In vivo evaluation of [11C]- and [18F]-labelled cocaine analogues as potential dopamine transporter ligands for positron emission tomography. Export

@article{citeulike:2794891, abstract = {Four analogues of the potent dopamine transporter ligand, WIN 35,428, were radiolabelled with 11C and 18F at the 2-beta-carboxy position for evaluation as potential ligands for imaging dopamine uptake sites by positron emission tomography (PET) namely, methyl (1R-2-exo-3-exo)-8- methyl-3-(4-methylphenyl)-8-azabicyclo[3.2.1]octane-2-carboxylate (RTI-32), its 4-chlorophenyl analogue (RTI-31), 2'-fluoroethyl (1R-2-exo-3-exo)-8-methyl-3-(4-methylphenyl)-8-azabicyclo[3.2.1]octane-2 - carboxylate (FETT) and its 4-chlorophenyl analogue (FECT). Upon intravenous injection in rats, all four radiotracers displayed preferential accumulation of radioactivity in regions known to contain high concentrations of dopamine uptake sites. Competition studies with two of the analogues, [11C]RTI-32 and [18F]FETT, demonstrated that, for both radiotracers, binding was saturable and displayed the appropriate pharmacology as potential PET ligands for imaging the dopamine transporter. Striatum to cerebellar ratios for [11C]RTI-32 (at 90 min post-injection) and [18F]FETT (at 120 min post-injection) were 27 and 21, respectively.}, address = {Pet Centre, Clarke Institute of Psychiatry, Toronto, On, Canada.}, author = {Wilson, A. A. and DaSilva, J. N. and Houle, S.}, citeulike-article-id = {2794891}, citeulike-linkout-0 = {http://view.ncbi.nlm.nih.gov/pubmed/8868286}, citeulike-linkout-1 = {http://www.hubmed.org/display.cgi?uids=8868286}, issn = {0969-8051}, journal = {Nuclear medicine and biology}, keywords = {cocaine, dopamine, fect}, month = {February}, number = {2}, pages = {141--146}, posted-at = {2008-05-13 13:45:16}, priority = {2}, title = {In vivo evaluation of [11C]- and [18F]-labelled cocaine analogues as potential dopamine transporter ligands for positron emission tomography.}, url = {http://view.ncbi.nlm.nih.gov/pubmed/8868286}, volume = {23}, year = {1996} }

TY - JOUR ID - citeulike:2794891 L3 - citeulike-article-id:2794891 N2 - Four analogues of the potent dopamine transporter ligand, WIN 35,428, were radiolabelled with 11C and 18F at the 2-beta-carboxy position for evaluation as potential ligands for imaging dopamine uptake sites by positron emission tomography (PET) namely, methyl (1R-2-exo-3-exo)-8- methyl-3-(4-methylphenyl)-8-azabicyclo[3.2.1]octane-2-carboxylate (RTI-32), its 4-chlorophenyl analogue (RTI-31), 2'-fluoroethyl (1R-2-exo-3-exo)-8-methyl-3-(4-methylphenyl)-8-azabicyclo[3.2.1]octane-2 - carboxylate (FETT) and its 4-chlorophenyl analogue (FECT). Upon intravenous injection in rats, all four radiotracers displayed preferential accumulation of radioactivity in regions known to contain high concentrations of dopamine uptake sites. Competition studies with two of the analogues, [11C]RTI-32 and [18F]FETT, demonstrated that, for both radiotracers, binding was saturable and displayed the appropriate pharmacology as potential PET ligands for imaging the dopamine transporter. Striatum to cerebellar ratios for [11C]RTI-32 (at 90 min post-injection) and [18F]FETT (at 120 min post-injection) were 27 and 21, respectively. IS - 2 JF - Nuclear medicine and biology SN - 0969-8051 AD - Pet Centre, Clarke Institute of Psychiatry, Toronto, On, Canada. EP - 146 TI - In vivo evaluation of [11C]- and [18F]-labelled cocaine analogues as potential dopamine transporter ligands for positron emission tomography. VL - 23 SP - 141 KW - cocaine KW - dopamine KW - fect AU - Wilson, AA AU - DaSilva, JN AU - Houle, S PY - 1996/02// UR - http://view.ncbi.nlm.nih.gov/pubmed/8868286 ER -