25024-99-1Relevant articles and documents
Synthesis, in silico, and in vitro studies of novel dopamine D2 and D3 receptor ligands
Elek, Milica,Djokovic, Nemanja,Frank, Annika,Oljacic, Slavica,Zivkovic, Aleksandra,Nikolic, Katarina,Stark, Holger
, (2021/02/26)
Dopamine is an important neurotransmitter in the human brain and its altered concentrations can lead to various neurological diseases. We studied the binding of novel compounds at the dopamine D2 (D2R) and D3 (D3/sub
Compound with dopamine D3 receptor adjusting activity, and applications thereof
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Paragraph 0155; 0164; 0166, (2019/03/22)
The invention relates to a compound with dopamine D3 receptor adjusting activity, and applications thereof, and more specifically discloses dopamine receptor D3R as a novel target of post-traumatic stress disorder (PTSD) in prevention, treatment/or auxiliary treatment of PTSD, and screening of anti-PTSD medicines, and relates to applications of a compound with dopamine receptor D3R adjusting activity in preparation of medicines used for preventing, treatment and/or auxiliary treatment of PTSD.
Fast and efficient 18F-labeling by [18F]fluorophenylazocarboxylic esters
Fehler, Stefanie K.,Maschauer, Simone,Hcfling, Sarah B.,Bartuschat, Amelie L.,Tschammer, Nuska,Hubner, Harald,Gmeiner, Peter,Prante, Olaf,Heinrich, Markus R.
supporting information, p. 370 - 375 (2014/04/03)
Introduction of [18F]fluoride ion into the aromatic core of phenylazocarboxylic esters was achieved in only 30 seconds, with radiochemical yields of up to 95% (85(±10) %). For labeling purposes, the resulting 18F-substituted azoester can be further converted in radical-arylation reactions to give biaryls, or in substitutions at its carbonyl unit to produce azocarboxamides.
Synthesis and pharmacological evaluation of [(4-Arylpiperazin-1-yl)-alkyl]- carbamic acid ethyl ester derivatives as potential anxiolytic agents
Khatri, Manisha,Rai, Santosh K.,Ranbhor, Ranjit,Kishore, Krishna,Tiwari, Manisha
experimental part, p. 1143 - 1152 (2012/11/07)
On the basis of our earlier studies, a series of N-{4-[4-(aryl) piperazin-1-yl]-phenyl}-amine derivatives containing terminal carbamoyl fragment with alkyl spacer of different lengths (15-20) were synthesized as ligands, for 5-hydroxytryptamine-1A (5-HT1A
Preparation, characterization, and screening of a high affinity organometallic probe for α-adrenergic receptors
Louie, Anika S.,Vasdev, Neil,Valliant, John F.
experimental part, p. 3360 - 3367 (2011/06/22)
Figure Presented. An organometallic rhenium complex having high and selective affinity for α-adrenergic receptors is reported. A series of methoxyphenylpiperazinecarborane ligands complexed to the [Re(CO) 3]+ core were prepared and t
Synthesis, biological evaluation and radiolabelling by 18F- fluoroarylation of a dopamine D3-selective ligand as prospective imaging probe for PET
H?fling,Maschauer,Hübner,Gmeiner,Wester,Prante,Heinrich
supporting information; experimental part, p. 6933 - 6937 (2011/03/17)
Radical 18F-fluoroarylation with fluorine-18-labelled arenediazonium chlorides has been successfully applied to the radiochemical synthesis of the dopamine D3-selective ligand SH 317 ([ 18F]8). SH 317 has been evaluated as
Bioisosteric replacement leading to biologically active [2.2]Paracyclophanes with altered binding profiles for aminergic g-protein-coupled receptors
Skultety, Marika,Hübner, Harald,L?ber, Stefan,Gmeiner, Peter
experimental part, p. 7219 - 7228 (2010/12/25)
Exploring the chemical diversity space of GPCR ligands, we recently discovered [2.2]paracyclophanes as valuable atypical bioisosteres for secondary affinity and selectivity generating moieties. To find out if such an exchange also works for structural moieties that simulate the endogenous neurotransmitter, π1 or π2 or both systems π1 and π2 of three representative privileged structures of types 1, 2, and 3 were replaced by a [2.2]paracyclophane unit. Contributions of the respective functionalities to the binding affinities of a panel of relevant monoaminergic GPCRs were systematically examined. The study led to the paracyclophanylpiperazine 3a displaying excellent D3 affinity (Ki = 1.6 nM) and a strongly attenuated binding to D4, 5-HT1 and α1. Whereas functional experiments showed neutral D3 antagonist properties, mutagenesis studies indicated a binding mode that is similar to its lead compounds of type 3.
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
Solventless microwave assisted protocol for synthesis of arylalkylpiperazines using Cs-base
Giuglio-Tonolo, Alain Gamal,Terme, Thierry,Vanelle, Patrice
experimental part, p. 160 - 162 (2010/04/22)
A series of some arylalkylpiperazines was prepared in good yields under microwave irradiation in dry media conditions using CsOH with high chemo- and regioselectivity.
3,4-dihydro-2-naphthamide derivatives as selective dopamine D3 ligands
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Page/Page column 10, (2008/06/13)
The invention relates to 3,4-dihydro-2-naphthamide derivatives of formula (I), pharmaceutical compositions containing them and their therapeutic applications as partial agonists or antagonists of the dopamine D3 receptor for the treatment of neuropsychological disorders.