[3H]BHDP as a novel and selective ligand for δ1 receptors in liver mitochondria and brain synaptosomes of the rat

Anis Klouz Jean-Paul Tillement 1 Marie-Françoise Boussard Michel Wierzbicki Vincent Berezowski 2 Roméo Cecchelli 2 Serge Labidalle Brigitte Onteniente Didier Morin 3
1 Laboratoire de Pharmacologie
2 LBHE - Laboratoire de Physiopathologie de la Barrière Hémato-Encéphalique
3 IMRB - Institut Mondor de Recherche Biomédicale
Abstract : The binding profile of [3H]BHDP [3H]N-benzyl-N'-(2-hydroxy-3,4-dimethoxybenzyl)-piperazine) was evaluated. [3H]BHDP labelled a single class of binding sites with high affinity (Kd = 2-3 nM) in rat liver mitochondria and synaptic membranes. The pharmacological characterization of these sites using δ reference compounds revealed that these sites are δ receptors and, more particularly, δ1 receptors. Indeed, BHDP inhibited [3H]pentazocine binding, a marker for δ1 receptors, with high affinity in a competitive manner. BHDP is selective for δ1 receptors since it did not show any relevant affinity for most of the other receptors, ion channels or transporters tested. Moreover, in an in vitro model of cellular hypoxia, BHDP prevented the fall in adenosine triphosphate (ATP) levels caused by 24 h hypoxia in cultured astrocytes. Taken together, these results demonstrate that [3H]BHDP is a potent and selective ligand for δ1 receptors showing cytoprotective effects in astrocytes.
Keywords : δ Receptor Liver mitochondrion Synaptosome Binding Hypoxia Astrocyte
Type de document :
Article dans une revue
FEBS Letters, Wiley, 2003, 553, p. 157-162
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https://hal-univ-artois.archives-ouvertes.fr/hal-00537718
Contributeur : Wilfried Déplanques <>
Soumis le : vendredi 19 novembre 2010 - 09:49:14
Dernière modification le : mercredi 25 juillet 2018 - 10:52:02

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Anis Klouz, Jean-Paul Tillement, Marie-Françoise Boussard, Michel Wierzbicki, Vincent Berezowski, et al.. [3H]BHDP as a novel and selective ligand for δ1 receptors in liver mitochondria and brain synaptosomes of the rat. FEBS Letters, Wiley, 2003, 553, p. 157-162. 〈hal-00537718〉

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