- Synthesis and monoamine transporter affinity of 2β-carbomethoxy-3β-(2-,3- or 4-substituted) biphenyltropanes
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A series of 11 novel 3β-substituted biphenyltropanes was synthesized and evaluated by selective radioligand binding assays for affinity to monoamine transporters. Both 5-HTT potency and selectivity for 5-HTT over DAT was greatest with electron withdrawing group at the 3-position. (C) 2000 Elsevier Science Ltd. All rights reserved.
- Tamagnan, Gilles,Baldwin, Ronald M.,Kula, Nora S.,Baldessarini, Ross J.,Innis, Robert B.
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- Isomerization study of aryltropane analogs of cocaine
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Isomerization of brain imaging agents aryltropane cocaine analogs have been examined by HPLC under chemical conditions similar to those encountered during radiolabeling.
- Zheng, Qi-Huang,Mulholland, G. Keith
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Read Online
- Synthesis and biological evaluation of 2β,3α-(substituted phenyl)nortropanes as potential norepinephrine transporter imaging agents
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A series of 2β,3α-(substituted phenyl)nortropanes was synthesized and evaluated in vitro for human monoamine transporters. All compounds studied in this series exhibited nanomolar potency for the norepinephrine transporter (NET). Radiolabeling and nonhuma
- Zeng, Fanxing,Stehouwer, Jeffrey S.,Jarkas, Nachwa,Voll, Ronald J.,Williams, Larry,Camp, Vernon M.,Votaw, John R.,Owens, Michael J.,Kilts, Clinton D.,Nemeroff, Charles B.,Goodman, Mark M.
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p. 3044 - 3047
(2008/02/05)
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- Fluoralkenyl nortropanes
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Provided are compounds of the following formula: wherein R is C2-C6 mono- or multi-unsaturated hydrocarbon having one or more ethylene, acetylene or allene groups, A is 18 or 19, and X is H or halogen. The compounds of the invention bind to dopamine transporter with high affinity and selectivity and are thus useful as diagnostic and therapeutic agents for diseases associated with dopamine transporter dysfunction. The radiolabeled compounds are useful as imaging agents for visualizing the location and density of dopamine transporter by PET imaging.
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Page column 17
(2008/06/13)
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- Dopamine transporter imaging ligand
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The 3α isomer of RTI-55, RTI-352, is an effective in vivo binding ligand that reflects greater selectivity for the dopamine transporter than is observed with RTI-55. In addition, there is also a more rapid achievement of apparent equilibrium in the striat
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(2010/01/30)
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- Synthesis and biological evaluation of a series of novel N- or O-fluoroalkyl derivatives of tropane: Potential positron emission tomography (PET) imaging agents for the dopamine transporter
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A series of novel fluoroalkyl-containing tropane derivatives was synthesized, and their binding affinities for the dopamine transporter (DAT), serotonin transporter (SERT), and norepinephrine transporter (NET) were determined via competitive binding assays. Among these derivatives, the fluoropropyl ester of β-CIT (19), the fluoroethyl ester of β-CIT (20), the N-fluoropropyl derivative of β-CBT (12), and the fluoropropyl ester of β-CMT (18) displayed higher affinity and greater selectivity for the DAT versus SERT and NET than FP-CIT, which indicates that they are attractive candidates for the development of 18F-labeled PET imaging agents for the DAT.
- Gu, Xiao-Hui,Zong, Rushi,Kula, Nora S.,Baldessarini, Ross J.,Neumeyer, John L.
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p. 3049 - 3053
(2007/10/03)
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- A direct iodination method with iodine and silver triflate for the synthesis of SPECT and PET imaging agent precursors
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A direct iodination method with iodine and silver triflate for the synthesis of SPECT and PET imaging agent precursors has been developed.
- Mulholland,Zheng
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p. 3059 - 3068
(2007/10/03)
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- Secondary amine analogues of 3 beta-(4'-substituted phenyl)tropane-2 beta-carboxylic acid esters and N-norcocaine exhibit enhanced affinity for serotonin and norepinephrine transporters.
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N-Norcocaine (2) and six N-nor-3 beta-(4'-substituted phenyl)tropane-2 beta-carboxylic acid esters (4a-f) were synthesized by N-demethylation of cocaine (1) and the appropriate 3 beta-(substituted phenyl)-tropane analogues (3a-f) with alpha-chloroethyl chloroformate. Radioligand binding affinities of 2 and 4a-f at the DA, 5-HT, and NE transporter were measured and compared to those of 1 and 3a-f. N-Demethylation produced relatively small effects at the DA transporter. In contrast, 4-19-fold and 2-44-fold enhanced affinity at the serotonin and norepinephrine transporter resulted from demethylation. N-Nor-3 beta-(4'-iodophenyl)tropane-2 beta-carboxylic acid methyl ester (4d) with an IC50 = 0.36 nM showed the greatest affinity for the serotonin transporter. However, N-nor-3 beta-(4'-ethylphenyl)tropane-2 beta-carboxylic acid methyl ester (4e) showed the greatest selectivity for the serotonin transporter.
- Boja,Kuhar,Kopajtic,Yang,Abraham,Lewin,Carroll
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p. 1220 - 1223
(2007/10/02)
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- Synthesis, ligand binding, QSAR, and CoMFA study of 3β-(p-substituted phenyl)tropane-2β-carboxylic acid methyl esters
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A series of 3β-(p-substituted phenyl)tropane-2β-carboxylic acid methyl esters (2) were synthesized and found to possess high affinity for the cocaine binding site in rat striatum. The p-chloro (2c) and p-iodo (2n) compounds, which were the most potent analogues prepared, were found to be 85 and 78 times more potent than (-)-cocaine. The p-bromo (2m) and p-methyl (2d) were also 56 and 60 times more potent than cocaine. QSAR and CoMFA studies were conducted to correlate binding affinity of the cocaine analogues with their structural features. Whereas the QSAR study gave relatively low correlations, the CoMFA study gave a correlation with high predictive value.
- Carroll,Gao,Rahman,Abraham,Parham,Lewin,Boja,Kuhar
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p. 2719 - 2725
(2007/10/02)
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