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陕西医学杂志 2007年第2期36卷 190-191页

作者：董补怀孙晓娟西安市红十字会医院麻醉科西安710054

目的:观察格拉司琼用于脊柱术后病人自控镇痛抗恶心、呕吐作用效果。方法:选择择期全麻下脊柱减压、融合植骨内固定术患者120例,采用双盲随机对照研究,分为3组:A组(n=40),镇痛药液为每毫升含芬太尼0.015mg、格拉司琼0.06mg;B组(n=40),... 详细信息

目的:观察格拉司琼用于脊柱术后病人自控镇痛抗恶心、呕吐作用效果。方法:选择择期全麻下脊柱减压、融合植骨内固定术患者120例,采用双盲随机对照研究,分为3组:A组(n=40),镇痛药液为每毫升含芬太尼0.015mg、格拉司琼0.06mg;B组(n=40),镇痛药液为每毫升含芬太尼0.015mg、氟哌利多0.02mg;C组(n=40),镇痛药液为每毫升含芬太尼0.015mg。所用药液用生理盐水稀释至100ml,采用艾可孚镇痛泵静脉镇痛,术后随访48h,观察3组恶心、呕吐发生情况。结果:恶心、呕吐发生率A组低于B组(P<0.05),B组低于C组(P<0.05)。结论:格拉司琼用于脊柱术后病人自控镇痛有明显抗恶心呕吐作用。

关键词：恶心呕吐/预防与控制血清素拮抗药/治疗应用 @格拉司琼

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Mice with reduced NMDA receptor expression display behaviors related to schizophrenia

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CELL 1999年第4期98卷 427-436页

作者： Mohn, AR Gainetdinov, RR Caron, MG Koller, BH Univ N Carolina Curriculum Genet & Mol Biol Chapel Hill NC 27599 USA Univ N Carolina Dept Med Chapel Hill NC 27599 USA Duke Univ Med Ctr Howard Hughes Med Inst Labs Dept Cell Biol & Med Durham NC 27710 USA

N-methyl-D-aspartate receptors (NMDARs) represent a subclass of glutamate receptors that play a critical role in neuronal development and physiology. We report here the generation of mice expressing only 5% of normal levels of the essential NMDAR1 (NR1) subunit. Unlike NR1 null mice, these mice survive to adulthood and display behavioral abnormalities, including increased motor activity and stereotypy and deficits in social and sexual interactions. These behavioral alterations are similar to those observed in pharmacologically induced animal models of schizophrenia and can be ameliorated by treatment with haloperidol or clozapine, antipsychotic drugs that antagonize dopaminergic and serotonergic receptors. These findings support a model in which reduced NMDA receptor activity results in schizophrenic-like behavior and reveals how pharmacological manipulation of monoaminergic pathways can affect this phenotype.

关键词：抗精神病药/治疗应用反社会性人格障碍/药物疗法反社会性人格障碍/遗传学行为动物/药物作用钙信号/药物作用氯氮平/药理学氯氮平/治疗应用疾病模型动物地卓西平马来酸盐/毒性多巴胺拮抗剂/药理学多巴胺拮抗剂/治疗应用兴奋性氨基酸拮抗剂/毒性谷氨酸/生理学氟哌啶醇/药理学氟哌啶醇/治疗应用小鼠基因敲除运动活动/药物作用运动活动/遗传学苯环利定/毒性受体 N-甲基-D-天冬氨酸/缺乏受体 N-甲基-D-天冬氨酸/遗传学受体 N-甲基-D-天冬氨酸/生理学精神分裂症心理学血清素拮抗药/药理学血清素拮抗药/治疗应用性行为动物/药物作用社会行为刻板行为/药物作用动物女(雌)性男(雄)性小鼠

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5-HT₄ receptor antagonism in irritable bowel syndrome:: effect of SB-207266-A on rectal sensitivity and small bowel transit

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ALIMENTARY PHARMACOLOGY & THERAPEUTICS 1999年第11期13卷 1437-1444页

作者： Houghton, LA Jackson, NA Whorwell, PJ Cooper, SM Univ S Manchester Hosp Dept Med Manchester M20 2LR Lancs England SmithKline Beecham Pharmaceut Harlow CM19 5AD Essex England

Background: Pre-clinical studies indicate that the 5-hydroxytryptamine (5-HT)(4) receptor may be involved in the pathophysiology of irritable bowel syndrome and that antagonism of this receptor may be an effective therapeutic strategy. Aim: To investigate the effects of SE-207266-A, a selective 5-HT4 receptor antagonist on rectal sensitivity and small bowel transit in patients with irritable bowel syndrome. Methods: Eighteen patients with diarrhoea-predominant irritable bowel syndrome and a history of increased rectal sensitivity were randomized to receive either SE-207266-A (20 mg) or placebo for 10 days. Following a washout period, patients were then crossed over to receive the alternative therapy for 10 days. Rectal sensitivity and orocaecal transit time were assessed on day 10 of each treatment period. In addition, patients were asked whether they had experienced any changes in their symptoms. Results: Fifteen patients completed the study. SB-207266-A significantly increased orocaecal transit time towards normal (placebo: 5.3 h (4.0-7.2 h), mean (IQR) vs. SE-207266-A: 6.5 h (4.8-8.0 h);P = 0.027) and tended to decrease rectal sensitivity (volume to discomfort 89 mL (60-150 mL), geometric mean (IQR) vs. 107 mL (75-150 mL);P = 0.134). Eleven out of 15 patients reported symptomatic improvements with SE-207266-A but none with placebo. SE-207266-A was well tolerated. Conclusion: Our results support a role for the 5-HT4 receptor in the pathophysiology of irritable bowel syndrome and suggest that the selective 5-HT4 antagonist, SE-207266-A, is worthy of further evaluation in this disorder.

关键词：气囊扩张术结肠疾病功能性/并发症结肠疾病功能性/药物疗法结肠疾病功能性/病理生理学交叉研究腹泻/药物疗法腹泻/病因学双盲法胃肠通过试验/药物作用吲哚类/治疗应用小肠/药物作用测压法哌啶类/治疗应用受体血清素/药物作用受体血清素 5-HT4 直肠/病理生理学血清素拮抗药/治疗应用成年人老年人女(雌)性人类男(雄)性中年人

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Alosetron, a 5-HT₃ receptor antagonist, delays colonic transit in patients with irritable bowel syndrome and healthy volunteers

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ALIMENTARY PHARMACOLOGY & THERAPEUTICS 2000年第6期14卷 775-782页

作者： Houghton, LA Foster, JM Whorwell, PJ Univ S Manchester Hosp Dept Med Manchester M20 2LR Lancs England

Background: Alosetron is a potent and selective 5-HT3 receptor antagonist, which has been shown to be beneficial in the treatment of female patients with non-constipated irritable bowel syndrome. Aim: To investigate the effect of alosetron on whole gut, small bowel and colonic transit in patients with irritable bowel syndrome (Study 1) and healthy volunteers (Study 2). Subjects: Thirteen patients with irritable bowel syndrome and 12 healthy volunteers. Methods: Both studies were randomized, double-blind, placebo-controlled with a two-way crossover design, in which each subject received alosetron (2 mg b.d. administered orally) or placebo for 8 days. Mean whole gut transit was determined from the excretion of radio-opaque markers;small bowel transit was determined from rise in breath hydrogen after a meal;and colonic transit and segmental transit were evaluated from abdominal X-ray. In addition, colonic transit was calculated by subtracting small bowel transit time from whole gut transit time. Results: Alosetron increased colonic transit time by prolonging left colonic transit in both patients with irritable bowel syndrome and controls. This resulted in a tendency for the whole gut transit to be delayed in irritable bowel syndrome patients (P=0.128), which was confirmed in controls (P=0.047). Conclusion: Alosetron delays colonic transit by prolonging left colonic transit. These results add to the body of evidence suggesting that alosetron should have a therapeutic role in patients with non-constipated irritable bowel syndrome.

关键词：咔啉类/药理学咔啉类/治疗应用结肠/药物作用结肠/生理学结肠疾病功能性/药物疗法结肠疾病功能性/病理学交叉研究双盲法胃肠通过试验/药物作用小肠/药物作用小肠/生理学血清素拮抗药/药理学血清素拮抗药/治疗应用成年人女(雌)性人类男(雄)性中年人

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Gastrointestinal functional bowel disorders: new therapies

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CURRENT OPINION IN CHEMICAL BIOLOGY 2000年第4期4卷 428-432页

作者： Chovet, M Parke Davis & Co Inst Rech Jouveinal F-94265 Fresnes France

Present therapies for functional gastrointestinal disorders are symptomatic and mainly treat altered bowel habits. New therapies are focused on nerve-gut communication dysfunction: 5-HT3 antagonists and 5-HT4 agonists have demonstrated activity in clinical trials. Promising targets for upper gut dysmotility drugs are motilin and cholecystokinin A receptors. Tachykinins, calcitonin gene-related peptide or glutamate antagonists are the most relevant candidates for visceral pain.

关键词：胃肠疾病/药物疗法受体胆囊收缩素A 受体胆囊收缩素/拮抗剂和抑制剂受体胃肠激素/激动剂受体毒蕈碱/代谢受体神经肽/激动剂血清素激动药/治疗应用血清素拮抗药/治疗应用人类

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Risperidone in Prader-Willi syndrome

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JOURNAL OF THE AMERICAN ACADEMY OF CHILD AND ADOLESCENT PSYCHIATRY 2000年第5期39卷 545-546页

作者： Durst, R Rubin-Jabotinsky, K Raskin, S Katz, G Zislin, J Hebrew Univ Jerusalem Hadassah Med Sch Hfar Shaul Hosp Mental Hlth Ctr IL-91010 Jerusalem Israel

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Effectiveness of a novel serotonin blocker, sarpogrelate, for patients with angina pectoris.

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American heart journal 2002年第2期144卷 E1页

作者： Kinugawa, Toru Fujita, Masatoshi Lee, Jong-Dae Nakajima, Hitoshi Hanada, Hiroyuki Miyamoto, Shoichi Division of Cardiology First Department of Internal Medicine Tottori University Tottori Japan

BACKGROUND: We have recently demonstrated that a single oral administration of sarpogrelate, a 5-HT(2A) receptor antagonist, may improve exercise capacity in anginal patients with well-developed collaterals. The aim of the current study was to investigate the effectiveness of 2-week treatment with sarpogrelate on anginal symptoms and exercise capacity in anginal patients. METHODS: A treadmill exercise test was repeated after a 2-week period with or without sarpogrelate (100 mg 3 times a day) in 20 patients with angiographically proven stable angina. Anginal symptoms and daily physical activity by the specific activity scale (SAS) were also evaluated. RESULTS: Treatment with sarpogrelate significantly increased the SAS score and prolonged exercise time to the onset of 0.1-mV ST depression. When data were analyzed in a subgroup of patients (n = 8) with well-developed collaterals, the treatment with sarpogrelate decreased the number of anginal attacks (control vs sarpogrelate, 3.0 +/- 2.8 vs 0.9 +/- 1.1/2 weeks, P <.05), increased the SAS score (5.2 +/- 1.6 vs 6.2 +/- 1.3 METS, P <.05), and increased the time to the onset of 0.1-mV ST depression (235 +/- 84 vs 295 +/- 127 seconds, P <.05). In addition, the double product at the onset of 0.1-mV ST depression increased by 15% (P <.05) after sarpogrelate. In contrast, all parameters were not significantly changed after sarpogrelate treatment in patients (n = 12) without well-developed collaterals. CONCLUSIONS: These findings indicate the therapeutic effectiveness of sarpogrelate for anginal patients, especially for patients with well-developed collaterals.

关键词：心绞痛/分类心绞痛/药物疗法心绞痛/病理生理学慢性病侧支循环冠状血管造影术药物疗法联合运动(Exercise) 运动试验硝酸甘油/投药和剂量血清素拮抗药/治疗应用琥珀酸盐/治疗应用治疗结果老年人女(雌)性人类男(雄)性中年人

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Sarpogrelate treatment reduces restenosis after coronary stenting

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AMERICAN HEART JOURNAL 2003年第3期145卷 E16页

作者： Fujita, M Mizuno, K Ho, M Tsukahara, R Miyamoto, A Miki, O Ishii, K Miwa, K Kyoto Univ Coll Med Technol Sakyo Ku Kyoto 6068507 Japan Chiba Hokusah Hosp Nippon Med Sch Dept Internal Med Chiba Japan Kawasaki Social Insurance Hosp Div Cardiol Kanagawa Japan Kawasaki Saiwai Hosp Div Cardiol Kanagawa Japan Kansai Elect Power Hosp Dept Internal Med 2 Osaka Japan

Background Sarpogrelate, a serotonin blacker, has been reported to inhibit the serotonin-induced proliferation of rat aortic smooth muscle cells. The aim of this study was to investigate whether sarpogrelate reduces restenosis after coronary stenting as a result of prevention of intimal hyperplasia. Methods We examined 79 patients with stable angina undergoing elective coronary stenting on de novo lesions of native coronary arteries in a prospective, randomized trial. All enrolled patients received aspirin and ticlopidine, and one third of the patients were assigned to receive oral sarpogrelote. Results Treatment with sarpogrelate in addition to aspirin and ticlopidine caused no major adverse cardiovascular events or hemorrhagic adverse effects during the 6-month follow-up period. The restenosis rate in the group of patients receiving sarpogrelate was 4.3%, which was significantly lower than the 28.6% rate found in the group of patients not receiving sarpogrelate. Conclusions Sarpogrelate treatment reduces restenosis after coronary stenting, which suggests that serotonin released from activated platelets may ploy an important role in stent restenosis.

关键词：心绞痛/放射摄影术心绞痛/外科学血管成形术经腔经皮冠状动脉阿司匹林/治疗应用细胞分裂/药物作用冠状血管造影术冠状动脉再狭窄/预防和控制冠状动脉再狭窄/放射摄影术药物疗法联合纤维蛋白溶解药/治疗应用随访研究肌平滑血管/药物作用肌平滑血管/生理学前瞻性研究血清素拮抗药/药理学血清素拮抗药/治疗应用琥珀酸盐/药理学琥珀酸盐/治疗应用噻氯匹定/治疗应用治疗结果老年人女(雌)性人类男(雄)性中年人

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Usefulness of intravenous granisetron for prevention of neurally mediated hypotension upon head upright tilt testing

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AMERICAN JOURNAL OF CARDIOLOGY 2000年第10期85卷 1262-+页

作者： Tsikouris, JP Kluger, J Chow, MSS White, CM Hartford Hosp Drug Informat Ctr Dept Pharm Hartford CT 06102 USA Hartford Hosp Div Cardiol Hartford CT 06102 USA Univ Connecticut Sch Pharm Storrs CT USA Univ Connecticut Sch Med Farmington CT USA Chinese Univ Hong Kong Shatin Hong Kong Peoples R China

The serotonergic system has been implicated in the pathophysiology of neurally mediated hypotension. The present pilot study suggests that 5-HT3 receptor antagonism with granisetron attenuates the early sympathetic component of neurally mediated syncope, and may contribute to the abolishment of syncope or presyncope upon head-up tilt testing.

关键词：肾上腺素能β激动剂/药理学队列研究心电描记术格兰塞隆/治疗应用低血压/病因学低血压/预防和控制异丙肾上腺素/药理学试点项目受体血清素受体血清素 5-HT3 血清素拮抗药/治疗应用晕厥/病因学晕厥/预防和控制倾斜台试验女(雌)性人类男(雄)性中年人

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Alosetron approved for treatment of irritable bowel syndrome

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AMERICAN JOURNAL OF HEALTH-SYSTEM PHARMACY 2000年第6期57卷 519-519页

作者： [Anonymous]

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