Biochemical and behavioural characterization of EMPA, a novel high-affinity, selective antagonist for the OX(2) receptor.

@article{Malherbe2009BiochemicalAB,
  title={Biochemical and behavioural characterization of EMPA, a novel high-affinity, selective antagonist for the OX(2) receptor.},
  author={Pari Malherbe and Edilio Borroni and Luca B Gobbi and Henner Knust and Matthias H Nettekoven and Emmanuel Pinard and Olivier Roche and Mark Rogers-Evans and Joseph G. Wettstein and J Moreau},
  journal={British journal of pharmacology},
  year={2009},
  volume={156 8},
  pages={1326-41}
}
BACKGROUND AND PURPOSE The OX(2) receptor is a G-protein-coupled receptor that is abundantly found in the tuberomammillary nucleus, an important site for the regulation of the sleep-wake state. Herein, we describe the in vitro and in vivo properties of a selective OX(2) receptor antagonist, N-ethyl-2-[(6-methoxy-pyridin-3-yl)-(toluene-2-sulphonyl)-amino]-N-pyridin-3-ylmethyl-acetamide (EMPA). EXPERIMENTAL APPROACH The affinity of [(3)H]EMPA was assessed in membranes from HEK293-hOX(2)-cells… CONTINUE READING
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