Todorov L D, Bjur R A, Westfall D P
Department of Pharmacology, University of Nevada School of Medicine, Reno.
J Pharmacol Exp Ther. 1994 Feb;268(2):985-9.
The effects of several purinoceptor agonists and antagonists on norepinephrine overflow were examined in the electrically field stimulated vas deferens and saphenous artery of the rabbit. Both the adenine nucleotides ATP and beta,gamma-methylene ATP and the adenine nucleosides adenosine and 2-chloroadenosine reduced the electrical field stimulation-evoked release of norepinephrine from the in vitro vas deferens. These responses are antagonized by both 8-(p-sulfophenyl)-theophylline and alpha,beta-methylene ATP, indicating that this effect is mediated by P3-receptors. Interestingly, the nucleotide and nucleoside agonists facilitated, rather than inhibited, the electrical field stimulation-evoked release of norepinephrine from the in vitro perfused saphenous artery. This facilitation was antagonized by 8-(p-sulfophenyl)-theophylline but not by alpha,beta-methylene ATP. These results indicate that there may be facilitatory prejunctional purinoceptors that exhibit structure-activity relationships similar to, but perhaps not identical to, those exhibited by inhibitory prejunctional purinoceptors.
在兔的电场刺激输精管和隐动脉中,研究了几种嘌呤受体激动剂和拮抗剂对去甲肾上腺素溢出的影响。腺嘌呤核苷酸ATP和β,γ-亚甲基ATP以及腺嘌呤核苷腺苷和2-氯腺苷均降低了体外输精管中电场刺激诱发的去甲肾上腺素释放。这些反应被8-(对磺苯基)茶碱和α,β-亚甲基ATP拮抗,表明这种作用是由P3受体介导的。有趣的是,核苷酸和核苷激动剂促进而非抑制体外灌注隐动脉中电场刺激诱发的去甲肾上腺素释放。这种促进作用被8-(对磺苯基)茶碱拮抗,但不被α,β-亚甲基ATP拮抗。这些结果表明,可能存在促进性的节前嘌呤受体,其结构-活性关系与抑制性节前嘌呤受体相似,但可能不完全相同。