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5-羟色胺拮抗剂ritanserin

国外医药.合成药.生化药.制剂分册 1988年第6期 369-370页

作者：吴国员

利坦舍林（ritanserin）是一种对5-羟色胺引起离体血管和气管收缩的有效拮抗剂,一般比酮舍林（Ketanserin）更为有效。与酮舍林相比,本品显然是一种非竞争性的拮抗剂,其抑制作用比酮舍林持久。两者对由胃肠组织内M或D受体传送的5-羟色... 详细信息

利坦舍林（ritanserin）是一种对5-羟色胺引起离体血管和气管收缩的有效拮抗剂,一般比酮舍林（Ketanserin）更为有效。与酮舍林相比,本品显然是一种非竞争性的拮抗剂,其抑制作用比酮舍林持久。两者对由胃肠组织内M或D受体传送的5-羟色胺反应均无作用,表明对抗5-羟色胺活性具选择性。当本品和酮舍林的浓度分别高于S2-5-羟色胺拮抗剂作用需要的20和4倍时,在兔的股动脉中可见H1-组胺反应。其他作用如α1肾上腺素能拮抗作用,在本品浓度高于S2拮抗作用需要的200倍时可以见到。在一项活动场地敞开的试验中确定大鼠

关键词：色胺吲哚 ritanserin 精神分裂症患者拮抗剂锥体外系静坐不能酮舍林本品

ritanserin治疗在神分裂症阴性症状

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国际精神病学杂志 1994年第2期 114-114页

作者：张毅

Ｒｉｔａｎｓｅｒｉｎ治疗在神分裂症阴性症状【英】／ＤｕｉｎｋｅｒｋｅＳＪ…／／ＢｒＪＰｓｙｃｈｉａｔｒｙ．－１９９３，１６３（１０）；－４５１～４５５Ｒｉｔａｎｓｅｒｉｎ是一种新型的５－ＨＴ２和５－ＨＴ４选择性拮抗剂... 详细信息

Ｒｉｔａｎｓｅｒｉｎ治疗在神分裂症阴性症状【英】／ＤｕｉｎｋｅｒｋｅＳＪ…／／ＢｒＪＰｓｙｃｈｉａｔｒｙ．－１９９３，１６３（１０）；－４５１～４５５Ｒｉｔａｎｓｅｒｉｎ是一种新型的５－ＨＴ２和５－ＨＴ４选择性拮抗剂。据报道此药能缓解分裂症患者的阴性...

关键词：阴性症状患者病人分裂症 ritanserin

5-Hydroxytryptamine:a potential therapeutic target in amyotrophic lateral sclerosis

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Neural Regeneration Research 2023年第9期18卷 2047-2055页

作者： Shi-Shi Jiang Meng-Ni Gong Wei Rao Wen Chai Wen-Zhi Chen Xiong Zhang Hong-Bing Nie Ren-Shi Xu Medical College of Nanchang University Department of NeurologyJiangxi Provincial People’s HospitalThe First Affiliated Hospital of Nanchang Medical CollegeClinical College of Nanchang Medical CollegeNanchangJiangxi ProvinceChina Department of Neurology The First Affiliated Hospital of Nanchang UniversityNanchangJiangxi ProvinceChina Department of Neurology Maoming People’s HospitalMaomingGuangdong ProvinceChina

Previous studies have indicated that the pathogenesis of amyotrophic lateral sclerosis(ALS) is closely linked to 5-hydroxytryptamine(5-HT).To investigate this further,we administered 5-HT receptor antagonists to SOD1*G93A transgenic(ALS mouse model) and wide-type *** involved intraperitoneal injections of either granisetron,piboserod,or ritanserin,which inhibit the 5-HT3,5-HT4,and 5-HT2 receptors,*** transgenic mice were found to have fewer5-HT-positive cells in the spinal cord compared with wide-type *** found that the administration of granisetron reduced the body weight of the transgenic mice,while piboserod and ritanserin worsened the motor functioning,as assessed using a hanging wire ***,none of the 5-HT receptor antagonists affected the disease *** analyzed the distribution and/or expression of TAR DNA binding protein 43(TDP-43) and superoxide dismutase 1 G93A(SOD1-G93A),which fo rm abnormal aggregates in *** found that the expression of these proteins increased following the administration of all three 5-HT receptor *** addition,the disease-related mislocalization of TD P-43 to the cytoplasm increased markedly for all three *** ce rtain anatomical regions,the 5-HT receptor antagonists also led to a marked increase in the number of astrocytes and microglia and a decrease in the number of *** results indicate that 5-HT deficiency may play a role in the pathogenesis of amyotrophic lateral sclerosis by inducing the abnormal expression and/or distribution of TDP-43 and SOD1-G93A and by activating glial cells.5-HT co uld therefore be a potential therapeutic target for amyotrophic lateral sclerosis.

关键词： 5-hydroxytryptamine amyotrophic lateral sclerosis astrocytes granisetron microglia neuron piboserod ritanserin SOD1-G93A TAR DNA-binding protein 43

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Influence of Withania somnifera on obsessive compulsive disorder in mice

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Asian Pacific Journal of Tropical Medicine 2012年第5期5卷 380-384页

作者： Bhanu PS Kaurav Manish M Wanjari Amol Chandekar Nagendra Singh Chauhan Neeraj Upmanyu Department of Pharmacology R.K.D.F.College of PharmacyBhopal M.P.India Department of Pharmacology Central Research Institute(ay.) AmkhoGwaliorM.P.India Department of Pharmaceutical Sciences.Doctor Hari Singh Gour Vishwavidyalaya Sagar-470003(M.P.) India Department of Pharmaceutical Sciences Doctor Hari Singh Gour Vishwavidyalaya Sagar-470003(M.P.) India

Objective:To study the influence of methanolic and aqueous extract of Withania somnifera (***) root on the marble-burying behavior of mice a well-accepted model of obsessive compulsive ***:Mice were divided in different groups(n=6).Fluoxetine(5,10,15 mg/kg), (10,25,50,100 mg/kg) and melhanolic extract ***(MEWS)(10,25,50,100 mg/kg) were administered i.p.30 *** to the assessment of marble burying behavior and locomotor *** control group received vehicle of the ***:Administration of aqueous extracts ***(AEWS) and MEWS(50 mg/kg) successively decreaesed the marble burying behavior activity without affecting motor *** effect of AEWS and MEWS was comparable to standard fluoxetine,ritanserin and ***:*** extract is effective in treating obsessive compulsive disorder.

关键词： Withania somnifera Fluoxetine ritanserin Parachlorophenylalanine Obsessive compulsive behavior

5-HT receptors mediating external carotid vasoconstriction in vagosympathectomized dogs

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中国药理学报 1999年第12期20卷 1057-1067页

作者： Carlos M VILLALóN David CENTURIóN Araceli SóNCHEZ-LóNEZ Peter DE VRIES Pramod SAXENA Departamento de Farmacologia CINVESTAV-IPNApdoPostal 2202614000 Mxico DFMxico Department of Pharmacology Dutch Migraine Research Group and Cardiovascular Research Institute"COEUR"Erasmus University Medical Centre Rotterdam"EMCR"PO Box 17383000 DR RotterdamThe Netherlands

One specific example reflecting the completity ofcardiovascular responses induced by serotonin(5-hydroxytryptamine;5-HT)and the progress achieved inthe pharmacological characterization of the receptorsinvolved can be illustrated by the effects of 5-HT on thecanine external carotid artery *** thisframework,it has been shown that the external carotidvasoconstrictor response to 5-HT in the dog is mediatedby'5-HT_(1)-like'receptors,which being blocked by the5-HT_(1B/1D)receptor antagonist GR127935,resemble 5-HT_(1B/1D)(previously called 5-HT_(1B/1D))*** was proposed that these receptors coilld belong to the 5-HT_(lB),rather than the 5-HT_(lD),subtype on the basis of their resistance to blockade by a high dose of ritanserin(a potential 5-HT_(lD)receptor antagomst and the presence of mRNA for 5-HT_(lB)(5-HT_(lDB))receptors,but not for 5-HT_(lD)(5-HT_(lD))receptors,in vascalar smooth *** the advent of subtype-selective antagonists it was subsequently shown that the external carotid vasocenstriction to 5-HT and surmantriptan is dose-dependently antagonized by the selective 5-HT_(lB)receptor antagonist SB224289[2,3,6.7-telrahydro-I'-methyl-5-[2'-methyl-4(5-methyl-1,2,4-oxadiazol-3-y1)biphenyl-4-carbonyl]]furo[2,3-f]indole-3-spiro-4'-piperidine hydrochloride],whereas the selective 5-HT_(lD)receptor antagonist BRL15572[l(3-chloropheny1)-4-[3,3-diphenyl(2-(S,R)hydroxypropany1)piperazine]hydrochloride was *** findings represent the first in vivo evidence showing that vascular constriction induced by 5-HT and sumatriptan is mediated primarily via 5-HT_(lB),but not 5-HT_(lD)*** pharmacological profile of these receptors could be similar(isolated human temporal artery and porcine carotid arteriovenous anastomoses)to other putative 5-HT_(lB)receptors mediating vasoconstrictor *** view of the putative pathophysiologic role of external carotid(and extracerebral)vasodilation in migraine,the constriction of these blood vessels by s

关键词： serotonin receptors BRL15572 external carotid artery GR127935 SB224289 sumatriptan vasoconstriction ritanserin ketanserin migraine

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Orexin-A对实验性酒精昏迷大鼠的促醒效应及神经机制

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Orexin-A对实验性酒精昏迷大鼠的促醒效应及神经机制

作者：贾晓军第三军医大学

学位级别：硕士

昏迷是指一种意识完全丧失、不易唤醒的状态,昏迷对机体功能影响大、预后差,致残及死亡率较高。如何提高昏迷的促醒治愈率是当今医学研究亟待解决的重要课题。据文献报道,颅脑外伤、脑血管疾病和酒精中毒是昏迷发生的三大主要病因。随... 详细信息

昏迷是指一种意识完全丧失、不易唤醒的状态,昏迷对机体功能影响大、预后差,致残及死亡率较高。如何提高昏迷的促醒治愈率是当今医学研究亟待解决的重要课题。据文献报道,颅脑外伤、脑血管疾病和酒精中毒是昏迷发生的三大主要病因。随着现代化生活节奏加快和人们精神压力的加重,酗酒者越来越多。酒精中毒逐渐成为国内外学者研究的热点,但由于中毒机制尚未完全明了,目前促醒药物仅局限于纳洛酮、醒脑静和麝香等。进一步明确酒精性昏迷发生机制及研发新型、更有效的促醒药物具有重要的现实意义。本实验首先建立大鼠酒精昏迷模型,通过行为反应检测、脑电图(ECoG)记录及单位放电记录,观察了酒精对大鼠觉醒能力的损害作用,并随后研究了orexin-A对酒精昏迷大鼠的促醒效应及其可能神经机制。结果如下: 1.大鼠酒精昏迷模型的建立腹腔注射(ip)32%(14ml/kg)酒精,建立酒精昏迷大鼠模型。酒精是生活中一种易得、合法及使用较广泛的药物,该模型经济适用。另外,该模型相似性好,易于复制。模型稳定,较好地模拟了酒精对觉醒能力的损害作用。 2. Orexin-A对酒精昏迷大鼠的促醒效应 (1) Orexin-A对酒精昏迷大鼠行为及ECoG的促醒效应通过翻正反射消失(LORR)持续时间及ECoG中δ波比例多少判断大鼠行为和ECoG改变。结果显示,32%酒精ip后,大鼠短时间内即出现LORR,意识状态Ⅴ‐Ⅵ级,行为上符合昏迷判定标准,LORR持续时间3.07±0.94h(n=30)。酒精ip至LORR止,ECoG中δ波比例为16.42±3.14%(n=6),LORR后ECoG中δ波比例逐渐增高,20-25min时明显增高(n=6, P<0.01)。大鼠翻正反射恢复时ECoG中δ波比例为22.79±4.73%(n=6),腹腔追加注射1?2量酒精后,δ波比例即可逐渐增高(n=6, P<0.05)。LORR持续时间3.39±0.86h。结果表明,腹腔注射酒精可使大鼠出现LORR及ECoG

关键词：酒精昏迷 orexin-A 促醒翻正反射 δ波单位放电前额叶皮层觉醒组胺去甲肾上腺素 5-羟色胺 pyrilamine prazosin ritanserin 模型大鼠酒精中毒皮层脑电图

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5-HT与动脉血压调节

中国医学生物技术应用 2002年第1期 1-15,43页

作者：杜文民苏定冯上海市药品不良反应监测中心上海200040 第二军医大学基础部药理学教研室上海200433

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