ZM241385 is an antagonist of the facilitatory responses produced by the A2A adenosine receptor agonists CGS21680 and HENECA in the rat hippocampus

British Journal of Pharmacology
R A CunhaJ A Ribeiro

Abstract

1. In the present study, we investigated the ability of a recently introduced non-xanthine A2A receptor antagonist, ZM241385 (4-(2-[7-amino-2-(2-furyl[1,2,4]-triazolo[2,3-a[1,3,5]triazin-5-yl -aminoethyl)phenol) to displace binding of the prototypical A2A adenosine receptor agonist [3H]CGS21680 (2-[4-(2-p-carboxyethyl)phenylamino]-5'-N-ethylcarboxamidoadenosine) and to modify the facilitatory responses caused by the A2A selective agonists, CGS21680 and HENECA (2-hexynl-5'-N-ethylcarboxamidoadenosine) in rat hippocampal preparations. 2. ZM241385 was nearly equipotent to displace [3H]CGS21680 (30 nM) binding to hippocampal (Ki of 0.52 nM) and to striatal membranes (Ki of 0.35 nM), whereas HENECA was a more potent displacer of [3H]CGS21680 binding to striatal (Ki of 4.5 nM) than to hippocampal membranes (Ki of 19 nM). 3. HENECA (3-30 nM) was equipotent with CGS21680 to facilitate veratridine-evoked [3H]acetylcholine release from superfused hippocampal synaptosomes and ZM241385 (20 nM) inhibited the facilitatory effects of both HENECA (30 nM) and CGS21680 (30 nM); this antagonism was mimicked by CSC (250 nM). 4. In contrast, CGS21680 (10-30 nM) was more potent than HENECA (10-30 nM) to facilitate synaptic transmission in Schaffer f...Continue Reading

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Citations

Sep 13, 2001·European Journal of Pharmacology·M R Nikbakht, T W Stone
Dec 1, 2001·European Journal of Pharmacology·V HarveyK Quirk
Dec 29, 1998·European Journal of Pharmacology·E M O'Kane, T W Stone
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Apr 13, 2000·Neuropharmacology·R A Cunha, J A Ribeiro
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Apr 22, 2014·Neuropharmacology·André Jerónimo-SantosMaria José Diógenes
Sep 8, 2007·Canadian Journal of Physiology and Pharmacology·Mohammad Ebrahim RezvaniMohammad Reza Palizvan
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Mar 3, 2018·Frontiers in Pharmacology·Estefanía MorenoVicent Casadó

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