CAS: 78263-90-8; 2-Methylserotonin

该化合物是属于无粉族的有机化合物,其特点是含有一个有引信的苯和烧红环的双环结构,该化合物具有氨基乙基侧链和氢氧基化合物组,有助于其潜在的生物活动,在室温中一般是固体,由于存在氢氧基化合物,极溶剂中可能出现溶解性.氨基化合物可以参与氢的结合,影响其再活动以及与其他分子的相互作用.该化合物可能具有药用化学和药理学方面的兴趣,因为据了解,无粉衍生物具有多种生物特性,包括抗微生物和抗癌活动.其具体特性,如熔点,沸点和光谱数据,将取决于化合物的纯度和形式.在处理和储存时,应参考安全数据,如任何化学物质.

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合成工艺路线路线简述

    📜5-Methoxy-2-Methyltryptamine置于三溴化硼体系中,用 二氯甲烷 作为反应溶剂,化学反应 2.0H,以100%的收率获得产物2-甲基-5-羟基色氨酸盐酸
    参考文献:Pharmacological Assessment Of Sepiapterin Reductase Inhibition On Tactile Response In The Rat
    标题:Pharmacological Assessment Of Sepiapterin Reductase Inhibition On Tactile Response In The Rat
    摘要:在人类中,对于非阿片类镇痛药物存在未被满足的医疗需求;目前正研究多条可能用于治疗干预的通路.四氢生物蝶呤(bh4)最近作为一种神经病理性疼痛介质引起了关注.最近的研究报告将塞帕肽还原酶(spr)与这一疼痛通路联系起来,将其视为调节bh4反应生成的一种酶.为了评价spr抑制对bh4减少的作用,我们开发了分析方法来监测试验药物血浆浓度与内源性蝶呤之间的关系,并将其应用于大鼠脊神经结扎疼痛模型中.塞帕蝶呤是一种内源性底物,在spr被抑制的情况下会累积.在高强度spr抑制剂的作用下,塞帕蝶呤的血浆浓度与暴露量成比例地增加.我们构建了一个间接效应药代动力学/药效学模型,以描述试验药物血浆药代动力学与大鼠血浆中塞帕蝶呤水平之间的关系,并据此计算体内spr的ic50值.我们在血浆及神经元损伤部位(即背根神经节)协同评估了spr抑制,机械异常痛觉及蝶呤生物标志物.连续3天每日口服给药后,试验药物的未结合血浆浓度在整个剂量间隔期内均超过了大鼠体内未结合的spr的ic90值,从而使背根神经节中的bh4含量减少了60%.尽管有证据表明bh4通路被药理学调控,但与对照组相比,试验组在触觉性爪回缩阈值方面并未表现出显著影响.
    DOI:10.1124/jpet.119.257105

    海关参考信息

    专利信息


    专利号:WO-0054773-A1
    优先权日:1999-03-12
    标题:Dopamine agonists in combination with nitric oxide donors, compositions and methods of use
    发明人:GARVEY DAVID S
    权利人:NITROMED INC; GARVEY DAVID S
    摘要:The present invention is directed to novel compositions comprising at least one dopamine agonist in combination with at least one nitric oxide donor (i.e. compounds that donate, transfer or release nitric oxide, elevate endogenous levels of endothelium-derived relaxing factor, stimulate endogenous synthesis of nitric oxide or are substrates for nitric oxide synthase). The novel compositions may optionally comprise at least one therapeutic agent, such as, a vasoactive agent, an antimetic agent, and mixtures thereof. The dopamine agonist is preferably apomorphine. The present invention is also directed to methods for treating and/or preventing sexual dysfunctions and/or enhancing sexual responses in patients. In other embodiments, the present invention is directed to methods treating or preventing neurodegenerative diseases, mitochondrial diseases, spinal cord injury, central or psychostimulant addiction, senile dementia, circulatory disorders, cardiovascular disorders, hyperprolactinaemia or myopia. The compounds and/or compositions of the present invention can also be provided in the form of a pharmaceutical kit.

    专利号:RU-2024516-C1
    优先权日:1989-02-02
    标题:Method of synthesis of tetrahydrobenzimidazole derivative or its pharmaceutically acceptable salt

    专利号:RU-2002748-C1
    优先权日:1989-03-01
    标 题:Method of synthesis of 2,3,4,5-tetrahydro-5-methyl-2-[5- methyl-1h-imidazole- -4-yl) methyl]-1h-pyrido (4,3-b)-indole-1-one or ots salt

    专利号:RU-2017737-C1
    优先权日:1990-05-11
    标题 :Method of isoxazole derivatives synthesis

    专利号:RU-2001915-C1
    优先权日:1988-09-27
    标题:Method of pyridoindole derivatives or theirs salts synthesis

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    📌 第三方产品分析报告

    ✅ COA系统入驻 | 共享模式

    合成参考文献


    参考文献:10.1007/bf00171053
    摘要:Bard JA, Kucharewicz SA, Zgombick JM, Weinshank RL, Branchek TA, Cohen ML. Differences in ligand binding profiles between cloned rabbit and human 5-HT1D alpha and 5-HT1D beta receptors: ketanserin and methiothepin distinguish rabbit 5-HT1D receptor subtypes. Naunyn Schmiedebergs Arch Pharmacol. 1996 Aug;354(3):237–44. doi: 10.1007/bf00171053.
    参考文献:10.1016/s0306-3623(98)00235-3
    摘要:O’Gara BA, Illuzzi FA, Chung M, Portnoy AD, Fraga K, Frieman VB. Serotonin induces four pharmacologically separable contractile responses in the pharynx of the leech Hirudo medicinalis. General Pharmacology: The Vascular System. 1999 Jun;32(6):669–81. doi: 10.1016/s0306-3623(98)00235-3.
    参考文献:10.1016/s0022-3565(24)34967-5
    摘要:Zhou X, Galligan JJ. Synaptic Activation and Properties of 5-Hydroxytryptamine3 Receptors in Myenteric Neurons of Guinea Pig Intestine. The Journal of Pharmacology and Experimental Therapeutics. 1999 Aug;290(2):803–10. doi: 10.1016/s0022-3565(24)34967-5.
    参考文献:10.1002/nau.10043
    摘要:Ishizuka O, Gu B, Igawa Y, Nishizawa O, Pehrson R, Andersson KE. Role of supraspinal serotonin receptors for micturition in normal conscious rats. Neurourol Urodyn. 2002;21(3):225–30. doi: 10.1002/nau.10043.
    参考文献:10.1016/s0006-8993(02)02367-3
    摘要:Seo K, Fujiwara N, Hu JW, Cairns BE, Someya G. Intrathecal administration of 5-HT(3) receptor agonist modulates jaw muscle activity evoked by injection of mustard oil into the temporomandibular joint in the rat. Brain Res. 2002 May 03;934(2):157–61. doi: 10.1016/s0006-8993(02)02367-3.
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