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Pindolol, a putative 5-Hydroxytryptamine_1A antagonist, does not reverse the inhibition of serotonergic neuronal activity induced by fluoxetine in awake cats:: Comparison to WAY-100635

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JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS 1999年第1期291卷 220-228页

作者： Fornal, CA Martin, FJ Metzler, CW Jacobs, BL Princeton Univ Dept Psychol Program Neurosci Princeton NJ 08544 USA

The ability of pindolol to enhance the clinical antidepressant response to selective serotonin reuptake inhibitors (SSRIs) is generally attributed to a blockade of the feedback inhibition of serotonergic neuronal activity mediated by somatodendritic 5-hydroxytryptamine (5-HT)(1A) autoreceptors. The current study examined the ability of pindolol to restore the single-unit activity of serotonergic dorsal raphe nucleus neurons in awake cats after acute treatment with the SSRI fluoxetine. The effects of pindolol were compared with those of N-[2-[4-(2-methoxyphenyl)-1-piperazinyl]ethyl]-N-(2-pyridinyl) cyclohexanecarboxamide (WAY-100635), a selective 5-HT1A receptor antagonist. Systemic administration of fluoxetine (0.5 and 5 mg/kg i.v.) decreased neuronal firing rates to similar to 50 and 1%, respectively, of baseline levels. The subsequent administration of cumulative doses of (+/-)-pindolol (0.1-5 mg/kg i.v.) failed to reverse the neuronal inhibition produced by either dose of fluoxetine. In addition to lacking efficacy as an antagonist in these experiments, (+/-)-pindolol produced an additional decrease in neuronal activity in animals pretreated with the low dose of fluoxetine. The active enantiomer, (-)-pindolol (1 mg/kg i.v.), also was ineffective in restoring neuronal activity after fluoxetine. In contrast, systemic administration of WAY-100635 completely reversed the effect of fluoxetine (5 mg/kg) at low doses (0.025 mg/kg i.v.), and further elevated the firing rate of these neurons above prefluoxetine baseline levels. Overall, these results indicate that pindolol, unlike WAY-100635, lacks appreciable antagonist activity at 5-HT1A autoreceptors. Thus, the clinical efficacy of pindolol in augmenting the antidepressant response to SSRIs, such as fluoxetine, may be unrelated to a restoration of serotonergic neuronal activity.

关键词：药物相互作用氟西汀/投药和剂量氟西汀/药理学神经元/药物作用神经元/代谢吲哚洛尔/投药和剂量吲哚洛尔/药理学哌嗪类/投药和剂量哌嗪类/药理学吡啶类/投药和剂量吡啶类/药理学中缝核/药物作用中缝核/代谢受体血清素/药物作用受体血清素/代谢受体血清素 5-HT1 血清素/代谢血清素拮抗药/投药和剂量血清素拮抗药/药理学血清素摄取抑制药/投药和剂量血清素摄取抑制药/药理学动物猫男(雄)性

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Combining ondansetron and naltrexone treats biological alcoholics: Corroboration of self-reported drinking by serum carbohydrate deficient transferrin, a biomarker

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ALCOHOLISM-CLINICAL AND EXPERIMENTAL RESEARCH 2001年第6期25卷 847-849页

作者： Ait-Daoud, N Johnson, BA Javors, M Roache, JD Zanca, NA Univ Texas Hlth Sci Ctr Dept Psychiat San Antonio TX 78229 USA Univ Texas Hlth Sci Ctr SW Texas Addict Res & Technol Ctr San Antonio TX 78229 USA Univ Texas Hlth Sci Ctr Dept Pharmacol San Antonio TX 78229 USA

Background: Recently, we showed by using self-report that combining ondansetron (4 mu /kg twice a day) and naltrexone (25 mg twice a day) was effective at reducing drinking and increasing abstinence among early-onset alcoholics (EOAs), who are characterized by a range of antisocial behaviors and high biological and familial disease predisposition. Here, we investigated whether the self-reported differences in drinking would be corroborated by measurements of serum carbohydrate-deficient transferrin (CDT) level, a sensitive, reliable, and well-validated marker of transient alcohol consumption. Method: An 8-week double-blind clinical trial was performed in which 20 EOAs were randomized to receive ondansetron (4 mug/kg twice a day) and naltrexone (25 mg twice a day) or placebo as an adjunct to weekly standardized cognitive behavioral therapy. Serum CDT was assessed at weeks 0 (baseline), 4, and 8. Results: Log serum CDT was significantly lower in the ondansetron and naltrexone group (group mean, 1.44 +/-: 0.076) compared with the placebo group (group mean, 1.82 +/- 0.113), as evidenced by a main effect of group [F(1,15) = 7.2,p = 0.017;effect size = 0.32], visit [F(1,16) = 11.2, p = 0.004;effect size = 0.41], and an interaction between group and visit [F(1,16) = 27.54,p < 0.001;effect size = 0.63];Conclusions: The combination of ondansetron plus naltrexone was superior to placebo at reducing serum CDT. This corroborated our self-reported drinking data and demonstrated that the medication combination is an effective treatment for EOAs.

关键词：饮酒/血液酒精中毒/药物疗法生物学标记/血液双盲法药物疗法联合纳曲酮/投药和剂量纳曲酮/治疗应用麻醉品拮抗药/投药和剂量麻醉品拮抗药/治疗应用昂丹司琼/投药和剂量昂丹司琼/治疗应用安慰剂血清素拮抗药/投药和剂量血清素拮抗药/治疗应用转铁蛋白/类似物和衍生物转铁蛋白/分析成年人女(雌)性人类男(雄)性

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Opioid-induced pruritus:: repeated vs single dose ondansetron administration in preventing pruritus after intrathecal morphine

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BRITISH JOURNAL OF ANAESTHESIA 1999年第5期83卷 822-822页

作者： Dimitriou, V Voyagis, GS Gennimatas Hosp Dept Anaesthesiol Athens Greece Sotiria Hosp Dept Anaesthesiol Athens Greece

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Linezolid, Alosetron, Levetiracetam.

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American journal of health-system pharmacy : AJHP : official journal of the American Society of Health-System Pharmacists 2000年第16期57卷 1480-1484页

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Microdialysis sampling coupled to HPLC for transdermal delivery study of ondansetron hydrochloride in rats

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BIOMEDICAL CHROMATOGRAPHY 2000年第3期14卷 141-143页

作者： Ding, PT Xu, H Wei, G Zheng, JM Shenyang Pharmaceut Univ Dept Pharm Shenyang 110015 Peoples R China

The transdermal delivery of ondansetron hydrochloride (ON) solution in propylene glycol (PG) with a widely used penetration enhancer, oleic acid (OA), was studied in rats by a microdialysis sampling technique. Dialysate samples collected from the probe were directly injected into the HPLC system without any pre-treatment and no interference occural in the blank sample. A good linearity between the standard concentrations and peak areas within the calibration range was achieved. In vivo recovery (32.52 +/- 1.8%) of the probe was assessed with the retrodialysis method, which was used to calculate the ON concentration in the dermis. Oleic acid at the concentrations of 2% and 5% (w/v) increased the steady-state delivery rate from 0.001 to 0.030 and 0.058 mu g/h, respectively OA proved to be an effective enhancer for transdermal delivery of ON in rats. Copyright (C) 2000 John Wiley & Sons, Ltd.

关键词：投药皮肤止吐药/投药和剂量止吐药/分析色谱法高压液相/方法动力学微透析油酸昂丹司琼/投药和剂量昂丹司琼/分析昂丹司琼/药代动力学丙二醇血清素拮抗药/投药和剂量血清素拮抗药/分析皮肤/化学皮肤/代谢溶液动物男(雄)性大鼠

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1-[2-[(heteroaryloxy)heteroaryl]carbamoyl]indolines:: Novel and selective 5-HT_2C receptor inverse agonists with potential as antidepressant/anxiolytic agents

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BIOORGANIC & MEDICINAL CHEMISTRY LETTERS 2000年第16期10卷 1863-1866页

作者： Bromidge, SM Dabbs, S Davies, S Duckworth, DM Forbes, IT Jones, GE Jones, J King, FD Saunders, DV Blackburn, TP Holland, V Kennett, GA Lightowler, S Middlemiss, DN Riley, GJ Trail, B Wood, MD SmithKline Beecham Pharmaceut Discovery Res Harlow CM19 5AW Essex England

Bisaryl ethers have been identified with excellent 5-HT2C affinity and selectivity over both 5-HT2A and 5-HT2B receptors. Compounds such as 11, 27 and 38 have potent oral activity in a centrally mediated pharmacodynamic model of 5-HT2C function and their potential as novel non-sedating anxiolytic and antidepressants is under investigation. (C) 2000 Elsevier Science Ltd. All rights reserved.

关键词：投药口服氨基吡啶类/投药和剂量氨基吡啶类/化学合成氨基吡啶类/化学氨基吡啶类/药理学抗焦虑药/投药和剂量抗焦虑药/化学合成抗焦虑药/化学抗焦虑药/药理学抗抑郁药/投药和剂量抗抑郁药/化学合成抗抑郁药/化学抗抑郁药/药理学药物设计吲哚类/投药和剂量吲哚类/化学合成吲哚类/化学吲哚类/药理学动力学分子结构运动活动/药物作用受体血清素 5-HT2C 受体血清素/化学受体血清素/代谢血清素拮抗药/投药和剂量血清素拮抗药/化学合成血清素拮抗药/化学血清素拮抗药/药理学构效关系动物人类大鼠

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1-[2-[(heteroarylmethoxy)aryl]carbamoyl]indolines are selective and orally active 5-HT_2C receptor inverse agonists

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BIOORGANIC & MEDICINAL CHEMISTRY LETTERS 2000年第16期10卷 1867-1870页

作者： Bromidge, SM Davies, S Duckworth, DM Forbes, IT Jones, GE Jones, J King, FD Blackburn, TP Holland, V Kennett, GA Lightowler, S Middlemiss, DN Riley, GJ Trail, B Wood, MD SmithKline Beecham Pharmaceut Discovery Res Harlow CM19 5AW Essex England

Bisarylmethoxyethers have been identified with nanomolar 5-HT2C affinity and selectivity over both 5-HT2A and 5-HT2B receptors. Compounds such as 1, 2, 8, 12, 14 and 18 have potent oral activity in a centrally mediated pharmacodynamic model of 5-HT2C function and their therapeutic potential is currently under further investigation. (C) 2000 Elsevier Science Ltd. All rights reserved.

关键词：氨基吡啶类/投药和剂量氨基吡啶类/化学合成氨基吡啶类/化学氨基吡啶类/药理学药物设计吲哚类/投药和剂量吲哚类/化学合成吲哚类/化学吲哚类/药理学动力学分子结构运动活动/药物作用受体血清素 5-HT2C 受体血清素/代谢血清素拮抗药/投药和剂量血清素拮抗药/化学合成血清素拮抗药/化学血清素拮抗药/药理学构效关系动物大鼠

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