High-affinity and selective dopamine D3 receptor full agonists
نویسندگان
چکیده
منابع مشابه
Effects of selective dopamine receptor (Dl and D2) agonists on stress-induced gastric ulcer in rat
It has been revealed that dopamine (DA) modulates gastro-duodenal responses to stress. Several investigations have been made to identify the mechanisms and/or receptors by which DA or its promoters exert their gastroprotective function against stress, however there are many discrepancies in this respect. In order to clarify the relative contribution and/or interaction of two DA receptor subty...
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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 ...
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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...
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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...
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Dopamine D3 receptor (D3R)-selective compounds may be useful medications for cocaine dependence. In this study, we identified two novel arylamide phenylpiperazines, OS-3-106 and WW-III-55, as partial agonists at the D3R in the adenylyl cyclase inhibition assay. OS-3-106 and WW-III-55 have 115and 862fold D3R:D2 receptor (D2R) binding selectivity, respectively. We investigated their effects (0, 3...
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ژورنال
عنوان ژورنال: Bioorganic & Medicinal Chemistry Letters
سال: 2012
ISSN: 0960-894X
DOI: 10.1016/j.bmcl.2012.07.003