CAS: 66711-21-5; Apraclonidine

该化合物是一种选择性的阿尔法-2肾上腺激动剂,主要用于眼科治疗,以降低青光眼等条件下的内压;其特点是能够减少水幽默生产和增加骨髓外流,从而减少内腔压力;该物质通常作为一种眼滴溶液施用;亚普拉克罗尼丁有相对较短的行动时间,并经常与其他药物一起使用,以提高功效;其化学结构包括替代的伊米达索林环,这对其药用活动至关重要;常见副作用可能包括眼刺激,口干口和疲劳,反映其系统吸收和...

结构式图片

欧盟法规

ECHA物质C&L通报

上下游产品

CAS号65936-26-7 N-(2,6-Dichloro... | CAS号73218-65-2 2,6-dichloro-1-... | CAS号81913-29-3 Clonidine 4-iso...

合成工艺路线路线简述

    📜2,6-二氯-4-硝基苯胺置于氯化亚砜,磺酰氯,Hydrazine Hydrate,5%-Palladium/activated Carbon,乙酸酐,三乙胺体系中,用 四氢呋喃,乙醇 作为反应溶剂,化学反应 21.41H,反应生成 阿可乐定
    参考文献:盐酸阿普乐定制备方法的改进
    标题:盐酸阿普乐定制备方法的改进
    摘要:青光眼是损害视神经并可能导致视力丧失的眼部疾病的总称.视神经损伤的主要原因是眼压(iop),除了...
    DOI:10.1080/00304948.2016.1206429

    海关参考信息

    专利信息


    专利号:US-2019374478-A1
    优先权日:2016-12-06
    标题:Ultrastable Gold Nanoparticles For Drug Delivery Applications And Synthesis Thereof
    发明人:BOISSELIER ÉLODIE; OUELLETTE MATHIEU; PERNET VINCENT; OMAR MAHMOUD
    权利人:UNIV LAVAL
    摘要:Herein presented are gold nanoparticles (AuNPs) used for the transport of medications to mucous membranes. The AuNPs are ultra-stable in that they withstand freeze-drying and heating treatments without noticeable change in their structure. In addition, they interact with mucous membranes, and therefore allow transport of certain drugs to these mucous membranes, allowing higher exposure time of the drugs, hence decreased dosing schedule of administration.

    专利号:US-6172066-B1
    优先权日:1996-05-16
    标 题:Dihydropyrimidines and uses thereof
    发明人:NAGARATHNAM DHANAPALAN; WONG WAI C; MIAO SHOU WU; PATANE MICHAEL A; GLUCHOWSKI CHARLES
    权利人:SYNAPTIC PHARMA CORP
    摘要:This invention is directed to dihydropyrimidine compounds which are selective antagonists for human α 1A receptors. This invention is also related to uses of these compounds for lowering intraocular pressure, inhibiting cholesterol synthesis, relaxing lower urinary tract tissue, the treatment of benign prostatic hyperplasia, impotency, cardiac arrhythmia and for the treatment of any disease where the antagonism of the α 1A receptor may be useful. The invention further provides a pharmaceutical composition comprising a therapeutically effective amount of the above-defined compounds and a pharmaceutically acceptable carrier.

    专利号:US-6228861-B1
    优先权日:1995-11-16
    标题 :Dihydropyrimidines and uses thereof
    发明人:NAGARATHNAM DHANAPALAN; WONG WAI C; MIAO SHOU WU; GLUCHOWSKI CHARLES; PATANE MICHAEL A
    权利人:SYNAPTIC PHARMA CORP
    摘要:This invention is directed to dihydropyrimidine compounds which are selective antagonists for human α 1A receptors. This invention is also related to uses of these compounds for lowering intraocular pressure, inhibiting cholesterol synthesis, relaxing lower urinary tract tissue, the treatment of benign prostatic hyperplasia, impotency, cardiac arrhythmia and for the treatment of any disease where the antagonism of the α 1A receptor may be useful. The invention further provides a pharmaceutical composition comprising a therapeutically effective amount of the above-defined compounds and a pharmaceutically acceptable carrier.

    专利号:US-6387909-B1
    优先权日:1999-07-30
    标 题 :Thienopyranecarboxamide derivatives
    发明人:LEONARDI AMEDEO; MOTTA GIANNI; RIVA CARLO; TESTA RODOLFO
    权利人:RECORDATI CHEM PHARM
    摘要:The invention relates to novel N-(substituted phenyl)-N'-[omega-(5-substituted-7-oxo-7H-thieno[3,2-b]pyran-3-carbonylamino)alkyl]piperazines their N-oxides and pharmaceutically acceptable salts thereof. The compounds are endowed with enhanced selectivity for alpha1-adrenergic receptors and a low activity in lowering blood pressure. The compounds are useful in the treatment of obstructive syndromes of the lower urinary tract, including benign prostatic hyperplasia (BPH), and in the treatment of lower urinary tract symptoms (LUTS) and neurogenic lower urinary tract dysfunction (NLUTD). The compounds are also useful in the treatment of excessive intraocular pressure, cardiac arrhythmia, erectile dysfunction, sexual dysfunction, and for inhibiting cholesterol synthesis or reducing sympathetically mediated pain.

    专利号:US-6245773-B1
    优先权日:1996-05-16
    标题:5-(heterocyclic alkyl)-6-aryl-dihydropyrimidines
    发明人:WONG WAI C; LAGU BHARAT; NAGARATHNAM DHANAPALAN; MARZABADI MOHAMMAD R; GLUCHOWSKI CHARLES
    权利人:SYNAPTIC PHARMA CORP
    摘要:This invention is directed to dihydropyrimidine compounds of the following formula: n which are selective antagonists for human α 1A receptors. This invention is also related to uses of these compounds for lowering intraocular pressure, inhibiting cholesterol synthesis, relaxing lower urinary tract tissue, the treatment of benign prostatic hyperplasia, impotency, cardiac arrhythmia and for the treatment of any disease where antagonism of the α 1A receptor may be useful. The invention further provides a pharmaceutical composition comprising a therapeutically effective amount of the above-defined compounds and a pharmaceutically acceptable carrier.

    专利号:US-2007148246-A1
    优先权日:2005-08-11
    标题:Nucleic Acid-Based Matrixes
    发明人:LUO DAN; LI YOUGEN
    权利人:LUO DAN; LI YOUGEN
    摘要:Various nucleic acid-based matrixes are provided, comprising nucleic acid monomers as building blocks, as well as nucleic acids encoding proteins, so as to produce novel biomaterials. Methods of utilizing such biomaterials include delivery of biologically active agents, cell and tissue culture, and cell-free protein synthesis.

    供应商参考报价(招募中)

    品牌试剂参考报价(招募中)

    📌 第三方产品分析报告

    ✅ COA系统入驻 | 共享模式

    主要参考文献


    1: Kauh CY, Bursztyn LL. Positive Apraclonidine Test in Horner Syndrome Caused by Thalamic Hemorrhage. J Neuroophthalmol. 2015 Sep;35(3):287-8. doi: 10.1097/WNO.0000000000000222. Japanese. doi: 10.1212/WNL.0b013e31821a4454. doi: 10.1097/WNO.0b013e31821a91fe.

    合成参考文献


    摘要:S76 | LUXPHARMA | Pharmaceuticals Marketed in Luxembourg | Pharmaceuticals marketed in Luxembourg, as published by d'Gesondheetskeess (CNS, la caisse nationale de sante, www.cns.lu), mapped by name to structures using CompTox by R. Singh et al. (2021) DOI:10.1021/acsenvironau.1c00008. List downloaded from
    摘要:Threlkeld AB, Assalian AA, Allingham RR, Shields MB. Apraclonidine 0.5% versus 1% for controlling intraocular pressure elevation after argon laser trabeculoplasty. Ophthalmic Surg Lasers. 1996 Aug;27(8):657–60.
    参考文献:10.2165/00128071-200203010-00007|10.2165/00128071-200203020-00006|10.2165/00128071-200203030-00008|10.2165/00128071-200203040-00007|10.2165/00128071-200203050-00008|10.2165/00128071-200203060-00007|10.2165/00128071-200203070-00009|10.2165/00128071-200203080-00010|10.2165/00128071-200203090-00006
    摘要:Cutaneous drug reaction case reports: from the world literature. Am J Clin Dermatol. 2002;3(9):637–43. doi: 10.2165/00128071-200203090-00006.
    参考文献:10.1159/000050886
    摘要:Avunduk AM, Sari A, Akyol N, Oztürk O, Kapicioglu Z, Erdöl H, Imamoglu HI. The one-month effects of topical betaxolol, dorzolamide and apraclonidine on ocular blood flow velocities in patients with newly diagnosed primary open-angle glaucoma. Ophthalmologica. 2001 Sep;215(5):361–5. doi: 10.1159/000050886.
    参考文献:10.1007/s00011-004-1259-z
    摘要:Szabó A, Farkas A, Vámos R, Bajor T, Hrabák A. The inhibition of retinal inducible nitric oxide synthase overexpression and the attenuation of experimental uveitis by anti-inflammatory drugs in rats. Inflamm Res. 2004 Jun;53(6):262–7. doi: 10.1007/s00011-004-1259-z.
    📝 需求与反馈
    尽可能描述清楚需求与问题信息
    ×

    通知