Functional models for the dopamine D3 receptor.
نویسندگان
چکیده
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, UER de Medecine et de Pharrnacie, Saint-Etienne du Rouvray, France, and SLaboratoire de Pharrnacologie Moleculaire, Centre de Neurochirnie, Strasbourg, France I93
منابع مشابه
P139: Role of Dopamine Receptor D3 in Depression and Anxiety
Dopamine (DA) is one of the main catecholamines in the brain and is crucial for movement coordination, endocrine function, reward, mood, memory and emotions. The dopaminergic system is the primary therapeutic target in the treatment of Parkinson’s disease (PD), drug addiction and schizophrenia. Notwithstanding, dysfunction of central dopaminergic neurotransmission has also been associated to de...
متن کاملTranylcypromine Substituted cis-Hydroxycyclobutylnaphthamides as Potent and Selective Dopamine D3 Receptor Antagonists
We report a class of potent and selective dopamine D3 receptor antagonists based upon tranylcypromine. Although tranylcypromine has a low affinity for the rat D3 receptor (K(i) = 12.8 μM), our efforts have yielded (1R,2S)-11 (CJ-1882), which has K(i) values of 2.7 and 2.8 nM at the rat and human dopamine D3 receptors, respectively, and displays respective selectivities of >10000-fold and 223-fo...
متن کاملNeurovascular coupling to D2/D3 dopamine receptor occupancy using simultaneous PET/functional MRI.
This study employed simultaneous neuroimaging with positron emission tomography (PET) and functional magnetic resonance imaging (fMRI) to demonstrate the relationship between changes in receptor occupancy measured by PET and changes in brain activity inferred by fMRI. By administering the D2/D3 dopamine receptor antagonist [(11)C]raclopride at varying specific activities to anesthetized nonhuma...
متن کاملDopamine D3 receptor mutant and wild-type mice exhibit identical responses to putative D3 receptor-selective agonists and antagonists.
Previous studies using a variety of drugs with different affinities for the dopamine (DA) D3 receptor suggested that this receptor is involved in regulating motor activity and hypothermia. However, the in vivo selectivity of many of these compounds has been repeatedly questioned. To examine the precise roles of the DA D3 receptor in motor activity and hypothermic responses, we used mutant mice ...
متن کاملHigh Affinity Dopamine D3 Receptor (D3R)-Selective Antagonists Attenuate Heroin Self-Administration in Wild-Type but not D3R Knockout Mice
The dopamine D3 receptor (D3R) is a promising target for the development of pharmacotherapeutics to treat substance use disorders. Several D3R-selective antagonists are effective in animal models of drug abuse, especially in models of relapse. Nevertheless, poor bioavailability, metabolic instability, and/or predicted toxicity have impeded success in translating these drug candidates to clinica...
متن کاملذخیره در منابع من
با ذخیره ی این منبع در منابع من، دسترسی به آن را برای استفاده های بعدی آسان تر کنید
برای دانلود متن کامل این مقاله و بیش از 32 میلیون مقاله دیگر ابتدا ثبت نام کنید
ثبت ناماگر عضو سایت هستید لطفا وارد حساب کاربری خود شوید
ورودعنوان ژورنال:
- Biochemical Society transactions
دوره 24 1 شماره
صفحات -
تاریخ انتشار 1996