82278-36-2Relevant academic research and scientific papers
Design, synthesis, and evaluation of N-(4-(4-phenyl piperazin-1-yl)butyl)-4-(thiophen-3-yl)benzamides as selective dopamine D3 receptor ligands
Chen, Peng-Jen,Taylor, Michelle,Griffin, Suzy A.,Amani, Armaghan,Hayatshahi, Hamed,Korzekwa, Kenneth,Ye, Min,Mach, Robert H.,Liu, Jin,Luedtke, Robert R.,Gordon, John C.,Blass, Benjamin E.
supporting information, p. 2690 - 2694 (2019/08/07)
As part of our on-going effort to explore the role of dopamine receptors in drug addiction and identify potential novel therapies for this condition, we have a identified a series of N-(4-(4-phenyl piperazin-1-yl)butyl)-4-(thiophen-3-yl)benzamide D3 ligands. Members of this class are highly selective for D3 versus D2, and we have identified two compounds (13g and 13r) whose rat in vivo IV pharmacokinetic properties that indicate that they are suitable for assessment in in vivo efficacy models of substance use disorders.
Synthesis and pre-clinical evaluation of a potential radiotracer for PET imaging of the dopamine D3 receptor
Stewart, Megan N.,Shao, Xia,Desmond, Timothy J.,Forrest, Taylor J.,Arteaga, Janna,Stauff, Jenelle,Scott, Peter J. H.
, p. 1315 - 1322 (2018/08/28)
There is considerable interest in using positron emission tomography (PET) imaging to understand the function of dopamine D3 receptors. Due to high sequence homology with D2 receptors, development of D3-selective PET radiotracers has been challenging. In an effort to overcome this issue, we report the radiosynthesis of a new selective D3 ligand with carbon-11 ([11C]1), and its initial preclincial evaluation as a potential PET radiotracer for in vivo imaging of D3 receptors. [11C]1 was prepared via [11C]CO2 fixation in 0.1% non-corrected radiochemical yield, good radiochemical purity (>95%) and high specific activity (>2000 Ci mmol-1). [11C]1 exhibited specific binding to D3 receptors using ex vivo autoradiography experiments with rat brain, but only 14-fold selectivity over D2 receptors which is lower than the 1400-fold value reported previously for cell studies. Rodent PET imaging revealed reasonable uptake of the radiotracer in areas of the brain known to be rich in D3 receptors.
Design, synthesis and evaluation of bitopic arylpiperazinephenyl-1,2,4-oxadiazoles as preferential dopamine D3 receptor ligands
Cao, Yongkai,Min, Chengchun,Acharya, Srijan,Kim, Kyeong-Man,Cheon, Seung Hoon
, p. 191 - 200 (2015/12/31)
The dopamine D3 receptor (D3R) was proposed as a therapeutic target for drug development to treat drug abuse and addiction and neuropsychiatric disorders. Several D3R-selective modulators over the dopamine D2 receptor (D2R) can avoid extrapyramidal sympto
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
Arylpiperaszine derivatives, to the process for the production thereof and to the use thereof as therapeutic agents
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Page/Page column 12, (2008/06/13)
The invention relates to compounds of the general formula (I): to the process for preparing them, and to the use thereof as a therapeutic agent.
BENZIMIDAZOLONE DERIVATIVES
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, (2008/06/13)
Pharmacologically active benzimidazolone derivatives as 5-HT. sub.1A and 5-HT 2 receptors, useful in the treatment of CNS disorders, of formula: STR1 wherein the substituents are defined herein.
