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双语推荐:羟色胺受体

目的 探讨功能性消化不良(FD)患者抗抑郁治疗初期出现胃肠道不良反应的机制,评价抗抑郁药物在FD治疗中的安全性.方法 将57例FD患者随机分为两组,研究组30例和对照组27例.前者给予SSRIs治疗,后者给予噻奈普汀治疗,于治疗后统计两组胃肠道不良反应的类型及发生率,并了解两种药物胃肠道不良反应与疗程的关系.结果 研究组胃肠道不良反应发生率明显高于对照组,且多发生于治疗早期,随着治疗时间的延长,不良反应症状逐渐减轻.结论 选择性5-羟色胺再摄取抑制剂(SSRIs)是一种新型的抗抑郁药,胃肠道不良反应的发生与胃肠道内环境的5-羟色胺浓度骤然增加有关,后者作用于胃肠道5-羟色胺受体亚型,引起各种胃肠道不良反应.
Objective To investigate the mechanism of gastrointestinal adverse reaction in the early antidepressant treatment of functional dyspepsia(FD) and evaluate the safety of antidepressant in the treatment of FD.Methods Fifty-seven FD patients were divided into two groups randomly,30 cases in the study group and 27 cases in the control group.The patients in study group were given selective serotonin reuptake inhibitors(SSRI),the patients in control group were given Tianeptine.The types and incidence of gastrointestinal adverse reaction were recorded and analyzed,meanwhile the relationship between gastrointestinal adverse reaction and the period of treatment was understanded.Results The incidence of gastrointestinal adverse reaction in the study group was obviously higher than that in the control group,and mostly happened in the earlier treatment.As the treatments going,the gastrointestinal adverse reaction reduced gradually.Conclusions SSRIs is a new antidepressant drug.In the treatments,su

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瘙痒是皮肤科的一种常见症状,是多因素相互作用的结果,其发生受到中枢和外周机制的双重调控,但具体发生机制尚不十分清楚。近年来随着研究的不断深入,多种物质如组胺、乙酰胆碱、5-羟色胺、蛋白酶和蛋白酶相关受体、细胞因子、阿片样肽等介质在瘙痒产生过程中起重要作用,这些介质通过刺激C类神经纤维或直接与皮肤感觉神经纤维受体相结合来介导瘙痒。本文就将皮肤瘙痒的神经传导及传导介质作一综述。
Objective:Itching is a common symptom of dermatology, is the result of the interaction of multiple factors, which by the central and peripheral mechanisms of dual control occur, but the exact mechanism is not clear.With the deepening of research in recent years, a variety of substances such as histamine, acetylcholine, serotonin, proteases and protease-related receptors, cytokines, opioid peptides, and other media play an important role in the generation process of pruritus, these media by stimulating type C nerve fibers or nerve fibers directly mediate receptor binding and skin feel itchy. Nerve conduction and conduction article will pruritus medium reviewed.

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帕金森病(Parkinson''s disease)是一种慢性进展的中枢神经系统变性疾病,临床上以静止性震颤、运动减少、肌张力障碍和步态异常为特点.罗替戈汀是当前治疗帕金森病的新型药物之一,为非麦角类多巴胺受体激动剂,可以结合多巴胺D1到D5受体以及五羟色胺1A受体,但是对D3受体的亲和力和激动作用最高[1].罗替戈汀透皮贴剂是第一个非麦角类多巴胺受体激动剂贴剂[1],每日给药1次就能够在24 h中提供稳定的血浆药物浓度.罗替戈汀透皮贴在欧洲和北美已经被批准用于帕金森病的治疗,在国内尚处于临床试验阶段.多个大型的多中心、双盲、随机、对照研究均显示,罗替戈汀对能明显改善帕金森病的运动症状,并且对帕金森病的非运动症状有一定改善作用[2].
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慢性便秘是老年人最常见的消化道症状之一,不仅影响老年人的生活质量,也存在诱发或加重其他疾病的危险性。老年人慢性便秘的病因复杂,治愈难度大,目前主要是根据便秘的病因、分类及其严重程度进行综合治疗,常见的治疗方法包括调整生活方式、药物治疗、精神心理治疗、手术治疗及生物反馈等。本文针对近年来国内外老年人慢性便秘药物治疗进展,尤其是5-羟色胺受体激动剂、鸟苷酸环化酶c受体激动剂、氯离子通道激活剂、阿片μ受体拮抗剂等新型药物的疗效及安全性进行综述。
As one of the most common gastrointestinal symptoms in the elderly, chronic constipation (CC) not only affects the seniors’ life quality, but also aggravates the risk of other diseases. Because of the complicated pathogenesis, CC in the elderly is difficult to cure. At present, comprehensive treatment is mainly based on the causes, classification and severity. Common treatments include adjusting life style, medication, psychological treatment, surgical treatment, biofeedback, etc. In this paper, the recent advances in the medication of CC in the elderly were reviewed, especially on the efficacy and safety of new drugs, such as 5-hydroxytryptamine (5-HT) receptor agonist, guanylate cyclase C agonist, chlorine ion channel activator, mu-opioid receptor antagonist, and so on.

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化疗相关性恶心呕吐( CINV)严重影响肿瘤患者的生活质量。随着止呕药物的发展,急性、延迟性CINV的控制率较前已有明显升高,但延迟性CINV的控制率仍偏低。第1代5-羟色胺3(5-HT3)受体拮抗剂对延迟性CINV的控制率并不优于单用地塞米松、甲氧氯普胺和丙氯拉嗪。最近研究表明第2代5-HT3受体拮抗剂帕洛诺司琼、神经激肽1受体拮抗剂在控制延迟性CINV方面上优于第1代5-HT3受体拮抗剂,当其联合抗精神病药物如奥氮平、丙氯拉嗪等可明显提高延迟性CINV的控制率。本文对延迟性化疗相关性恶心呕吐的治疗进展作一综述。
Chemotherapy-induced nausea and vomiting( CINV) is associated with a significant deterioration in quality of life. With the development of antiemetic drugs, the control rate of acute and delayed CINV has significantly improved,but the control rate of delayed CINV is still low. The effect of first generations of 5-hydroxytryptamine-3(5-HT3) receptor antagonists are not significantly su-perior to dexamethasone, metoclopramide or prochlorperazine alone in the control of delayed CINV. Recent studies have shown that pal-onosetron, the second generation of 5-HT3 receptor antagonists, and NK-1 receptor antagonists are better than the first generation of 5-HT3 receptor antagonists in the prevention of delayed CINV. Combination with antipsychotics drugs such as olanzapine, prochlorperazine can effectively control delayed CINV.

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γ-氨基丁酸(γ-aminobutyric acid,GABA)是哺乳动物中枢神经系统中主要的抑制性神经递质,与焦虑、抑郁、精神分裂等多种神经和精神疾病有关。近年来,越来越多的研究提示,抑郁症的发生与中枢GABA功能缺陷密切相关。但目前基于单胺类递质失调及谷氨酸能神经的研究较多,而对GABA的研究相对较少且比较分散。本文主要通过介绍GABA受体及其作用,以及GABA与5-羟色胺(5-hydroxytryptamine,5-HT)、多巴胺(dopamine,DA)和谷氨酸(glutamic acid,Glu)的相互作用,讨论GABA与抑郁症发生的关系,以期为抑郁症的发生机制与治疗的深入研究提供思路。
γ-aminobutyric acid (GABA)is the major inhibitory neurotransmitter of the central nervous system (CNS)in mammalian,which involved in several mood disorders such as anxiety,depression and schizophrenia.Nowadays,there are growing evidences showed that the depression is concerned with a de-ficiency in brain GABA.However,there are numerous studies based on the monoamine hypothesis and glutamatergic dysfunction,while the study on GABA is relatively less and scattered.Our aim is to discuss the relationship between depression and GABA by introducing the role of GABA receptors and the interac-tion between GABA and 5-hydroxytryptamine,dopamine and glutamic acid.It provides new ideas for fur-ther study on the pathogenesis and therapy of depression.

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上气道扩张肌在维持上气道开放中起到重要作用,其中颏舌肌为典型的上气道扩张肌.阻塞性睡眠呼吸暂停低通气综合征(obstructive sleep apnea and hypopnea syndrome,OSAHS)主要表现为在睡眠过程中反复出现上气道塌陷,导致在睡眠中反复出现呼吸暂停和(或)低通气,引起低氧血症、高碳酸血症等一系列病理生理改变的综合征.目前已发现OSAHS患者觉醒时存在颏舌肌中枢代偿.中缝核5-羟色胺1受体(5-HT1受体)可能参与介导颏舌肌的中枢调控.
Upper airway dilator muscles play an important role in maintaining upper airway open,while the genioglossus is an important one of upper airway dilator muscles.Obstructive sleep apnea and hypopnea syndrome (OSAHS) is a disease characterized by frequent episodes of upper airway collapse during sleep,which results in a series of pathophysiological changes such as intermittent hypoxemia with/ without hypercapnia.Currently,it has been discovered that there exists central compensation of genioglossus in OSAHS patients during wakefulness.Raphe nucleus 5-hydroxytryptamine 1 receptor probably involves in the central control of genioglossus.
研究了5-羟色胺(5-HT)对马氏珠母贝解剖获得卵母细胞的促熟作用及5-HT受体(5-HTpf)在其性腺中的分布情况。通过体外浸泡的方法处理马氏珠母贝卵母细胞使其成熟,结果表明一定浓度的5-HT可显著促使马氏珠母贝卵母细胞生发泡破裂,并使已经发生生发泡破裂的卵母细胞进一步成熟,同时可诱导5-HT受体基因的表达。用原位杂交的方法对5-HT受体在马氏珠母贝性腺中的分布的研究结果揭示,卵巢中次级卵母细胞和卵细胞均存在5-HT受体,有阳性信号出现;精巢中仅滤泡壁及精母细胞中有少量表达。以上结果表明马氏珠母贝的卵母细胞不仅能产生5-HT并且可表达5-HT受体
To investigate the effect of 5-HT on the maturation of oocyte stripped from the pearl oyster Pinctada fucata, oocytes were treated with 5-HT solution in vitro. Results showed that 5-HT was able to induce not only the Germinal Vesicle Breakdown (GVBD) of the oocytes remarkably, but also the maturation of the oocytes already GVBD. Gene expression of the 5-HT receptor was able to be induced at the same time. Distribution of 5-HT receptor (5-HTpf) within gonads of P. fucata was also studied using in situ hybridization (ISH) technique. The results revealed that 5-HT receptor 5-HTpf existed in the oocytes of different development stages and in the spermatocytes, and the reactive substances of 5-HTpf distributed along the cytoplasm and membrane of oocytes and showed blue. The above results indicate that the oocytes of P.fucata can not only produce 5-HT, but also express its receptor.

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背景 5-羟色胺3(5-HT3)受体拮抗剂特别是第2代5-HT3受体拮抗剂帕洛诺司琼对术后恶心呕吐(postoperative nausea and vomiting,PONV)具有较好的预防作用,其药理学机制及临床应用状况近年来有了较为深入的研究和临床应用.目的 分析总结帕洛诺对各类手术PONV的预防效果及其作用机制.内容 第2代5-HT3受体拮抗剂帕洛诺司琼具有高度亲和性、长效性、副作用少等优点,通过阻断5-HT3与外周或中枢神经元的5-HT3受体结合,阻断迷走神经传入呕吐中枢和第四脑室化学感受区触发带,抑制呕吐反射,临床应用其预防PONV的高效性不断得到认可. 趋向 深入探讨其药理机制、副作用、预防PONV的临床应用等方面,以供临床工作者更加合理地应用其预防PONV.
Background The 5-HT3 antagonist,especially the second-generation of 5-HT3 antagonist palonosetron shows better efficacy against postoperative nausea and vomiting (PONV),its pharmacological mechanism and clinical efficacy were further investigated.Objective This paper sums up litures on its pharmacological mechanism and clinical efficacy on PONV prophylaxis.Content The second-generation 5-HT3 antagonist palonosetron has properties of greater receptor affinity,prolonged duration of action and few adverse effects.It blocks serotonin binding at vagal afferents in the gut and in the regions of the CNS involved in emesis,including the chemoreceptor trigger zone and the nucleus tractus solitarii,inhibits and emesis reflex,the high efficacy of palonosetron is being recognized.Trend This review summarizes its pharmacological mechanism of action,adverse effects,and clinical application on prevention of PONV,offering clinical reference to clinician to prevent PONV more reasonably.

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目的 探讨中国北方汉族人群中单胺氧化酶A(MAOA)受体基因、儿茶酚-O-甲基转移酶(COMT)受体基因、多巴胺D3受体(DRD3)基因和5-羟色胺2C(5-HT2c)受体基因与强迫症的关系.方法 采用聚合酶链反应扩增片段长度多态技术测定164例强迫症患者包括103个核心家系的MAOA-T1460C、COMT-Val158Met、DRD3-Ser9Gly、5-HT2c-Cys23Ser四个位点受体基因多态性,并进行关联和连锁不平衡(TDT)分析.结果 病例组与对照组MAOA-T1460C、COMT-Val158Met、DRD3-Ser9Gly、5-HT2c-Cys23Ser受体基因的基因型和等位基因总体分布均差异无统计学意义(P>0.05),四个受体基因位点均符合H-W平衡,其中MAOA-T1460C受体基因在女性病例组与对照组、早发组与对照组、既有强迫思维又有强迫行为组与对照组、仅有强迫观念组与对照组的基因型和等位基因总体分布差异有统计学意义(P<0.05),且与家系组间存在连锁(P=0.0001);5-HT2c-Cys23Ser受体基因在男性病例组与对照组、既有强迫思维又有强迫行为组与对照组的基因型和等位基因总体分布差异有统计学意义(P<0.05),且与家系组之间存在连锁(P=0.0389);COMT-Val158Met受体基因在此对照实验中均差异无统计学意义(P>0.05),且与家系组间不存在连锁(P=0.0622);DRD3-Ser9Gly
Objective To explore the relationship between Monoamine oxidase A (MAOA) receptor gene,catechol-O-methyltransferase (COMT) receptor gene,dopamine D3 receptor(DRD3) gene and 5-HT2C receptor gene(5-HT2c) of Han population in northern China and obsessive compulsive disorder.Methods Polymerase chain reaction amplification determination of MAOA-T1460C,COMT-Val158Met,DRD3-Ser9Gly,5-HT2c-C ys23Ser four loci receptor gene polymorphism in 164 patients with OCD patients including 103 core pedigrees of fragment length polymorphism,and association and linkage disequilibrium (TDT)analysis.Results There was no significant difference of MAOA-T1460C,COMT-Val158Met,DRD3-Ser9Gly,5-HT2c-Cys23Ser four receptor gene in the patient group and the control group of genotype and allele distribution difference(P>0.05),four receptor gene loci were in accordance with the balance of the H-W,the MAOA-T1460C receptor gene in female patients group and control group,the early group and control group,which ha