DOPAMINE D3 RECEPTOR OCCUPANCY AND D3 RECEPTOR-MEDIATED ACTIONS OF CARIPRAZINE, A DOPAMINE D3/D2 RECEPTOR PARTIAL AGONIST ANTIPSYCHOTIC CANDIDATE

2014 ◽  
Vol 153 ◽  
pp. S23
Author(s):  
Ashok Rakhit ◽  
Suresh Durgam ◽  
Nika Adham ◽  
István Gyertyán ◽  
Béla Kiss ◽  
...  
1992 ◽  
Vol 225 (4) ◽  
pp. 331-337 ◽  
Author(s):  
Pierre Sokoloff ◽  
Marc Andrieux ◽  
Roger Besançon ◽  
Catherine Pilon ◽  
Marie-Pascale Martres ◽  
...  

2018 ◽  
Vol 171 ◽  
pp. 46-53 ◽  
Author(s):  
Gregory L. Powell ◽  
John Paul Bonadonna ◽  
Annika Vannan ◽  
Kuiying Xu ◽  
Robert H. Mach ◽  
...  

1995 ◽  
Vol 282 (1-3) ◽  
pp. R3-R4 ◽  
Author(s):  
Nathalie Griffon ◽  
Catherine Pilon ◽  
Jean-Charles Schwartz ◽  
Pierre Sokoloff

2021 ◽  
Author(s):  
Thomas Oh ◽  
Elyas Daadi ◽  
Jeffrey Kim ◽  
Etienne Daadi ◽  
Peng-Jen Chen ◽  
...  

Abstract Parkinson’s disease (PD) is a complex multisystem, chronic and so far incurable disease with significant unmet medical needs. The incidence of PD increases with aging and the expected burden will continue to escalate with our aging population. Since its discovery in the 1961 levodopa remains the gold standard pharmacotherapy for PD. However, the progressive nature of the neurodegenerative process in and beyond the nigrostriatal system causes a multitude of side effects, including levodopa-induced dyskinesia within 5 years of therapy. Attenuating dyskinesia has been a significant challenge in the clinical management of PD. We report on a small molecule that eliminates the expression of levodopa-induced dyskinesia and significantly improves PD-like symptoms. The lead compound PD13R we discovered is a dopamine D3 receptor partial agonist with high affinity and selectivity, orally active and with desirable drug-like properties. Future studies are aimed at developing this lead compound for treating PD patients with dyskinesia.


2009 ◽  
Vol 616 (1-3) ◽  
pp. 134-140 ◽  
Author(s):  
Megan E. Breuer ◽  
Lucianne Groenink ◽  
Ronald S. Oosting ◽  
Erich Buerger ◽  
Michiel Korte ◽  
...  

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