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    標題: N6-Substituted Adenosine Derivatives Ⅱ: Radioprotection and Pharmacological Actions of 6-Diethyladenosine, 6-( 1-Hydroxymethylpropyl) adenosine and 6-Carboethoxymethyladenosine
    N6-置換腺嘌呤核苷衍生物Ⅱ
    作者: Yang, Meei Shieu
    Ho, Shien Tsong
    Lee, Kong Ko
    貢獻者: 私立嘉南藥學專科學校
    日期: 1980
    上傳時間: 2013-12-19 11:33:53 (UTC+8)
    摘要: Since colloidal sulfur and thiourea were showed to possess activity against the damaging effects of ionizing radiation by X-rays , the redioprotective action of a number of substances such as thioglycolic acid, glutathione, tryptophane, cysteine and cystine ,cyanide, 2-mercaptopropylguanidine4, EDAT5 had been achieved. Histamine6, serotonin, dopa8, catecholamine and morphine derivatives, were believed to be radioprotective by causing pharmacological changes. Other compounds that altered the ability of hemoglobin to transport oxygen and showed radioprotective action included sodium nitrite, aniline and some of its derivatives and carbon monoxide.
    In adenosine dervatives, a series of 6-(2-hydroxyethyl)-adenosine, 6-(2-aminoethyl) adenosine, 6-(3-hydroxypropyl) adenosine, 6-(2-hydroxypropyl) adenosine, 6-(2-aminopropyl) adensine and 6-(2-mercaptoethyl) adenosine were active in protecting animals against radiation as well as in lowering blood pressure and pulse rate. In order to analyze the effect of adenosine derivatives and to study the relationship between the chemical structure and biological activities, 6-diethyladenosine (compound 7), 6-(1-hydroxymethylproptl) adenosine (compound 8) and 6-carboethoxymethyladenosine (compound 9) were preared. The evaluation of radioprotection of these compounds had been carried out on whole body irradiation of mice with lethal dose of Co gamma-ray from an external source.
    The pharmacological properties of these compounds wrer studied in an attempt to obtain information on relationship between radioprotection and cardiovascular depression.
    探討N6—置換腺嘌呤核苷之三種衍生物即6-二乙基腺嘌呤核苷(6-diethyladenosine,化合物7),6-(1-羥甲丙基) 腺嘌呤核苷 〔6-(1-hydroxymethylpropyl) adenosine,化合物8〕及6-羧乙氧甲基腺嘌呤核苷(6-Carboethoxymethyl adenosine,化合物9)的放射線防護作用和藥理作用。
    這些化合物均造成抑制心臟作用及血壓降下作用同時具有放射線防護效果。化合物7、8及9分別均能引起大白鼠血壓下降,心跳減慢。呼吸速率先短暫的增加之後降低。大白鼠心電圖的紀錄,顯示出這些化合物會引起心跳減慢,P波降下,消失或反轉及PR間距縮短。對兔子及大白鼠的離體心臟,這三種化合物均首先造成暫時性輕微的收縮力加大隨後產生負的收縮能作用(negative inotropic effect )及負的變時性作用(negative chrotropic effect)。在這些化合物中,化合物8具有最強的心臟抑制作用及血壓降下作用同時其放射線防護作用也最強。而化合物7的作用最弱。腺嘌呤核苷衍生物使血壓下降的可能機序及構造與活性之間的相關關係也一併列在此篇討論之。
    關聯: 嘉南學報 6 : (轉載論文) A21-A31
    台灣藥學雜誌第30卷第2期 (1978)
    Appears in Collections:[嘉南學報] 6期 (1980)
    [藥學系(所)] 期刊論文

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