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Adenosine‐5′‐O‐(2‐thiodiphosphate) is a potent agonist at P 2 purinoceptors mediating insulin secretion from perfused rat pancreas
Author(s) -
Bertrand G.,
Chapal J.,
Puech R.,
LoubatièresMariani M.M.
Publication year - 1991
Publication title -
british journal of pharmacology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 2.432
H-Index - 211
eISSN - 1476-5381
pISSN - 0007-1188
DOI - 10.1111/j.1476-5381.1991.tb12223.x
Subject(s) - medicine , endocrinology , adenosine , purinergic receptor , insulin , agonist , biology , adenosine diphosphate , secretion , adenosine triphosphate , chemistry , receptor , platelet , platelet aggregation
1 The effects of a P 2 purinoceptor agonist, adenosine 5′‐O‐(2‐thiodiphosphate) (ADP‐β‐S) have been studied on insulin secretion and flow rate of the isolated perfused pancreas of the rat. 2 In the presence of a moderately stimulating glucose concentration (8.3 m m ), ADP‐/7‐S (4.95–495 n m ) evoked a biphasic insulin response in a concentration‐dependent manner. A comparison of relative potency between ADP‐β‐S and adenosine 5′‐triphosphate (ATP) showed that ADP‐β‐S was 100 times more potent than ATP. On the other hand, in the presence of a non stimulatory glucose concentration (4.2 m m ), ADP‐β‐S (165 n m ) did not modify the basal insulin secretion. 3 ADP‐β‐S, at concentrations effective on insulin secretion and also at higher concentrations (1.65 and 16.5 μ m ), provoked an increase of the pancreatic flow rate in a concentration‐dependent manner. 4 Our results show that ADP‐β‐S is a potent insulin secretory P 2 purinoceptor agonist. As it is resistant to hydrolysis it might be useful in studying the effect of activation of the P 2 purinoceptor of β cells on insulin secretion in vivo .