📜2-氯-2,3-O-异亚丙基腺苷酸-5-N-乙基羧酰胺置于盐酸体系中,化学反应 4.0H,反应生成3-{4-[2-({6-氨基-9-[(2R,3R,4S,5S)-5-(乙基氨基甲酰)-3,4-二羟基四氢-2-呋喃基]-9H-嘌呤-2-基}氨基)乙基]苯基}丙酸盐酸盐(1:1)
参考文献:2-(Arylalkylamino)Adenosin-5'-Uronamides: A New Class Of Highly Selective Adenosine A2 Receptor Ligands
标题:2-(Arylalkylamino)Adenosin-5'-Uronamides: A New Class Of Highly Selective Adenosine A2 Receptor Ligands
摘要:The Synthesis And Receptor-Binding Profiles At Adenosine Receptor Subtypes For A Series Of 2-(Arylalkylamino)-Adenosin-5'-Uronamides Is Described. Halogenated 2-Phenethylamino Analogues Such As 3E Show Greater Than 200-Fold Selectivity For The A2 Receptor Subtype On The Basis Of Rat Brain Receptor Binding. The General Structure-Activity Relationship Of This Series Of Compounds Is Discussed Both In Terms Of Potency At A2 Receptors As Well As Receptor Subtype Selectivity. It Is Possible To Introduce A Hydrophilic Carboxyalkyl Substituent To This Series Such As In Cgs 21680A (3H) And Still Retain Good Potency And Selectivity For A2 Receptors. In Addition,Functional Data In A Perfused Working Rat Heart Model Shows That These Compounds Possess Full Agonist Properties At A2 Receptors With 3H Having A Greater Than 1500-Fold Separation Between A2 (Coronary Vasodilatory) And A1 (Negative Chronotropic) Receptor Mediated Events.
Doi:10.1021/jm00169A015