Raberger G, Schütz W, Kraupp O
Arch Int Pharmacodyn Ther. 1977 Nov;230(1):140-9.
The coronary dilatory action of 23 adenosine analogues was investigated on a comparative basis after i.v. administration in anaesthetized dogs. Substitution of adenosine in position 5' with a COOH group and esterification led to a 50- to 100-fold increase in coronary efficacy (flow increase integrated over the time of action). Amidation of the carboxylic acid analogue further enhanced the coronary efficacy. The most effective analogue, adenosine-5'-ethyl-carboxamide, showed 20000 times greater activity than adenosine. Additional substitution in positions 2' and 3' with NO2, O-methoxy-methyliden or O-methoxyethyliden resulted in a delayed onset and prolonged duration of action.
在麻醉犬静脉注射后，对23种腺苷类似物的冠状动脉扩张作用进行了比较研究。腺苷5'位被COOH基团取代并酯化后，冠状动脉效能（作用时间内流量增加的积分）提高了50至100倍。羧酸类似物的酰胺化进一步增强了冠状动脉效能。最有效的类似物腺苷-5'-乙基-羧酰胺的活性比腺苷高20000倍。在2'和3'位额外用NO2、O-甲氧基-亚甲基或O-甲氧基乙基取代会导致起效延迟和作用持续时间延长。
