Collis M G, Palmer D B, Saville V L
J Pharm Pharmacol. 1985 Apr;37(4):278-80. doi: 10.1111/j.2042-7158.1985.tb05063.x.
The potency of 8-phenyltheophylline as an antagonist at A1 adenosine receptors in guinea-pig atria and at A2 adenosine receptors in the guinea-pig aorta has been investigated. 8-Phenyltheophylline was an apparently competitive antagonist of the negative chronotropic effect of adenosine, 2-chloroadenosine, L-N6-phenyl-isopropyl adenosine (L-PIA) and 5'-N-ethylcarboxamide adenosine (NECA) on atria and of the relaxant effect of adenosine, 2-chloroadenosine and NECA on the aorta. The pA2 values for 8-phenyltheophylline ranged from 6.4 to 6.6 and were not significantly different, irrespective of the agonist or tissue used. These results indicate that 8-phenyltheophylline is a relatively potent antagonist at adenosine receptors but does not exhibit selectivity for either of the putative sub-types in isolated tissues.
研究了8-苯基茶碱对豚鼠心房A1腺苷受体和豚鼠主动脉A2腺苷受体的拮抗作用。8-苯基茶碱是腺苷、2-氯腺苷、L-N6-苯基异丙基腺苷（L-PIA）和5'-N-乙基羧酰胺腺苷（NECA）对心房负性变时作用以及腺苷、2-氯腺苷和NECA对主动脉舒张作用的明显竞争性拮抗剂。8-苯基茶碱的pA2值在6.4至6.6之间，无论使用何种激动剂或组织，均无显著差异。这些结果表明，8-苯基茶碱是腺苷受体的相对强效拮抗剂，但对分离组织中的任何一种假定亚型均无选择性。
