85-79-0
85-79-0 結(jié)構(gòu)式
基本信息
地布卡因
辛可卡因
辛可(地布)卡因
2-BUTOXY-N-[2-(DIETHYLAMINO)ETHYL]CINCHONAMIDE
2-butoxy-n-(2-diethylaminoethyl)quinoline-4-carboxamide
A-BUTOXYCINCHONINIC ACID DIETHYLETHYLENEDIAMIDE
CINCHOCAINE
DIBUCAINE
DIBUCAINE BASE
2-butoxy-n-(2-(diethylamino)ethyl)-4-quinolinecarboxamid
2-butoxy-n-(2-(diethylamino)ethyl)-cinchoninamid
2-butoxy-n-(2-(diethylamino)ethyl)cinchoninamide
2-butoxy-n-(2-(diethylamino)ethyl-4-quinolinecarboxamid
2-Butoxy-N-(beta-diethylaminoethyl)cinchoninamide
2-Butoxy-N-[2-(diethylamino)ethyl]cinchoninamide
2-Butoxyquinoline-4-carboxylic acid diethylaminoethylamide
2-butoxyquinoline-4-carboxylicaciddiethylaminoethylamide
2-n-butoxy-n-(2-diethylaminoethyl)cinchoninamide
4-Quinolinecarboxamide, 2-butoxy-N-[2-(diethylamino)ethyl]-
alpha-butyloxycinchonicacid-gamma-diethylethylenediamine
alpha-Butyloxycinchoninic acid diethylethylenediamide
alpha-butyloxycinchoninicaciddiethylethylenediamide
物理化學(xué)性質(zhì)
安全數(shù)據(jù)
常見(jiàn)問(wèn)題列表
辛可卡因主要適用于硬膜外麻醉以及腰麻。本品容易通過(guò)粘膜，也用于表面麻醉，但因其毒性過(guò)大（約比普魯卡因高15倍），較少用于浸潤(rùn)麻醉。
1、2-氯-N-[2-(二乙基氨基)乙基]-4-喹啉甲酰胺的合成
室溫下向3000ml三口瓶中加入2-羥基-4-喹啉羧酸200g，甲苯1500ml攪拌下滴加氯化亞砜158g，升溫至75℃反應(yīng)2小時(shí)，降溫至25℃，減壓濃縮，再加500ml甲苯，繼續(xù)減壓濃縮至干，直接加入2000ml甲苯稀釋后加入到5000ml三口瓶中，再加入N,N－二乙基二乙胺100g，升溫70℃攪拌，反應(yīng)完全后降至室溫，加水?dāng)嚢?0分鐘，分液，有機(jī)層用水洗兩次，飽和食鹽水洗滌一次，無(wú)水硫酸鈉干燥，過(guò)濾，濾液旋干，得2-氯-N-[2-(二乙基氨基)乙基]-4-喹啉甲酰胺即辛可酰胺274g，收率85％。
2.辛可卡因的合成
將200g辛可酰胺，550ml正丁醇和300g正丁醇鈉加入至3000ml反應(yīng)瓶中，逐漸升溫至回流3小時(shí)后，降溫至室溫，加入純化水1000ml，攪拌30分鐘，靜止分層30min，將水層棄去，有機(jī)層加入無(wú)水硫酸鈉干燥，過(guò)濾，濾液減壓濃縮，然后加入500ml甲苯并升溫至60℃攪拌30min，靜置，分層，上層甲苯層降溫析晶，得辛可卡因精制品146g，收率65％,純度為99.7％。
Dibucaine (Cinchocaine) reduces the degradation of BSA-gold complex in the reservosomes, which was not caused either by an inhibition of the whole proteolytic activity of the parasite or by a reduction on the expression levels of cruzipain. Dibucaine, a quaternary ammonium compound, inhibited SChE to a minimum within 2 min in a reversible manner. The inhibition was very potent. It had an IC(50) of 5.3 microM with BuTch or 3.8 microM with AcTch. The inhibition was competitive with respect to BuTch with a K(i) of 1.3 microM and a linear-mixed type (competitive/noncompetitive) with respect to AcTch with inhibition constants, K(i) and K(I) of 0.66 and 2.5 microM, respectively. Dibucaine possesses a butoxy side chain that is similar to the butryl group of BuTch and longer by an ethylene group from AcTch.