- Synthesis, in silico, and in vitro studies of novel dopamine D2 and D3 receptor ligands
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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
- Elek, Milica,Djokovic, Nemanja,Frank, Annika,Oljacic, Slavica,Zivkovic, Aleksandra,Nikolic, Katarina,Stark, Holger
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- Compound with dopamine D3 receptor adjusting activity, and applications thereof
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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.
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Paragraph 0155; 0164; 0166
(2019/03/22)
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- Fast and efficient 18F-labeling by [18F]fluorophenylazocarboxylic esters
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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.
- Fehler, Stefanie K.,Maschauer, Simone,Hcfling, Sarah B.,Bartuschat, Amelie L.,Tschammer, Nuska,Hubner, Harald,Gmeiner, Peter,Prante, Olaf,Heinrich, Markus R.
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supporting information
p. 370 - 375
(2014/04/03)
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- Synthesis and pharmacological evaluation of [(4-Arylpiperazin-1-yl)-alkyl]- carbamic acid ethyl ester derivatives as potential anxiolytic agents
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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
- Khatri, Manisha,Rai, Santosh K.,Ranbhor, Ranjit,Kishore, Krishna,Tiwari, Manisha
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experimental part
p. 1143 - 1152
(2012/11/07)
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- Preparation, characterization, and screening of a high affinity organometallic probe for α-adrenergic receptors
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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
- Louie, Anika S.,Vasdev, Neil,Valliant, John F.
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experimental part
p. 3360 - 3367
(2011/06/22)
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- Synthesis, biological evaluation and radiolabelling by 18F- fluoroarylation of a dopamine D3-selective ligand as prospective imaging probe for PET
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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
- H?fling,Maschauer,Hübner,Gmeiner,Wester,Prante,Heinrich
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supporting information; experimental part
p. 6933 - 6937
(2011/03/17)
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- Bioisosteric replacement leading to biologically active [2.2]Paracyclophanes with altered binding profiles for aminergic g-protein-coupled receptors
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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.
- Skultety, Marika,Hübner, Harald,L?ber, Stefan,Gmeiner, Peter
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experimental part
p. 7219 - 7228
(2010/12/25)
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- Synthesis and evaluation of amides surrogates of dopamine D3 receptor ligands
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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
- Jean, Micka?l,Renault, Jacques,Levoin, Nicolas,Danvy, Denis,Calmels, Thierry,Berrebi-Bertrand, Isabelle,Robert, Philippe,Schwartz,Lecomte,Uriac, Philippe,Capet, Marc
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scheme or table
p. 5376 - 5379
(2010/12/24)
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- Solventless microwave assisted protocol for synthesis of arylalkylpiperazines using Cs-base
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A series of some arylalkylpiperazines was prepared in good yields under microwave irradiation in dry media conditions using CsOH with high chemo- and regioselectivity.
- Giuglio-Tonolo, Alain Gamal,Terme, Thierry,Vanelle, Patrice
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experimental part
p. 160 - 162
(2010/04/22)
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- 3,4-dihydro-2-naphthamide derivatives as selective dopamine D3 ligands
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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.
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Page/Page column 10
(2008/06/13)
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- Synthesis and in vitro binding of N-phenyl piperazine analogs as potential dopamine D3 receptor ligands
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The synthesis of a series of N-(2-methoxyphenyl)piperazine and N-(2,3-dichlorophenyl)piperazine analogs and their in vitro binding affinities for dopamine D2, D3, D4 are presented. A series of N-(2-methoxyphenyl)piperazine
- Chu, Wenhua,Tu, Zhude,McElveen, Elizabeth,Xu, Jinbin,Taylor, Michelle,Luedtke, Robert R.,MacH, Robert H.
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- Synthesis and evaluation of 18F-labeled dopamine D3 receptor ligands as potential PET imaging agents
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A series of fluoro substituted aryl carboxamides was synthesized revealing high affinity for the dopamine D3 receptor. In contrast to 2-methoxy substitution, a 2,3-dichloro substitution pattern at the phenylpiperazine moiety induces a 10-fold increase of
- Hocke, Carsten,Prante, Olaf,L?ber, Stefan,Hübner, Harald,Gmeiner, Peter,Kuwert, Torsten
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p. 4819 - 4823
(2007/10/03)
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- Synthesis and radioiodination of selective ligands for the dopamine D3 receptor subtype
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Starting from FAUC 365, a series of iodine substituted heteroaryl carboxamides has been synthesized revealing high affinity and selectivity for the dopamine D3 receptor. Binding data showed a 15-560-fold selectivity for the dopamine D3 over D2. A 2,3-dich
- Hocke, Carsten,Prante, Olaf,Loeber, Stefan,Huebner, Harald,Gmeiner, Peter,Kuwert, Torsten
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p. 3963 - 3966
(2007/10/03)
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- N-(ω)-(4-(2-methoxyphenyl)piperazin-1-yl)alkyl)carboxamides as dopamine D2 and D3 receptor ligands
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The dopamine D3 receptor is recognized as a potential therapeutic target for the treatment of various neurological and psychiatric disorders. Targetting high affinity and D3 versus D2 receptor-preferring ligands, the parti
- Hackling, Anneke,Ghosh, Robin,Perachon, Sylvie,Mann, André,H?ltje, Hans-Dieter,Wermuth, Camille G.,Schwartz, Jean-Charles,Sippl, Wolfgang,Sokoloff, Pierre,Stark, Holger
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p. 3883 - 3899
(2007/10/03)
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- 2-NAPHTHAMIDE DERIVATIVES AND THEIR THERAPEUTIC APPLICATIONS
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The invention related to 2-naphthamide derivatives, in the form of bases or of salts, corresponding to the following general formula (I): STR1 in which: the Z--Y entity represents an N--CH 2, C= CH or CH--CH. sub.2 group;R 1 represents a hydrogen, f
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- 5-HT(1A), and D-2 receptor affinity of o-methoxyphenylpiperazine derivatives with terminal benzamide fragment on N-4 alkyl chain. 2
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The synthesis of some o-methoxyphenylpiperazines with a benzamide moiety on N-4 alkyl chain was accomplished and their affinity for dopamine and serotonin receptor subtypes was assayed by in vitro receptor binding. The results show that several derivative
- Perrone,Berardi,Leopoldo,Tortorella,Lograno,Daniele,Govoni
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p. 505 - 510
(2007/10/02)
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