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[Congress of French-language Pharmacology. Rouen, 5-7 May 1986. Abstracts]. 法语药理学大会。鲁昂,1986年5月5日至7日。摘要]。
Pub Date : 1986-07-01
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引用次数: 0
[Chemotactic response of human polynuclear neutrophils after in vivo administration of spiramycin]. [体内给药螺旋霉素后人多核中性粒细胞的趋化反应]。
Pub Date : 1986-07-01
J Y Lombard, J Descotes, A Eyraud, J C Evreux

The chemotactic response of polymorphonuclear leukocytes using the agarose method, has been studied in six healthy volunteers, immediately prior and after a 5-day oral administration of spiramycin, 6 million units per day. The influence of spiramycin proved to be small as the directed and spontaneous migration were decreased by 21% and 18% respectively. Despite the fact that spiramycin can penetrate into leukocytes, these results indicate that no clinically relevant alterations of chemotaxis are likely under therapeutic conditions.

在6名健康志愿者中,使用琼脂糖法研究了多形核白细胞的趋化反应,在服用螺旋霉素5天之前和之后,每天口服600万单位。螺旋霉素的影响很小,直接迁移和自发迁移分别减少了21%和18%。尽管螺旋霉素可以渗透到白细胞中,但这些结果表明,在治疗条件下,趋化性不可能发生临床相关的改变。
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引用次数: 0
[Serotonergic neurons and behavior]. [血清素能神经元和行为]。
Pub Date : 1986-04-01
P Soubrié

The hypothesis linking decreased serotonin transmission to reduced anxiety as the mechanism in the anxiolytic activity of benzodiazepines conflicts with most clinical observations. Serotonin antagonists show no marked capacity to alleviate anxiety. On the other hand, clinical signs of reduced serotonergic transmission (low 5-HIAA levels in the cerebrospinal fluid) are frequently associated with aggressiveness, suicide attempts and increased anxiety. This brief review attempts to reconcile these human and animal findings by investigating whether anxiety reduction or increased impulsivity are likely to account for animal behavioral changes associated with decreased serotonergic transmission. The effects of manipulating central serotonin on experimental anxiety paradigms in animals (punishment, novelty) are reviewed and compared to the effects of anti-anxiety drugs. Anxiety seems neither necessary nor sufficient to induce control by serotonergic neurons on behavior. Further evidence suggests that behavioral effects of anxiolytics thought to be mediated by decreases in anxiety are not caused by the ability of these drugs to reduce serotonin transmission. Blockade of serotonin transmission, especially at the level of the substantia nigra, results in a shift of behavior towards facilitation of responding. This behavioral shift is particularly marked when there is competition between acting and restraining response tendencies and when obstacles prevent the immediate attainment of an anticipated reward. It is proposed that serotonergic neurons are not only involved in behavioral arousal but also in enabling the organism to arrange or tolerate delay before acting. Decreases in serotonin transmission seem to be associated with the increased performance of behaviors which are usually suppressed though not necessarily because of the alleviation of anxiety which might contribute to the suppression.

在苯二氮卓类药物抗焦虑活性的机制中,将减少血清素传递与减少焦虑联系起来的假设与大多数临床观察相冲突。血清素拮抗剂对缓解焦虑没有明显的作用。另一方面,血清素能传递减少的临床症状(脑脊液中5-HIAA水平低)通常与攻击性、自杀企图和焦虑增加有关。这篇简短的综述试图通过调查焦虑的减少或冲动的增加是否可能解释与血清素能传递减少相关的动物行为变化来调和这些人类和动物的发现。本文综述了操纵中枢血清素对实验性动物焦虑范式(惩罚、新奇)的影响,并与抗焦虑药物的作用进行了比较。焦虑似乎既不是必要的也不是充分的,以诱导5 -羟色胺能神经元对行为的控制。进一步的证据表明,被认为是通过减少焦虑介导的抗焦虑药的行为影响,并不是由这些药物减少血清素传递的能力引起的。阻断5 -羟色胺的传递,特别是在黑质水平上,导致行为向促进反应的转变。当行动和抑制反应倾向之间存在竞争时,以及当障碍阻碍了预期奖励的立即获得时,这种行为转变尤其明显。有人提出,血清素能神经元不仅参与行为唤醒,而且还参与使生物体在行动前安排或容忍延迟。血清素传递的减少似乎与行为表现的增加有关,这些行为通常被抑制,但不一定是因为焦虑的缓解,而焦虑可能有助于抑制。
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引用次数: 0
Binding of (3H)-piretanide to a specific receptor of renal medulla. (3H)-吡列脲与肾髓质特定受体的结合。
Pub Date : 1986-04-01
E M Giesen-Crouse, P Fandeleur, J L Imbs

We had previously demonstrated that (3H)-piretanide binds to a receptor located on medullary membranes of canine kidney. Here we show that binding is specific for a particular group of loop diuretics. Sulfonamide diuretics of the benzoic acid family, other substituted sulfonamides, and phenoxy-acetic acid derivates displace (3H)-piretanide from its receptor. Loop diuretics that do not act at the luminal tubular membrane do not displace piretanide, nor do diuretics with a different site and mode of action (thiazides; inhibitors of the Na+/H+ antiporter (amiloride), of Na+K+ ATPase (ouabain), or of carbonic anhydrase (acetazolamide). We demonstrate that no interference occurs between the piretanide receptor and membrane bound receptors of several neurotransmitters.

我们以前已经证明(3H)-吡列他胺与位于犬肾髓膜上的受体结合。在这里,我们表明结合是特定的一组环利尿剂。苯甲酸家族的磺酰胺利尿剂、其他取代的磺酰胺和苯氧乙酸衍生物从其受体取代(3H)-吡脲。不作用于管状管膜的环状利尿剂不会取代吡他尼,不同部位和作用方式的利尿剂也不会取代吡他尼(噻嗪类;Na+/H+反转运蛋白(阿米洛利)、Na+K+ atp酶(瓦巴因)或碳酸酐酶(乙酰唑胺)的抑制剂。我们证明吡列胺受体和几种神经递质的膜结合受体之间没有干扰。
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引用次数: 0
Comparative study of the effects of stimulation or blockade of beta-adrenoceptors on the head-twitches induced in mice by 5-hydroxytryptophan versus 5-methoxy-N, N-dimethyltryptamine. 刺激或阻断肾上腺素受体对5-羟色胺与5-甲氧基- n, n -二甲基色胺致小鼠头抽搐影响的比较研究。
Pub Date : 1986-04-01
P Martin, P Soubrié, P Simon

This study aimed at comparing the effects of blockade or stimulation of beta-adrenoceptors on the head-twitch response induced in mice by direct (5-MeODMT) or indirect (5-HTP) activation of serotonergic receptors shows that: beta-agonists (clenbuterol and salbutamol) increased the 5-HTP-induced head-twitches and decreased the response to 5-MeODMT. beta-agonists (propranolol and penbutolol) reduced the head-twitches elicited by 5-HTP but enhanced those induced by 5-MeODMT. Under our experimental conditions, desipramine behaved like the beta-agonists studied. Prior intracerebroventricular injection of 5,7-DHT enhanced the response to 5-MeODMT but did not prevent the antagonism of clenbuterol against 5-MeODMT-induced head-twitches. These findings suggest that beta-receptors are in a position to regulate differentially serotonin transmission.

本研究旨在比较阻断或刺激β -肾上腺素能受体对直接(5-MeODMT)或间接(5-HTP)激活5-羟色胺能受体诱导的小鼠头抽搐反应的影响,结果表明:β -激动剂(克仑特罗和沙丁胺醇)增加了5-HTP诱导的头抽搐,降低了对5-MeODMT的反应。-激动剂(心得安和喷布托尔)减少了5-羟色胺引起的头抽搐,但增强了5-羟色胺引起的头抽搐。在我们的实验条件下,地西帕明的表现与研究的β激动剂相似。先前脑室内注射5,7- dht增强了对5- meodmt的反应,但不能阻止盐酸克仑特罗对5- meodmt诱导的头抽搐的拮抗作用。这些发现表明-受体能够调节不同的血清素传递。
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引用次数: 0
Idazoxan: a novel pharmacological tool for the study of alpha 2-adrenoceptors. 依唑赞:研究α 2-肾上腺素受体的新药理学工具。
Pub Date : 1986-04-01
H Dabiré

The pharmacological properties of idazoxan, 2-[2-(1,4-benzodioxanyl)]-2-imidazoline, were first described four years ago; since then, this compound has been revealed to be one of the most selective alpha 2-adrenoceptor blocking agent presently available. At peripheral sites, idazoxan antagonized the effects of alpha 2 agonists such as azepexole, B-HT 920, M 7, UK 14,304, alpha-methylnoradrenaline, clonidine but was ineffective against alpha 1 agonists such as cirazoline and phenylephrine. At presynaptic sites idazoxan increased the tachycardia due to the stimulation of the cardioaccelerator nerve of the dog and antagonized the inhibitory effects of alpha 2 agonists in dogs and rats. As compared to the classical alpha 2-adrenoceptor blocking agents, idazoxan was more selective and as potent as yohimbine, rauwolscine, RS 21361, Wy 26703. At central sites, idazoxan has been found to antagonize the sympathoinhibitory effects of alpha 2 agonists. Therefore, idazoxan is a potent and probably the most selective alpha 2-adrenoceptor blocking agent presently available and is now frequently used for the investigation of peripheral and central alpha 2-adrenoceptors.

咪唑啉2-[2-(1,4-苯二氮氧基)]-2-咪唑啉的药理学性质在四年前首次被描述;从那时起,该化合物已被发现是目前可用的最具选择性的α 2-肾上腺素受体阻断剂之一。在外周部位,咪唑嗪可拮抗α - 2激动剂如阿西哌唑、B-HT 920、m7、UK 14304、α -甲基去甲肾上腺素、克拉定的作用,但对α - 1激动剂如唑啉和苯肾上腺素无效。在突触前部位,咪唑嗪由于刺激狗的加速神经而增加了心动过速,并且在狗和大鼠中拮抗α 2激动剂的抑制作用。与经典的α 2-肾上腺素受体阻滞剂相比,咪唑嗪的选择性更强,效力与育亨宾、劳沃辛、RS 21361、Wy 26703相当。在中心部位,已发现咪唑嗪可拮抗α 2激动剂的交感神经抑制作用。因此,咪唑嗪是一种有效的,可能是目前可用的最具选择性的α 2-肾上腺素受体阻断剂,现在经常用于外周和中枢α 2-肾上腺素受体的研究。
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引用次数: 0
[The influence in the rat of counter-irritation by turpentine on the leukocyte content of exudates induced by sponge implants]. [松节油抗刺激对大鼠海绵植入诱导的渗出液白细胞含量的影响]。
Pub Date : 1986-04-01
E Deflandre, J Damas

In normal rats, PGE1, arachidonic acid, indomethacin and diclofenac did not modify the leucocyte content of sponge exudates withdrawn 4 hours after implantation while arachidonic acid increased the level in PGE2 and indomethacin reduced it. The leucocyte content of sponges exudates withdrawn 18 hours after implantation was not modified by PGE1 and TXB2, but diminished by indomethacin and NDGA and increased by arachidonic acid. As the chemotactic effect of arachidonic acid was slightly reduced by indomethacin and abolished by NDGA, it could depend on the formation of lipoxygenase derivatives. In normal rats, the leucocyte content of sponge exudates withdrawn 18 hours after implantation was increased slightly by normal serum and largely by serum from turpentine-treated rats. The blood leucocyte content was not modified in turpentine-treated rats. However in these rats, the leucocyte content of sponge exudates was low comparatively to the leucocyte content in normal rats. This low level was not affected by indomethacin, arachidonic acid and normal serum. The leucocytes of turpentine-treated rats seem to be desensitizated towards chemotactic factors. Similar desensitization was observed in rats treated by iota carrageenan.

在正常大鼠中,PGE1、花生四烯酸、吲哚美辛和双氯芬酸对海绵渗出液中白细胞含量没有影响,而花生四烯酸使PGE2升高,吲哚美辛降低。PGE1和TXB2对海绵着床后18 h撤出的渗出液白细胞含量无影响,吲哚美辛和NDGA降低了白细胞含量,花生四烯酸增加了白细胞含量。由于花生四烯酸的趋化作用被吲哚美辛略微降低,而被NDGA消除,可能与脂氧合酶衍生物的形成有关。正常大鼠植入18小时后提取的海绵渗出液白细胞含量被正常血清略微增加,而被松节油处理的大鼠血清大量增加。经松节油处理的大鼠血液白细胞含量未见改变。但海绵渗出液的白细胞含量较正常大鼠低。这一低水平不受吲哚美辛、花生四烯酸和正常血清的影响。松节油处理的大鼠白细胞似乎对趋化因子脱敏。大鼠经角叉菜胶处理后也出现类似的脱敏现象。
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引用次数: 0
[The effects of different inhibitors on bronchoconstriction induced by leukotriene D4 in isolated and perfused guinea pig lung]. [不同抑制剂对白三烯D4诱导豚鼠离体肺和灌注肺支气管收缩的影响]。
Pub Date : 1986-04-01
G Trocklé, G Catau, C Kalt, M Jacque

The effects of selective inhibitions of both cyclo-oxygenase and lipoxygenase pathways were studied in the isolated, perfused and ventilated guinea-pig lungs. Leukotriene D4 (0.3 nmol) induced a significant bronchoconstriction. This effect was significantly inhibited by IPL 55712 (a SRS-A antagonist) and by Imidazole or Dazoxiben (specific thromboxane synthetase inhibitors), but aspirin and indomethacin were without significant effect on this broncho-constriction. Our results suggest that the principal component of leukotriene D4 induced bronchoconstriction in guinea-pig lungs is primary.

在离体、灌注和通气豚鼠肺中研究了选择性抑制环加氧酶和脂加氧酶途径的作用。白三烯D4 (0.3 nmol)引起支气管明显收缩。IPL 55712(一种SRS-A拮抗剂)和咪唑或达昔苯(一种特异性血栓素合成酶抑制剂)显著抑制了这种作用,但阿司匹林和吲哚美辛对这种支气管收缩无显著影响。我们的结果表明,白三烯D4诱导豚鼠肺支气管收缩的主要成分是原发的。
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引用次数: 0
[Pharmacologic profile of an original psychotropic drug. Minaprine: comparison with six reference antidepressives]. 一种原始精神药物的药理学特征。米那普林:与6种参考抗抑郁药的比较[j]。
Pub Date : 1986-04-01
P Worms, J P Kan, A Perio, C G Wermuth, K Bizière, R Roncucci

Minaprine (MIN) is a 3-amino-pyridazine derivative which exhibits a profile of psychotropic activities which resembles that of antidepressant drugs as well as that of several dopaminomimetic drugs. This spectrum of activity differs from those observed in the same conditions for tricyclic (imipramine, clomipramine) and atypical (indalpine, nomifensine, amineptine, mianserin) antidepressant drugs. It must be noted that MIN is devoid of anticholinergic and motor stimulant effects. In addition, MIN induces behavioural effects predictive of a dopaminergic stimulation; the profile of this activity differs from that of apomorphine, as well as from those of amphetamine and nomifensine, but somewhat resembles that of bromocryptine. MIN does not induce neuroleptic, anxiolytic or anticonvulsant activities in rodents. These data suggest that MIN is an atypical antidepressant drug which activates both serotonergic and dopaminergic neurotransmissions, by as yet not clearly identified mechanisms.

米那普利是一种3-氨基吡啶衍生物,具有类似于抗抑郁药和几种多巴胺类药物的精神药物活性。这种活性谱不同于在相同条件下观察到的三环(丙咪嗪,氯丙咪嗪)和非典型(吲哚平,诺非芬,氨奈汀,米安色林)抗抑郁药物。必须注意的是,MIN缺乏抗胆碱能和运动刺激作用。此外,MIN诱导行为效应预测多巴胺能刺激;这种活性的特征不同于阿波啡,也不同于安非他明和诺非芬,但在某种程度上类似于溴隐碱。在啮齿类动物中,MIN不诱导神经镇静、抗焦虑或抗惊厥活性。这些数据表明,MIN是一种非典型的抗抑郁药物,激活血清素能和多巴胺能神经传递,其机制尚未明确。
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引用次数: 0
Classification of benzodiazepine receptor agonists, inverse agonists and antagonists using bicuculline in an in vitro test. 苯二氮卓受体激动剂、逆激动剂和双库兰拮抗剂的分类体外试验。
Pub Date : 1986-04-01
P Jacqmin, M Wibo, M Lesne

The mechanism by which a substance that binds to the benzodiazepine receptor acts as an agonist, an inverse agonist (e.g. methyl-beta-carboline-3-carboxylate (beta-CCM] or an antagonist (e.g. Ro 15-1788) was investigated. For this purpose, we studied the influence of bicuculline, an antagonist of gamma-aminobutyric acid (GABA), on the binding of these substances in crude synaptosomal preparation (P2 fraction) containing high levels of endogenous GABA. Displacement curves were performed, using 3H-flunitrazepam in the absence and in the presence of a high concentration (7.10(-5) M) of bicuculline. The ratios of IC50 values with and without bicuculline were significantly higher than 1 for all benzodiazepine agonists investigated (e.g. 1.91 +/- 0.11 (n = 3) for diazepam), about 1 for Ro 15-1788 (0.94 +/- 0.06 (n = 4)) and lower than 1 for beta-CCE (0.55 +/- 0.05 (n = 4)). Statistically significant differences were also observed among benzodiazepine agonists e.g. between flunitrazepam (a sedative-hypnotic drug) and clonazepam (an anticonvulsant drug) or lorazepam (an anxiolytic drug). These data indicate that the ratios of IC50 values with and without bicuculline might provide the basis for an in vitro, pharmacologically relevant, classification of drugs acting on the benzodiazepine receptor. This procedure does not require extensive washing of the membrane preparation, in contrast to the method in which the ratios of IC50 values were determined with and without addition of GABA.

研究了与苯二氮卓受体结合的物质作为激动剂、逆激动剂(如甲基- β -羰基-3-羧酸酯(β - ccm))或拮抗剂(如Ro 15-1788)的机制。为此,我们研究了γ -氨基丁酸(GABA)拮抗剂双库兰(bicuculline)对含有高水平内源性GABA的粗突触体制剂(P2部分)中这些物质结合的影响。用3h -氟硝西泮在不存在和高浓度(7.10(-5)M)二胡兰存在的情况下绘制位移曲线。所有苯二氮卓类激动剂的IC50比值(如地西泮为1.91 +/- 0.11 (n = 3))均显著高于1,Ro 15-1788约为1 (0.94 +/- 0.06 (n = 4)), β - cce低于1 (0.55 +/- 0.05 (n = 4))。在苯二氮卓类激动剂之间,例如氟硝西泮(一种镇静催眠药物)与氯硝西泮(一种抗惊厥药物)或劳拉西泮(一种抗焦虑药物)之间,也观察到统计学上的显著差异。这些数据表明,使用和不使用双库兰的IC50值比值可能为作用于苯二氮卓受体的药物的体外药理学相关分类提供依据。与添加GABA和不添加GABA测定IC50值的方法相比,该方法不需要对膜制备进行大量洗涤。
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引用次数: 0
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Journal de pharmacologie
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