Gonçalves M L, Ribeiro J A
Laboratory of Pharmacology, Gulbenkian Institute of Science, Oeiras, Portugal.
Fundam Clin Pharmacol. 1987;1(3):169-78. doi: 10.1111/j.1472-8206.1987.tb00556.x.
Effects of adenosine triphosphate (ATP), adenosine diphosphate (ADP), adenosine monophosphate (AMP), and adenosine on the antihaemolytic action of procaine, and the effect of ATP on the antihaemolytic actions of lidocaine, dibucaine, tetracaine, pentobarbitone, and chlorpromazine were investigated in rat erythrocytes. The effects of adenosine and its analogues D-N6-phenylisopropyladenosine (D-PIA), L-N6-phenylisopropyladenosine (L-PIA), N6-cyclohexyladenosine (CHA), 2-chloroadenosine, and N6-methyladenosine, as well as the effects of cyclic-AMP (cAMP), dibutyryl cAMP, and forskolin on haemolysis were also investigated in rat erythrocytes. ATP, ADP, and AMP, but not adenosine, antagonized in a concentration-dependent manner the antihaemolytic action of procaine, and ATP was ineffective against the antihaemolytic actions of lidocaine, dibucaine, tetracaine, pentobarbitone, and chlorpromazine. Adenosine and its analogues, but not N6-methyladenosine, protected erythrocytes against hypotonic haemolysis in a concentration-dependent manner. The order of potencies was: D-PIA greater than CHA greater than L-PIA greater than adenosine greater than 2-chloroadenosine. The effect of adenosine on haemolysis was not prevented by theophylline, 8-phenyltheophylline, or 8-sulfophenyltheophylline. Dibutyryl cAMP, a stable analogue of cAMP, and forskolin, a specific activator of adenylate cyclase, mimicked the antihaemolytic action of adenosine. cAMP was less efficient than adenosine. Adenine nucleotides antagonized the antihaemolytic action of procaine, probably due to calcium-chelating properties. In contrast, adenine nucleosides have antihaemolytic properties. The possibility that the antihaemolytic effects of these substances relate to cAMP and/or to lipophilicity is discussed.
在大鼠红细胞中研究了三磷酸腺苷（ATP）、二磷酸腺苷（ADP）、一磷酸腺苷（AMP）和腺苷对普鲁卡因抗溶血作用的影响，以及ATP对利多卡因、丁卡因、丁哌卡因、戊巴比妥和氯丙嗪抗溶血作用的影响。还研究了腺苷及其类似物D-N6-苯异丙基腺苷（D-PIA）、L-N6-苯异丙基腺苷（L-PIA）、N6-环己基腺苷（CHA）、2-氯腺苷和N6-甲基腺苷，以及环磷酸腺苷（cAMP）、二丁酰环磷腺苷（dibutyryl cAMP）和福斯可林对溶血的影响。ATP、ADP和AMP，但不是腺苷，以浓度依赖的方式拮抗普鲁卡因的抗溶血作用，并且ATP对利多卡因、丁卡因、丁哌卡因、戊巴比妥和氯丙嗪的抗溶血作用无效。腺苷及其类似物，但不是N6-甲基腺苷，以浓度依赖的方式保护红细胞免受低渗溶血。效力顺序为：D-PIA＞CHA＞L-PIA＞腺苷＞2-氯腺苷。茶碱、8-苯基茶碱或8-磺基苯基茶碱不能阻止腺苷对溶血的影响。二丁酰环磷腺苷，一种cAMP的稳定类似物，和福斯可林，一种腺苷酸环化酶的特异性激活剂，模拟了腺苷的抗溶血作用。cAMP的效率低于腺苷。嘌呤核苷酸拮抗普鲁卡因的抗溶血作用，可能是由于其钙螯合特性。相反，嘌呤核苷具有抗溶血特性。讨论了这些物质的抗溶血作用与cAMP和/或亲脂性相关的可能性。
