107188-91-0Relevant academic research and scientific papers
Arylamides hybrids of two high-affinity σ2 receptor ligands as tools for the development of PET radiotracers
Abate, Carmen,Ferorelli, Savina,Contino, Marialessandra,Marottoli, Roberta,Colabufo, Nicola Antonio,Perrone, Roberto,Berardi, Francesco
experimental part, p. 4733 - 4741 (2011/11/29)
1-Cyclohexyl-4-[3-(5-methoxy-1,2,3,4-tetrahydronaphthalen-1-yl)propyl] piperazine 1 (PB28) and 2-Methoxy-5-methyl-N-[4-(6,7-dimethoxy-3,4-dihydro-1H- isoquinolin-2-yl)butyl]benzamide 2 (RHM-1) represent leads for tumor diagnosis, given their high affinity
Synthesis of 3-(5-bromo-2,3-dimethoxy-phenyl)-[1, 2, 4] oxadiazole analogues and their evaluation as anti-Parkinson's agents
Tiwari, Shashi B.,Kohli
, p. 386 - 398 (2008/12/22)
A series of 3-(5-bromo-2,3-dimethoxy-phenyl)-[1, 2, 4] oxadiazole derivatives was prepared and their evaluation for anti-Parkinson's activity was measured in vivo using albino rats. The result of the biological activity studies indicated that some of the
Sigma-2 receptor radiotracers for imaging the proliferative status of solid tumors
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Page/Page column 16, (2008/06/13)
Novel benzamide compounds of Formula (I), Formula (II) and Formula (III, salts, water soluble salts, analogs and radiolabeled counterparts thereof as sigma-2 receptor radiotracers for imaging the proliferative status of solid tumors. A method for diagnosi
Synthesis of 2-(5-Bromo-2,3-dimethoxyphenyl)-5-(aminomethyl)-1H-pyrrole analogues and their binding affinities for dopamine D2, D3, and D4 receptors
Mach, Robert H.,Huang, Yunsheng,Freeman, Rebekah A.,Wu, Li,Blair, Suwanna,Luedtke, Robert R.
, p. 225 - 233 (2007/10/03)
A series of 2-(5-bromo-2,3-dimethoxyphenyl)-5-(aminomethyl)-1H-pyrrole analogues was prepared and their affinity for dopamine D2, D3, and D4 receptors was measured using in vitro binding assays. The results of receptor bin
Synthesis of 2-(2,3-dimethoxyphenyl)-4-(aminomethyl)imidazole analogues and their binding affinities for dopamine D2 and D3 receptors
Huang, Yunsheng,Luedtke, Robert R.,Freeman, Rebekah A.,Wu, Li,Mach, Robert H.
, p. 3113 - 3122 (2007/10/03)
A series of 2-(2,3-dimethoxyphenyl)-4-(aminomethyl)imidazole derivatives was prepared and their affinity for dopamine D2 and D3 receptors was measured using in vitro binding assays. Several oxadiazole analogues were also prepared and tested for their affinity for dopamine D2 and D3 receptors. The results of receptor binding studies indicated that the incorporation of an imidazole moiety between the phenyl ring and the basic nitrogen did not significantly increase the selectivity for dopamine D3 receptors, whereas the incorporation of an oxadiazole at the same region resulted in a total loss of affinity for both dopamine receptor subtype binding sites. The most selective compound in this series is 2-(5-bromo-2,3-dimethoxyphenyl)-4-(6,7-dimethoxy-1,2,3, 4-tetrahydroisoquinolinomethyl)imidazole (5i), which has a D3 receptor affinity of 21 nM and a 7-fold selectivity for D3 versus D2 receptors. The binding affinity for σ1 and σ2 receptors was also measured, and the results showed that several analogues were selective σ1 receptor ligands.
Improved specific radioactivity of the PET radioligand [11C]FLB 457 by use of the GE Medical Systems PETtrace MeI MicroLab
Sandell, Johan,Langer, Oliver,Larsen, Peter,Dolle, Frederic,Vaufrey, Francoise,Demphel, Stephane,Crouzel, Christian,Halldin, Christer
, p. 331 - 338 (2007/10/03)
[11C]FLB 457 is a high affinity dopamine D2 receptor radioligand that is used for visualisation and quantitation of extrastriatal dopamine D2 receptors with positron emission tomography (PET). In this study, we report a co
Structure-activity relationship studies of N-(9-benzyl)-9- azabicyclo[3.3.1]nonan-3-β-yl benzamide analogues for dopamine D2 and D3 receptors
Mach, Robert H.,Hammond, Philip S.,Huang, Yunsheng,Yang, Biao,Xu, Yueping,Cheney, Jason T.,Freeman, Rebekah,Luedtke, Robert R.
, p. 355 - 373 (2007/10/03)
A series of benzamide derivatives were prepared in order to determine the nature of the substituent effects in the benzamide aromatic ring on the affinity to dopamine D2 and D3 receptors. Both quantitative structure- activity relatio
Synthesis and 5-HT-3 receptor binding activity of 5-[125I]iodo-2,3-dimethoxy-N-(1-azabicyclo[2.2.2]oct-3-yl]benzamide and its 5-halogen-2-alkoxyl homologues
De Paulis,Hewlett,Schmidt,Mason,Trivedi,Ebert
, p. 385 - 396 (2007/10/03)
(S)-5-Iodo-2,3-dimethoxy-N-(1-azabicyclo[2.2.2]oct-3-yl)benzamide (MIZAC) was prepared from 5-iodo-2,3-dimethoxybenzoyl chloride and (S)-3-aminoquinuclidine. [125I]Iodode-stannylation of its corresponding 5-tri-n-butyltin derivative gave [125I]-MIZAC at 1800 Ci/mmol. Binding of [125I]-MIZAC in rat entorhinal cortex revealed a K(D) of 1.37 ± 0.21 nM. A series of racemic 2-O-alkyl derivatives of MIZAC were prepared and 5-HT-3 receptor affinities were determined by inhibition of [125I]-MIZAC binding. Optimal affinity for the receptor was obtained with small, electron-withdrawing substituents in the aromatic 5-position and with bulky substituents in the 3-position. [125I]-MIZAC is a selective radioligand useful for in vitro identification of the 5-HT-3 receptor.
