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Chemical Compound Review

Indatralinum     (1R,3S)-3-(3,4- dichlorophenyl)-N-methyl-2...

Synonyms: Lopac-I-119, CHEMBL341898, SureCN9252640, CHEBI:344099, CCG-204769, ...
 
 
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Disease relevance of Lu 19005

 

High impact information on Lu 19005

 

Biological context of Lu 19005

 

Anatomical context of Lu 19005

 

Associations of Lu 19005 with other chemical compounds

  • As a first step towards developing such an agent, we established an in vitro assay which selectively detects transporter substrates and used this assay to profile the ability of a lead compound, indatraline, to block the releasing effects of METH and MDMA at the DA, 5-HT, and NE transporters [8].
  • The adaptive effects of 2 weeks treatment with Lu 19-005, on receptor binding in vitro and on d-amphetamine responsiveness in vivo have been investigated in rats [6].
  • Reduction of the extracellular Na+ concentration by introduction of a perfusion media containing 50mM Na+ (with choline replacement) produced an excessive release of DA that could be effectively blocked by nomifensine and Lu 19-005, potent inhibitors of an amine transport carrier [9].
 

Analytical, diagnostic and therapeutic context of Lu 19005

  • Two combinations of indatraline (0.32 and 0.56 mg/kg/day) + buprenorphine (0.10 and 0.18 mg/kg/day) significantly reduced speedball self-administration in comparison to the saline treatment baseline (p <.01-.001), whereas the same doses of each compound alone had no significant effect on speedball-maintained responding [3].

References

  1. Pharmacology in vivo of the phenylindan derivative, Lu 19-005, a new potent inhibitor of dopamine, noradrenaline and 5-hydroxytryptamine uptake in rat brain. Arnt, J., Christensen, A.V., Hyttel, J. Naunyn Schmiedebergs Arch. Pharmacol. (1985) [Pubmed]
  2. Cocaine receptors labeled by [3H]2 beta-carbomethoxy-3 beta-(4-fluorophenyl)tropane. Madras, B.K., Spealman, R.D., Fahey, M.A., Neumeyer, J.L., Saha, J.K., Milius, R.A. Mol. Pharmacol. (1989) [Pubmed]
  3. Effects of indatraline and buprenorphine on self-administration of speedball combinations of cocaine and heroin by rhesus monkeys. Mello, N.K., Negus, S.S. Neuropsychopharmacology (2001) [Pubmed]
  4. Design, synthesis, and monoamine transporter binding site affinities of methoxy derivatives of indatraline. Gu, X.H., Yu, H., Jacobson, A.E., Rothman, R.B., Dersch, C.M., George, C., Flippen-Anderson, J.L., Rice, K.C. J. Med. Chem. (2000) [Pubmed]
  5. Studies of the biogenic amine transporters. XI. Identification of a 1-[2-[bis(4-fluorophenyl)methoxy]ethyl]-4-(3-phenylpropyl)piperazine (GBR12909) analog that allosterically modulates the serotonin transporter. Nightingale, B., Dersch, C.M., Boos, T.L., Greiner, E., Calhoun, W.J., Jacobson, A.E., Rice, K.C., Rothman, R.B. J. Pharmacol. Exp. Ther. (2005) [Pubmed]
  6. Down-regulation of dopamine D-2, 5-HT2 receptors and beta-adrenoceptors in rat brain after prolonged treatment with a new potential antidepressant, Lu 19-005. Nowak, G., Arnt, J., Hyttel, J., Svendsen, O. J. Neural Transm. (1985) [Pubmed]
  7. Active [3H]-dopamine uptake by human lymphocytes: correlates with serotonin transporter activity. Faraj, B.A., Olkowski, Z.L., Jackson, R.T. Pharmacology (1994) [Pubmed]
  8. Neurochemical neutralization of methamphetamine with high-affinity nonselective inhibitors of biogenic amine transporters: a pharmacological strategy for treating stimulant abuse. Rothman, R.B., Partilla, J.S., Baumann, M.H., Dersch, C.M., Carroll, F.I., Rice, K.C. Synapse (2000) [Pubmed]
  9. Influence of a carrier transport process on in vivo release and metabolism of dopamine: dependence on extracellular Na+. Hurd, Y.L., Ungerstedt, U. Life Sci. (1989) [Pubmed]
 
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