The adenosine receptor agonist, APNEA, increases calcium influx into rat cortical synaptosomes through N-type channels associated with A2a receptors.

Abstract	N6-2-(4-aminophenyl)ethyladenosine (APNEA) is a nonselective adenosine receptor agonist known to have a high affinity for the adenosine A1 and A3 receptors. It was found to be able to dose-dependently increase the sustained (4 min) Ca2+ influx into rat cortical synaptosomes while 2-chloro-N6-(3-iodobenzyl)-adenosine-5-N-methyluronamide (Cl-IB-MECA), a selective A3 agonist has no effect. However, this effect of APNEA was not affected by the presence of 8-cyclopentyl-1,3-dimethylxanthine (CPT), a selective A1 antagonist; but instead completely abolished by 8-(3-chlorostyryl)caffeine (CSC), a selective A2a antagonist, or omega-conotoxin GVIA. These results show that in the rat cortex, presynaptic A2a receptors can mediate neurotransmitter release by increasing Ca2+ influx through the N-type calcium channels. A1 and A3 receptors appear not to be involved.
Authors	S N Li, P T Wong
Journal	Neurochemical research (Neurochem Res) Vol. 25 Issue 4 Pg. 457-9 (Apr 2000) ISSN: 0364-3190 [Print] United States
PMID	10823578 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
Chemical References	1,3-dimethyl-8-cyclopentylxanthine Calcium Channel Blockers Calcium Channels, N-Type N(6)-2-(4-aminophenyl)ethyladenosine Purinergic P1 Receptor Agonists Purinergic P1 Receptor Antagonists Receptor, Adenosine A2A Receptor, Adenosine A3 Receptors, Purinergic P1 Xanthines 8-(3-chlorostyryl)caffeine Caffeine omega-Conotoxin GVIA Adenosine Calcium 2-chloro-N(6)-(3-iodobenzyl)adenosine-5'-N-methyluronamide
Topics	Adenosine (analogs & derivatives, pharmacology) Animals Brain Chemistry Caffeine (analogs & derivatives, pharmacology) Calcium (metabolism) Calcium Channel Blockers (pharmacology) Calcium Channels, N-Type (drug effects, metabolism) Cerebral Cortex (chemistry, drug effects, metabolism) Dose-Response Relationship, Drug Male Purinergic P1 Receptor Agonists Purinergic P1 Receptor Antagonists Rats Rats, Sprague-Dawley Receptor, Adenosine A2A Receptor, Adenosine A3 Receptors, Purinergic P1 (metabolism) Synaptosomes (drug effects, metabolism) Xanthines (pharmacology) omega-Conotoxin GVIA (pharmacology)

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