本文關(guān)鍵詞：以藥物化學(xué)方法研發(fā)的首創(chuàng)藥物蘇沃雷生　出處：《藥學(xué)學(xué)報(bào)》2016年12期 　論文類型：期刊論文

  更多相關(guān)文章： 結(jié)構(gòu)變換 食欲素 活性化合物 新藥創(chuàng)制 構(gòu)效關(guān)系 技術(shù)創(chuàng)造 醫(yī)療效果 智力活動(dòng) 新藥研究 研發(fā)者

【摘要】：新藥創(chuàng)制是復(fù)雜的智力活動(dòng),涉及科學(xué)研究、技術(shù)創(chuàng)造、產(chǎn)品開發(fā)和醫(yī)療效果等多維科技活動(dòng)。每個(gè)藥物都有自身的研發(fā)軌跡,而構(gòu)建化學(xué)結(jié)構(gòu)是最重要的環(huán)節(jié),因?yàn)樗w了藥效、藥代、安全性和生物藥劑學(xué)等性質(zhì)。本欄目以藥物化學(xué)視角,對(duì)有代表性的藥物的成功構(gòu)建,加以剖析和解讀。2014年上市的蘇沃雷生,無論在策略上還是實(shí)施上都是一個(gè)"摸著石頭過河"的原創(chuàng)性藥物的研發(fā)實(shí)例�；谂潴w-受體的生物功能研制藥物往往因多重生理功能而改變研究方向和目標(biāo),以多肽食欲素-受體為靶標(biāo)的新藥研究由減肥藥轉(zhuǎn)向?yàn)榇呙咚?乃至研制成功,就是一個(gè)范例。從300萬個(gè)化合物隨機(jī)篩選出苗頭化合物,到用藥物化學(xué)方法和分析構(gòu)效關(guān)系作結(jié)構(gòu)變換,在活性方面,要對(duì)雙靶標(biāo)有相同(近)的活性,在受體的分子水平和功能的細(xì)胞水平上優(yōu)化出高活性化合物,并對(duì)實(shí)驗(yàn)動(dòng)物的睡眠/覺醒有良好的調(diào)節(jié)作用。在成藥性上,吸收性、代謝性、安全性等多方面的一步步優(yōu)化,顯示出研發(fā)者的學(xué)術(shù)嚴(yán)謹(jǐn)性和技術(shù)嫻熟性。全新的靶標(biāo)和首創(chuàng)的藥物在實(shí)驗(yàn)室、臨床和市場(chǎng)曾經(jīng)并繼續(xù)受到審視,因?yàn)橐粋�(gè)藥物靶標(biāo)的確證還要到"真實(shí)世界"大范圍考量。
[Abstract]:Drug discovery is a complicated intellectual activity, involving scientific research, technology creation, product development and effect of multi-dimensional medical science and technology activities. Each drug has its own development trajectory and the construction of chemical structure, is the most important link, because it covers the pharmacodynamics, pharmacokinetics, safety and biopharmaceutical properties. In this column from the perspective of medicinal chemistry, the representative drug is successfully constructed to analyze and interpret the.2014 listed suvo Lei, both in strategy and implementation are the original drug a "stones" research examples. The biological function of the ligand receptor drugs often due to multiple physiological function change the research direction and goal based on the orexin receptor peptide to study drug targets by weight-loss drug to hypnotic, and even developed, is a good example. From 3 million randomly selected compounds Signs of compounds, to pharmaceutical chemistry and structure-activity relationship analysis method for structural transformation, in terms of activity, to be marked with the same double target (near) activity at the molecular level and the function of the receptor on the cell level optimization of high active compounds, and the experimental animal sleep / wake have the good effect. In medicine, absorption, metabolism and many other aspects of security step by step optimization, showing the academic rigor and a skilled R & D researchers. The new target and the first drug in the laboratory, clinical and market have been and continue to be scrutinized, as confirmed a drug target but also to the real world "a wide range of considerations.

【作者單位】： 中國(guó)醫(yī)學(xué)科學(xué)院 北京協(xié)和醫(yī)學(xué)院藥物研究所;
【分類號(hào)】：R914
【正文快照】： 1 背景 1998年美國(guó)霍華德休斯醫(yī)學(xué)研究中心(HHMI)發(fā)現(xiàn)了一種肽類神經(jīng)遞質(zhì),命名為下視丘泌素(hypocretin)(De Lecea L,Kilduff TS,Peyron C,et al.Proc Natl Acad Sci U S A,1998,95:322-327),是源于在下丘腦(hypothalamus)發(fā)現(xiàn)了特異性的mR NA。同年Scrips研究所也獨(dú)立發(fā)現(xiàn)了

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