Lead Optimization of Thiazolo [5, 4??c] piperidines: 3??Cyclobutoxy Linker as a Key Spacer for H3R Inverse Agonists

…, ML Delporte, T Demaude, V Durieu, M Gillard…

Index: Provins, Laurent; Denonne, Frederic; Celanire, Sylvain; Christophe, Bernard; Defays, Sabine; Delaunoy, Christel; Delporte, Marie-Laure; Demaude, Thierry; Durieu, Veronique; Gillard, Michel; Hubert, Delphine; Lamberty, Yves; Lorent, Genevieve; Valade, Anne; Vanbellinghen, Alain; Vanhoutvin, Nathalie ChemMedChem, 2012 , vol. 7, # 12 p. 2087 - 2092

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Abstract

The H3 histamine receptor (H3R) is a G protein-coupled receptor (GPCR) mainly expressed in the central nervous system (CNS) and a key modulatory site for several neurotransmitters. It acts as an autoreceptor on histaminergic neurons, inhibiting the release and synthesis of histamine, but it is also present as a heteroreceptor on other non-histaminergic neurons, where it modulates the release of neurotransmitters such as acetylcholine, dopamine or ...