Development of molecular tools based on the dopamine D3 receptor ligand FAUC 329 showing inhibiting effects on drug and food maintained behavior

Beitrag in einer Fachzeitschrift
(Originalarbeit)


Details zur Publikation

Autor(en): Stößel A, Brox R, Purkayastha N, Hübner H, Hocke C, Prante O, Gmeiner P
Zeitschrift: Bioorganic & Medicinal Chemistry
Jahr der Veröffentlichung: 2017
Band: 25
Heftnummer: 13
Seitenbereich: 3491-3499
ISSN: 0968-0896


Abstract


Dopamine D3 receptor-mediated networks have been associated with a wide range of neuropsychiatric diseases, drug addiction and food maintained behavior, which makes D3 a highly promising biological target. The previously described dopamine D3 receptor ligand FAUC 329 (1) showed protective effects against dopamine depletion in a MPTP mouse model of Parkinson's disease. We used the radioligand [(18)F]2, a [(18)F]fluoroethoxy substituted analog of the lead compound 1 as a molecular tool for visualization of D3-rich brain regions including the islands of Calleja. Furthermore, structural modifications are reported leading to the pyrimidylpiperazine derivatives 3 and 9 displaying superior subtype selectivity and preference over serotonergic receptors. Evaluation of the lead compound 1 on cocaine-seeking behavior in non-human primates showed a substantial reduction in cocaine self-administration behavior and food intake.



FAU-Autoren / FAU-Herausgeber

Brox, Regine Dr.
Lehrstuhl für Pharmazeutische Chemie
Gmeiner, Peter Prof. Dr.
Lehrstuhl für Pharmazeutische Chemie
Hübner, Harald Dr.
Lehrstuhl für Pharmazeutische Chemie
Stößel, Anne Dr.
Lehrstuhl für Pharmazeutische Chemie


Zusätzliche Organisationseinheit(en)
Emil-Fischer-Zentrum (Emil Fischer Center)


Autor(en) der externen Einrichtung(en)
Universitätsklinikum Ulm


Zitierweisen

APA:
Stößel, A., Brox, R., Purkayastha, N., Hübner, H., Hocke, C., Prante, O., & Gmeiner, P. (2017). Development of molecular tools based on the dopamine D3 receptor ligand FAUC 329 showing inhibiting effects on drug and food maintained behavior. Bioorganic & Medicinal Chemistry, 25(13), 3491-3499. https://dx.doi.org/10.1016/j.bmc.2017.04.036

MLA:
Stößel, Anne, et al. "Development of molecular tools based on the dopamine D3 receptor ligand FAUC 329 showing inhibiting effects on drug and food maintained behavior." Bioorganic & Medicinal Chemistry 25.13 (2017): 3491-3499.

BibTeX: 

Zuletzt aktualisiert 2018-07-10 um 02:43