Comparative Study
doi: 10.1016/0014-2999(90)90627-i.
New, potent cocaine analogs: ligand binding and transport studies in rat striatum
Affiliations
- PMID: 2079102
- DOI: 10.1016/0014-2999(90)90627-i
Item in Clipboard
Comparative Study
New, potent cocaine analogs: ligand binding and transport studies in rat striatum
Eur J Pharmacol.
.
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.
Similar articles
-
Highly potent cocaine analogs cause long-lasting increases in locomotor activity.Eur J Pharmacol. 1996 Sep 12;311(2-3):109-14. doi: 10.1016/0014-2999(96)00423-2. Eur J Pharmacol. 1996. PMID: 8891589
-
Isothiocyanate derivatives of cocaine: irreversible inhibition of ligand binding at the dopamine transporter.Mol Pharmacol. 1991 Mar;39(3):339-45. Mol Pharmacol. 1991. PMID: 1826041
-
Translocation of dopamine and binding of 2 beta-carbomethoxy-3 beta-(4-fluorophenyl) tropane (WIN 35,428) measured under identical conditions in rat striatal synaptosomal preparations. Inhibition by various blockers.Biochem Pharmacol. 1995 Jan 31;49(3):339-50. doi: 10.1016/0006-2952(94)00485-5. Biochem Pharmacol. 1995. PMID: 7857321
-
Two-carbon bridge substituted cocaines: enantioselective synthesis, attribution of the absolute configuration and biological activity of novel 6- and 7-methoxylated cocaines.Farmaco. 1999 May 30;54(5):275-87. doi: 10.1016/s0014-827x(99)00027-0. Farmaco. 1999. PMID: 10418122 Review.
-
The New Rival of Cocaine.Daniels Tex Med J. 1887 Oct;3(4):141-142. Daniels Tex Med J. 1887. PMID: 36953021 Free PMC article. Review. No abstract available.
Cited by
-
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.J Med Chem. 2010 Aug 12;53(15):5549-57. doi: 10.1021/jm100269c. J Med Chem. 2010. PMID: 20597489 Free PMC article.
-
Fluorine-18 Radiolabeled PET Tracers for Imaging Monoamine Transporters: Dopamine, Serotonin, and Norepinephrine.PET Clin. 2009 Jan;4(1):101-28. doi: 10.1016/j.cpet.2009.05.006. PET Clin. 2009. PMID: 20216936 Free PMC article.
-
Effects of SCH 23390 and eticlopride on cocaine-seeking produced by cocaine and WIN 35,428 in rats.Psychopharmacology (Berl). 2003 Jul;168(1-2):118-123. doi: 10.1007/s00213-002-1276-y. Epub 2002 Nov 5. Psychopharmacology (Berl). 2003. PMID: 12420155
-
Cocaine binding sites in fetal rat brain: implications for prenatal cocaine action.Psychopharmacology (Berl). 1993;112(4):445-51. doi: 10.1007/BF02244892. Psychopharmacology (Berl). 1993. PMID: 7871055
-
Tracers for metabolic imaging of brain and heart. Radiochemistry and radiopharmacology.Eur J Nucl Med. 1992;19(7):527-51. doi: 10.1007/BF00185860. Eur J Nucl Med. 1992. PMID: 1644110 Review. No abstract available.
Publication types
MeSH terms
Substances
Grants and funding
LinkOut - more resources
Full Text Sources
Other Literature Sources
Miscellaneous
