883874-56-4Relevant articles and documents
Evaluation of substituted n-phenylpiperazine analogs as D3 vs. D2 dopamine receptor subtype selective ligands
Lee, Boeun,Taylor, Michelle,Griffin, Suzy A.,McInnis, Tamara,Sumien, Nathalie,Mach, Robert H.,Luedtke, Robert R.
, (2021/06/14)
N-phenylpiperazine analogs can bind selectively to the D3 versus the D2 dopamine receptor subtype despite the fact that these two D2-like dopamine receptor subtypes exhibit substantial amino acid sequence homology. The binding for a number of these receptor subtype selective compounds was found to be consistent with their ability to bind at the D3 dopamine receptor subtype in a bitopic manner. In this study, a series of the 3-thiophenephenyl and 4-thiazolylphenyl fluoride substituted N-phenylpiperazine analogs were evaluated. Compound 6a was found to bind at the human D3 receptor with nanomolar affinity with substantial D3 vs. D2 binding selectivity (approximately 500-fold). Compound 6a was also tested for activity in two in-vivo assays: (1) a hallucinogenic-dependent head twitch response inhibition assay using DBA/2J mice and (2) an L-dopa-dependent abnormal involuntary movement (AIM) inhibition assay using unilateral 6-hydroxydopamine lesioned (hemiparkinsonian) rats. Compound 6a was found to be active in both assays. This compound could lead to a better understanding of how a bitopic D3 dopamine receptor selective ligand might lead to the development of pharmacotherapeutics for the treatment of levodopa-induced dyskinesia (LID) in patients with Parkinson’s disease.
Synthesis and biological evaluation of 2-fluoro and 3-trifluoromethyl-phenyl-piperazinylalkyl derivatives of 1H-imidazo[2,1-f]purine-2,4(3H,8H)-dione as potential antidepressant agents
Zagórska, Agnieszka,Bucki, Adam,Ko?aczkowski, Marcin,Siwek, Agata,G?uch-Lutwin, Monika,Starowicz, Gabriela,Kazek, Grzegorz,Partyka, Anna,Weso?owska, Anna,S?oczyńska, Karolina,P?kala, El?bieta,Paw?owski, Maciej
, p. 10 - 24 (2016/12/16)
A series of 2-fluoro and 3-trifluoromethylphenylpiperazinylalkyl derivatives of 1H-imidazo[2,1-f]purine-2,4(3H,8H)-dione (4–21) were synthesized and evaluated for their serotonin (5-HT1A/5-HT7) receptor affinity and phosphodiesterase
Synthesis and evaluation of amides surrogates of dopamine D3 receptor ligands
Jean, Micka?l,Renault, Jacques,Levoin, Nicolas,Danvy, Denis,Calmels, Thierry,Berrebi-Bertrand, Isabelle,Robert, Philippe,Schwartz,Lecomte,Uriac, Philippe,Capet, Marc
scheme or table, p. 5376 - 5379 (2010/12/24)
Isosteric replacement of the amide function and modulation of the arylpiperazine moiety of known dopamine D3 receptor ligands led to potent and selective compounds. Enhanced bioavailability and preferential brain distribution make compound 6c a good candi