Ge. Knight et G. Burnstock, IDENTIFICATION OF PURINOCEPTORS IN THE ISOLATED STOMACH AND INTESTINEOF THE 3-SPINED STICKLEBACK GASTEROSTEUS-ACULEATUS L, Comparative biochemistry and physiology. C. Comparative pharmacologyand toxicology, 106(1), 1993, pp. 71-78
1. Adenine nucleosides and nucleotides were examined for pharmacologic
al activity in isolated stomach and intestine from the stickleback Gas
terosteus aculeatus L. 2. Adenosine and its stable analogues all conce
ntration-dependently relaxed carbachol-contracted stomach and intestin
e, with no significant difference in the potency of the analogues. Onl
y 8-(p-sulphophenyl) theophylline inhibited the relaxant response to a
denosine in both tissues; other adenosine antagonists such as 1,3-dipr
opyl-8-cyclopentylxanthine were not active. 3. ATP, alpha, beta-methyl
ene ATP (alpha,beta-MeATP) and 2-methylthio ATP (2-MeSATP) all caused
concentration-dependent contractions of the stomach and intestine. 4.
In the stomach, the order of potency was 2-MeSATP > alpha,beta-MeATP =
ATP; the P2Y-purinoceptor antagonist reactive blue 2 inhibited respon
ses to ATP. 5. In the intestine, the order of potency was alpha,beta-M
eATP > 2-MeSATP = ATP; reactive blue 2 did not affect responses to ATP
, nor did prolonged incubation with alpha,beta-MeATP. 6. It is conclud
ed that in both the stomach and intestine, adenosine is acting through
a non-specific or undifferentiated P1-purinoceptor. In the stomach, h
owever, the P2-purinoceptor appears to be analogous to the mammalian P
2Y-purinoceptor, and in the intestine, the receptor is more similar to
the mammalian P2X-subtype, although it was not susceptible to desensi
tization.