Katsuragi T, Su C
Br J Pharmacol. 1981 Nov;74(3):709-13. doi: 10.1111/j.1476-5381.1981.tb10482.x.
1 The effect of clonidine on the 3H-purine release evoked by KCl or (-)-adrenaline was assessed in the superfused helical strip of the rabbit pulmonary artery pretreated with [3H]-adenosine. 2 Clonidine (3 x 10(-5) M to 10(-4) M) significantly enhanced the 3H-purine efflux evoked by 50 mM KCl but not by 3 x 10(-6) M) (-)-adrenaline. 3 This facilitatory effect of clonidine on the KCl-induced purine release was unaltered by phentolamine 3 x 10(-6) M. It was absent in arterial segments denervated with 6-hydroxydopamine 30 microgram/ml. 4 A sustained contractile response was evoked by clonidine 3 x 10(-5) M without an increase in the 3H-purine efflux. This was significantly reduced by phentolamine 3 x 10(-6) M, but not by yohimbine 10(-5) M or by denervation with 6-hydroxydopamine. 5 The uptake of [3H]-adenosine into the segments was not inhibited by clonidine 3 x 10(-5) M. 6 It is suggested that the facilitation by clonidine of the KCl-induced purine release is due to prevention of presynaptic autoinhibition of purine release from adrenergic nerves, by an antiadenosine action of the drug.
在用[3H] - 腺苷预处理的兔肺动脉螺旋条上,评估可乐定对由氯化钾或(-) - 肾上腺素诱发的3H - 嘌呤释放的影响。
可乐定(3×10(-5)M至10(-4)M)显著增强了由50 mM氯化钾诱发的3H - 嘌呤流出,但对3×10(-6)M(-) - 肾上腺素诱发的流出无影响。
3×10(-6)M酚妥拉明不改变可乐定对氯化钾诱导的嘌呤释放的促进作用。在以30微克/毫升6 - 羟基多巴胺去神经支配的动脉节段中,该作用不存在。
3×10(-5)M可乐定诱发持续的收缩反应,但3H - 嘌呤流出未增加。这被3×10(-6)M酚妥拉明显著降低,但未被10(-5)M育亨宾或6 - 羟基多巴胺去神经支配降低。
3×10(-5)M可乐定不抑制[3H] - 腺苷向节段中的摄取。
提示可乐定对氯化钾诱导的嘌呤释放的促进作用是由于该药物的抗腺苷作用,防止了肾上腺素能神经嘌呤释放的突触前自身抑制。