂量却对神经元放电有一定抑制。然而(-)THP可使蓝斑核去甲肾上腺素能神经元出现可逆性放电抑制。 相似文献
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利用大肠杆菌表达系统进行葡萄糖-6-磷酸脱氢酶(G-6-PD)的生化鉴定卢义钦(湖南医科大学生化教研室,长沙410078)关键词葡萄糖-6-磷酸脱氢酶(G-6-PD),大肠杆菌,表达葡萄糖-6-磷酸脱氢酶(G6PD)缺乏症在各民族人群中均有发现,据估... 相似文献
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在74张大鼠下丘脑脑片上,用玻璃微电极记录到弓状核自发放电单位176个,其放电形式有三种:慢不规则型(119个,67.6%);快连续型(46个,26.1%);位相型(11个,6.3%)。5-HT(10-6mol/L,3min)对不同形式放电单位的作用均以抑制为主:对部分慢不规则单位(9/119)则表现为先抑制后兴奋的双相性反应,对少数神经元有兴奋作用。12个被5-HT抑制的单位,其抑制作用不能被噻庚啶(CHD,10-5mol/L)阻断,4个被5-HT抑制的的单位中,其抑制作用可被二甲基麦角新碱(MSG10-6mol/L)部分或完全阻断。7个被5-HT抑制的单位,其中4个单位中,5-HT的抑制作用可被特异性5-HT1A受体阻断剂Pindobind-5-HT1A部分阻断;但另外3个单位的阻断效果不明显。上述结果表明:5-HT对弓状核不同形式放电单位的作用均以抑制为主,其作用可能是通过5-羟色胺(5-HT1)受体介导的,部分还可能是通过5-HT1A受体介导的。 相似文献
4.
本工作观察到10-6—10-5mol/L去甲肾上腺素(NE)和10-7—10-5mol/L异丙基肾上腺素(ISO)可明显促进离体培养的血管平滑肌细胞(VSMC)的增殖和DNA的合成,并呈剂量依赖效应,该效应可为相应的受体阻断剂phentolamine(10-6mol/L)和proptanolol(10-5mol/L)所抑制;nifedipine(10-6mol/L)和veraromil(10-6mol/L)分别与同样浓度的NE同时加入细胞培养液中,其细胞计数和3H-TdR掺入率分别较单用NE时显著降低(P<0.01),nifedipine与verapamil亦明显抑制ISO促VSMC增殖的作用。 相似文献
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L-NNA及NO供体对延髓腹外侧头端区神经元自发放电的影响 总被引:3,自引:1,他引:2
在麻醉大鼠观察了静注NO合成酶抑制剂N-硝基左旋精氨酸(L-NNA)和NO供体──硝普钠(SNP)和SIN-I对血压、心率和延髓腹外侧头端区(RVLM)神经元自发放电活动的影响,旨在探讨L-arg:NO通路对动脉血压调节的中枢作用部位。所得结果如下:(1)静注L-NNA后,平均动脉压(MAP)升高,心率(HR)加快,11个RVLM神经元自发放电频率增加。这些变化发生于给药后5min,持续时间达30min以上。(2)静注SNP后,MAP降低,HR加快,23个RVLM神经元自发放电频率降低,且有剂量依赖性。SNP作用发生快,持续时间短。为了排除脑缺血的影响,还特意向一侧颈动脉内注射相同剂量SNP,结果引起MAP轻度降低,而HR无明显改变,但RVLM神经元自发放电频率仍显著降低。(3)静注另一NO供体SIN-I后,MAP降低,11个RVLM神经元自发放电频率降低.与SNP的效应基本一致。以上结果提示,RVLM是L-arg:NO通路实现动脉血压调节的一个中枢作用部位。 相似文献
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AVP_(4-8)结合点在大鼠海马内的分布和AVP_(4-8)对其受体发育的影响:放射自显影研究 总被引:2,自引:0,他引:2
本文利用放射自显影方法结合神经毒对海马神经元的选择性损毁观察AVP(4-8)结合点在大鼠海马内的分布和定位;利用外源性AVP(4-8)对新生大鼠的处理,观察海马AVP(4-8)结合点的发育调节。在成年大鼠海马内,AVP(4-8)结合点集中分布在整个海马的锥体细胞层和齿回的颗粒细胞层。秋水仙碱处理后,齿回颗粒细胞层消失,齿回区的AVP(4-8)结合点也消失。红藻氨酸(Kainicacid)处理后海马CA3-CA4的锥体细胞层消失,该区的AVP(4-8)结合点也消失。新生大鼠海马锥体细胞层的AVP(4-8)结合点在出生后第6天开始出现,齿回颗粒细胞层的AVP(4-8)结合点在出生后第7天开始出现。然而,新生大鼠每天经外源性AVP(4-8)处理,海马锥体细胞层和齿回颗粒细胞层的结合点均在出生后第5天已变得十分稠密。本文就大鼠海马AVP(4-8)结合点的特异性分布和AVP(4-8)处理促进海马AVP(4-8)结合点的发育与成年后大鼠学习能力的提高的相互关系作了讨论。 相似文献
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ATP-敏感钾通道和内源性腺苷参与刺激蓝斑引起的脊髓抗痛作用 总被引:3,自引:0,他引:3
根据蓝斑刺激可以通过脊髓下行性去甲肾上腺素能纤维阻断由背角上传到束旁核神经元的伤害性放电的事实,本实验用脊髓鞘内给予相应工具药的方法,进一步分析了上述下行性抑制作用在脊髓背角中阻止伤害性传入信号向上传递的可能机制,结果发现:(1)鞘内注入ATP-敏感钾通道阻断剂格列苯脲或腺苷受体拮抗剂氨茶碱,均可以阻断或取消刺激蓝斑引起的对束旁核伤害性放电的抑制作用;(2)鞘内注入ATP-钾通道激动剂nic-orandil或腺苷受体激动剂5‘-N-ethylcarboxamido-adenosine(NECA),都可抑制束旁核神经元的伤害性放电;(3)鞘内注入氨茶碱可阻断鞘内注入nicorandil引起的束旁核痛放电的抑制,再鞘内注入格列苯脲不能阻断鞘内注入NE-CA引致的束旁核痛放电的抑制。这些结果提示:(1)蓝斑刺激在脊髓背角中抑制痛信号的上传,要有ATP-敏感钾通道的激活和内源性腺苷的释放为中介;(2)ATP-敏感钾通道的激活发生在腺苷的释放之前。 相似文献
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莱氏衣原体膜上Mg~(2+)-ATPase用DOC溶解后,经Sepharose-6B和DEAE-CelluloseDE-52离子交换柱,得到了部分纯化的Mg~(2+)ATPase,并将此ATPase与不同极性头部的磷脂和膜糖脂重组,研究了不同的极性头部的磷脂和膜糖脂对ATPase活性的影响。此酶的活性不依赖酸性磷脂,PG、DPG、大豆磷脂等明显抑制酶活性,中性磷脂DMPC、PE、PC则能增加酶活性,其中尤以非双层脂PE的作用最为明显。从莱氏衣原体膜上提取的糖脂(MGDG,DGDG)单独和ATPase重组时,酶活性增加并不明显,当MGDG和DGDG以等比例混合时,能大大地增加酶活性。这表明Mg~(2+)-ATPase的活性很大程度上与磷脂的表面电荷及磷脂的组成相关。 相似文献
11.
左旋千金藤啶碱D1激动—D2阻滞作用引起伏核双相放电活动的电生理研究 总被引:3,自引:0,他引:3
为确定左旋千金藤啶碱(SPD)对中脑边缘DA神经系统的作用特性,本研究采用细胞外记录的电生理学方法,观察微电泳和尾静脉给药对6-OHDA损毁及未损毁大鼠的伏核(NAc)单位放电的影响。结果显示:SPD累积给药(0.02-2mg/kg,iv)可诱发NAc神经元双相放电特征,即小剂量抑制、大剂量兴奋。预先给予D2受体拮抗剂speperone,SPD则仅产生兴奋效应,并被D1拮抗剂SCH-23390所翻 相似文献
12.
(-)-Stepholidine (SPD), with D1 agonistic action, elicited an excitatory firing activity of nucleus accumbens (NAc) neurons by intravenous administration, but this effect was hardly observed by iontophoresis of SPD into the NAc. The present study intends to determine whether D1 receptors in the medial prefrontal cortex (mPFC) are involved in the action of SPD on the firing activity of NAc neurons in the chloral hydrate-anesthetized male rats. The results showed that the intra-mPFC microinjected SCH-23390 (D1 antagonist, 30 mM), but not the D2 antagonist spiperone (30 mM), significantly attenuated the enhanced firing activity induced by intravenous injection of SPD (2 mg/kg). Similarly, the excitatory firing of NAc neurons was also exhibited by the microinjection of either SPD or D1 agonist SKF-38393 into the mPFC. The SPD-induced excitatory effect was in a dose-dependent way from 277.8 +/- 51.3% (10 mM) to 1105.4 +/- 283.5% (30 mM) of NAc basal firing, which was completely reversed by SCH-23390 (i.v.). Furthermore, the direct D1 agonistic action of SPD on the mPFC neuron was observed with microiontophoresis. These results indicate that SPD possesses a direct agonistic action on the mPFC D1 receptors, by which it modulates the firing activity of NAc neurons. 相似文献
13.
The effects of a newly synthesized quinolinone derivative, 7-[3-(4-(2,3-dimethylphenyl)piperazinyl) propoxy]-2(1H)-quinolinone (OPC-4392) on neuronal activities of the caudate nucleus (CN) were investigated in cats anesthetized with alpha-chloralose using a microiontophoretic method. In the CN neurons of which spikes elicited by stimulation of the pars compacta of substantia nigra (SN) were suppressed by iontophoretically applied domperidone, a dopamine D-2 receptor antagonist, application of OPC-4392 (100-200 nA) inhibited the spike generation induced by SN stimulation. Conversely, the CN neurons insensitive to domperidone were unaffected by OPC-4392. Iontophoretic application of CPC-4392 up to 200 nA did not affect glutamate-induced firing of the CN neurons, of which the firing was blocked by dopamine less than 100 nA. In addition, OPC-4392 did not inhibit firing induced by bromocriptine, a dopamine D-2 agonist; while domperidone suppressed the bromocriptine-induced firing without affecting the glutamate-induced firing. These results suggest that OPC-4392 acts on the dopaminergic nerve terminals and inhibits excitatory transmission from the SN to the CN. 相似文献
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Tetrahydropalmatine (THP) is a biologically active ingredient isolated from a traditional Chinese herb Rhizoma corydalis (yanhusuo). THP is a racemic mixture which contains 50% of the (+) and 50% of (-) enantiomer. The (-) enantiomer accounts for most of the analgesic effects. Plasma concentrations of THP enantiomers were analyzed by chiral high-performance liquid chromatography (HPLC) on a Chiralcel OJ column with quantification by UV at 230 nm. The method was used to determine the pharmacokinetics of THP enantiomers in rats and dogs after oral administration of rac-THP or (-)-THP. The pharmacokinetic profiles of the two enantiomers after dosing with rac-THP were significantly different both in rats and dogs. The mean C(max) and AUC(0-infinity) values in rats were 1.93 +/- 0.36 microg/ml and 6.65 +/- 2.34 microg x h/ml for the (-) enantiomer, and 1.11 +/- 0.25 microg/ml and 2.03 +/- 0.45 microg x h/ml for the (+) enantiomer. The mean C(max) and AUC(0-infinity) in dogs were 1.60 +/- 0.81 microg/ml and 9.88 +/- 2.58 microg x h/ml for the (-) enantiomer, while 0.36 +/- 0.21 microg/ml and 1.22 +/- 0.40 microg x h/ml for the (+) enantiomer. rac-THP at 40 mg/kg and (-)-THP at 20 mg/kg had very similar plasma concentration-time profiles, and C(max), AUC(0-infinity), and t(1/2) of the (-) enantiomer in both rats and dogs, indicating that the two treatments were equivalent with respect to the pharmacokinetic properties of the (-) enantiomer. 相似文献
15.
Atypical neuroleptic properties of l-stepholidine -Electrophysiological and behavioral studies 总被引:1,自引:0,他引:1
Intravenous administration of l-stepholidine (SPD), a dopamine (DA) receptor antagonist, in-creased the firing rate of DA neurons located in the ventral tegmental area (VTA) and substantia nigra pars compacta (SNC) in both anaesthetized and paralyzed rats. However, with the increase of dose, SPD selectively inhibited the fir-ing activity of DA neurons in the VTA but not in the SNC. The inhibition was reversed by the DA agonist apomor-phine (APO), suggesting that it may be via the mechanism of depolarization inactivation (DI). In rats, chronic admin-istration of SPD for 21 d dose-dependently decreased the number of spontaneously active DA neurons in the VTA, of which effect was reversed by APO (i. v. ). In contrast, the same treatment failed to affect the population of DA neu-rons in the SNC. Similarly, the acute treatment of SPD also decreased the number of spontaneously firing DA neurons in the VTA, but not in the SNC. SPD per se only induced very weak catalepsy. Its catalepsy which was not in pro-port 相似文献
16.
Intravenous administration ofl-stepholidine (SPD), a dopamine (DA) receptor antagonist, increased the firing rate of DA neurons located in the ventral tegmental area (VTA) and substantia nigra pars compacta (SNC) in both anaesthetized and paralyzed rats. However, with the increase of dose, SPD selectively inhibited the firing activity of DA neurons in the VTA but not in the SNC. The inhibition was reversed by the DA agonist apomorphine (APO), suggesting that it may be via the mechanism of depolarization inactivation (DI). In rats, chronic adrninistration of SPD for 21 d dose-dependently decreased the number of spontaneously active DA neurons in the VTA, of which effect was reversed by APO (i. v.). In contrast, the same treatment failed to affect the population of DA neurons in the SNC. Similarly, the acute treatment of SPD also decreased the number of spontaneously firing DA neurons in the VTA, but not in the SNC. SPD per se only induced very weak catalepsy. Its catalepsy which was not in proportion to dosage was only observed in the dose range of 10–40 mg/kg and lasted 15 min. SPD effectively antagonized the APO (2 mg/kg, i. p.)-induced stereotypy.The above-mentioned results suggest that SPD selectively inactivates the DA neurons in the VTA not in the SNC. SPD may associate with a low incidence of extrapyramidal side-effects and may be ranked as a promising compound for searching for a new kind of atypical neuroleptics. 相似文献
17.
Takahiro Ishikawa Kasumi Maeda Koichi Hayakawa Takakazu Kojima 《Journal of Molecular Catalysis .B, Enzymatic》1996,1(3-6):173-179
Microbial production of a 6-hydroxy-3-pyridylmethyl compound from 3-pyridylmethyl compound was investigated. The hydroxylation of 3-(methylaminomethyl)pyridine to 5-(methylaminomethyl)-2(1H)-pyridinone, tautomer of 2-hydroxy-5(methylaminomethyl)pyridine, by resting cells ofArthrobacter ureafaciens JCM3873 was found to proceed regio- and chemo-selectively with an almost quantitative yield. The addition of molybdate ion and nicotine as an inducer to the culture medium was required for the preparation of cells containing high hydroxylation activity. The optimal temperature and pH for the hydroxylation by using resting cells were 35°C and around 7, respectively. This hydroxylation enzyme does undergo inhibition by the substrate. The inhibitory effect could be eliminated by stepwise feeding of the substrate. Under adequate conditions, 23 mg/ml of 5-(methylaminomethyl)-2(1H)-pyridinone was produced with a molar yield of nearly 100% from 3-(methylaminomethyl)pyridine. 相似文献
18.
The subcutaneous administration of 1 mg/kg tetrabenazine, once daily for 5 days, which depletes the catecholamine stores in the brain, significantly inhibits in rats the acquisition of a two-way conditioned avoidance reflex in the shuttle box. Enhancer substances, the tryptamine-derived selective and highly potent enhancer, R-(-)-1-(benzofuran-2-yl)-2-propylaminopentane HCl [(-)-BPAP] (0.05-10 mg/kg), the beta-phenylethylamine (PEA)-derived enhancer, (-)-deprenyl (1-5 mg/kg) and the (-)-deprenyl analogue, free of MAO-B inhibitory potency, (-)-1-phenyl-2-propylaminopentane HCl [(-)-PPAP], (1-5 mg/kg), antagonize in a dose-dependent manner the inhibition of learning caused by tetrabenazine. 1-(Benzofuran 2 yl)-2-(3,3,3-trifluoropropyl)aminopentane HCl [3 F BPAP], a newly synthetized analogue of (-)-BPAP with low specific activity, significantly antagonized the enhancer effect of (-)-BPAP but left the effect of (-)-deprenyl and (-)-PPAP unchanged. This is the first proof for a difference in the mechanism of action between a PEA-derived enhancer substance and its tryptamine-derived peer. 相似文献
19.
Crespy V Nancoz N Oliveira M Hau J Courtet-Compondu MC Williamson G 《Free radical research》2004,38(9):1025-1031
The flavonoids (-)-epigallocatechin-3-gallate (EGCg) and (-)-epicatechin-3-gallate (ECg) are major components of green tea and show numerous biological effects. We investigated the glucuronidation of these compounds and of quercetin by microsomes. Quercetin was almost fully glucuronidated by liver microsomes after 3 h, whereas ECg and ECGg were conjugated to a lesser extent ([Formula: See Text] and [Formula: See Text] respectively). The intestinal microsomes also glucuronidated quercetin much more efficiently than ECg and EGCg. Although the rates were lower than quercetin, intestinal microsomes exhibited higher activity on the galloyl group of ECg and EGCg compared to the flavonoid ring, whereas hepatic glucuronidation was higher on the flavonoid ring of EGCg and ECg compared to the galloyl groups. The low glucuronidation rates could partially explain why these flavanols are present in plasma as unconjugated forms. 相似文献
20.
本工作用全细胞膜片箝方法,观察了氟啶醇(haloperidol以下简称HALO)和R(-)-Propylnorapomorphine(以下简称NPA)对C6神经胶质瘤细胞(C6gliomacells)的电压依赖性钾电流的作用,并初步分析了它们的作用机制。结果表明,HALO和NPA都能抑制C6细胞的K^+J电流中的慢成分,而对快成分的作用有所不同。它们的抑制作用不是由多巴胺D2受体介导的,也不是通过 相似文献