Literature DB >> 2079102

New, potent cocaine analogs: ligand binding and transport studies in rat striatum.

J W Boja1, F I Carroll, M A Rahman, A Philip, A H Lewin, M J Kuhar.   

Abstract

Two potent cocaine analogs have been developed that have the highest known affinities for the cocaine binding site in rat striatum. Both 3 beta-(4-chlorophenyl)- (RTI-COC-31) and 3 beta-(4-methylphenyl)-tropane-2-carboxylic acid methyl ester (RTI-COC-32) compete for [3H]WIN 35,428 and [3H]mazindol binding with a IC50 that is 100 times more potent than that of (-) cocaine. Additionally, these compounds inhibit [3H]dopamine uptake with a similar, high potency. These results may lead to the development of high affinity probes for the cocaine binding site.

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Year:  1990        PMID： 2079102     DOI： 10.1016/0014-2999(90)90627-i

Source DB:  PubMed          Journal:  Eur J Pharmacol        ISSN： 0014-2999            Impact factor:   4.432


  13 in total

1.  VMAT2 knockout mice: heterozygotes display reduced amphetamine-conditioned reward, enhanced amphetamine locomotion, and enhanced MPTP toxicity.

Authors:  N Takahashi; L L Miner; I Sora; H Ujike; R S Revay; V Kostic; V Jackson-Lewis; S Przedborski; G R Uhl
Journal:  Proc Natl Acad Sci U S A       Date:  1997-09-02       Impact factor: 11.205

Review 2.  Tracers for metabolic imaging of brain and heart. Radiochemistry and radiopharmacology.

Authors:  G Stöcklin
Journal:  Eur J Nucl Med       Date:  1992

3.  Molecular mechanisms of cocaine reward: combined dopamine and serotonin transporter knockouts eliminate cocaine place preference.

Authors:  I Sora; F S Hall; A M Andrews; M Itokawa; X F Li; H B Wei; C Wichems; K P Lesch; D L Murphy; G R Uhl
Journal:  Proc Natl Acad Sci U S A       Date:  2001-04-24       Impact factor: 11.205

4.  Synthesis, fluorine-18 radiolabeling, and biological evaluation of N-((E)-4-fluorobut-2-en-1-yl)-2beta-carbomethoxy-3beta-(4'-halophenyl)nortropanes: candidate radioligands for in vivo imaging of the brain dopamine transporter with positron emission tomography.

Authors:  Jeffrey S Stehouwer; Lauryn M Daniel; Ping Chen; Ronald J Voll; Larry Williams; Susan J Plott; John R Votaw; Michael J Owens; Leonard Howell; Mark M Goodman
Journal:  J Med Chem       Date:  2010-08-12       Impact factor: 7.446

5.  Fluorine-18 Radiolabeled PET Tracers for Imaging Monoamine Transporters: Dopamine, Serotonin, and Norepinephrine.

Authors:  Jeffrey S Stehouwer; Mark M Goodman
Journal:  PET Clin       Date:  2009-01

6.  Effects of SCH 23390 and eticlopride on cocaine-seeking produced by cocaine and WIN 35,428 in rats.

Authors:  Susan Schenk; Dave Gittings
Journal:  Psychopharmacology (Berl)       Date:  2002-11-05       Impact factor: 4.530

7.  Cocaine binding sites in fetal rat brain: implications for prenatal cocaine action.

Authors:  J S Meyer; L P Shearman; L M Collins; R L Maguire
Journal:  Psychopharmacology (Berl)       Date:  1993       Impact factor: 4.530

Review 8.  Biomechanisms of cocaine-induced hepatocyte injury mediated by the formation of reactive metabolites.

Authors:  U A Boelsterli; C Göldlin
Journal:  Arch Toxicol       Date:  1991       Impact factor: 5.153

9.  Voltammetric characterization of the effect of monoamine uptake inhibitors and releasers on dopamine and serotonin uptake in mouse caudate-putamen and substantia nigra slices.

Authors:  Carrie E John; Sara R Jones
Journal:  Neuropharmacology       Date:  2007-03-16       Impact factor: 5.250

Review 10.  PE2I: a radiopharmaceutical for in vivo exploration of the dopamine transporter.

Authors:  Patrick Emond; Denis Guilloteau; Sylvie Chalon
Journal:  CNS Neurosci Ther       Date:  2008       Impact factor: 5.243
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