Functional models for the dopamine D3 receptor N. Griffon*II, F. Sautel*, C. Pilon*, D. Levesque*, P. SokolofP, 1.-C. Schwartz*, J. Diazt, P. Simon*, J. Costentin*, A. Mann§ and C. G. Wermuthg *Unite de Neurobiologie et Pharrnacologie, Centre Paul Broca de I'INSERM, Paris, France, tLaboratoire de Physiologie, Universite Rene Descarte, Paris, France, SLaboratoire de Pharrnacologie et Physiologie...

The construct of impulsivity is considered as a major trait of personality. There is growing evidence that the mesolimbic dopamine system plays an important role in the modulation of impulsivity and venturesomeness, the two key components within the impulsivity-construct. The aim of the present study was to explore an association between trait impulsivity measured with self-assessment and the d...

•Structures of dopamine receptor D3R with agonists pramipexole and PD128907•Different binding modes similar pharmacological properties to D3R•Conformational changes associated activation selective G protein coupling•Selective mechanism versus D2R D4R The system, including five receptors (D1R–D5R), plays essential roles in the central nervous system (CNS), ligands that activate have been used tr...

During last 15 years dopamine has emerged as a major regulator of inflammation. All five dopamine receptors (DRs, DRD1-DRD5) have been found to be expressed in immune cells where they exert a complex regulation of immunity [1]. Of note, DRs have been found not only in cells of the adaptive immune system, but also in cells belonging to the innate immunity, even including glial cells. The outcome...

BACKGROUND Antipsychotics are divided into typical and atypical compounds based on clinical efficacy and side effects. The purpose of this study was to characterize in vitro a series of novel azecine-type compounds at human dopamine D1-D5 and 5HT2A receptors and to assign them to different classes according to their dopamine/5HT2A receptor profile. RESULTS Regardless of using affinity data (p...

A specific role for the dopamine D3 receptor in behavior has yet to be elucidated. We now report that dopamine D2/D3 agonists elicit dose-dependent yawning behavior in rats, resulting in an inverted U-shaped dose-response curve. A series of experiments was directed toward the hypothesis that the induction of yawning is a D3 receptor-mediated effect, whereas the inhibition of the yawning observe...