Ken-ichi Otsuguro, Toshio Ohta, Shigeo Ito and Yoshikazu Nakazato (*)
Laboratory of Pharmacology, Graduate School of Veterinary Medicine, Hokkaido University, Sapporo 060-0818, Japan
(*) To whom correspondence should be addressed.
Abstract: Effects of purinoceptor antagonists on the relaxant responses to adenine nucleotides were examined to characterize the subtypes of P2-receptor in rat gastric circular muscle. In tissues contracted by acetylcholine, a P2-receptor antagonist, suramin (100 microM), inhibited the relaxant responses to ATP, adenosine 5'-O-(2-thiodiphosphate) (ADPbetaS) and alpha,beta-methylene ATP but not that to adenosine, while a P1-receptor antagonist, 8-phenyltheophylline (3 microM) did vice versa. The inhibitory effect of suramin was more potent for the relaxant responses to alpha,beta-methylene ATP than those to ATP or ADPbetaS. Pyridoxalphosphate-6-azophenyl-2',4'-disulphonic acid (PPADS) (3 - 30 microM) and 4,4'-diisothiocyanatostilbene-2,2'-disulphonate (DIDS) (30 and 1OO microM) inhibited the relaxation caused by alpha,beta-methylene ATP but not by ATP, ADPbetaS or adenosine. These results suggest that ATP and ADPbetaS cause relaxation via the classical P2Y receptors resistant to PPADS and DIDS. In addition, alpha,beta-methylene ATP causes relaxation via the distinct P2 receptors sensitive to PPADS and DIDS in rat gastric circular muscle.
Keywords: ATP, Purinoceptor, Suramin, PPADS, DIDS