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RTI-336: Wikis


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Systematic (IUPAC) name
ATC code  ?
PubChem 9800708
Chemical data
Formula C24H25ClN2O 
Mol. mass 392.920
SMILES eMolecules & PubChem
Therapeutic considerations
Pregnancy cat.  ?
Legal status

RTI-336, (LS-193,309, (-)-2β-(3-(4-methylphenyl)isoxazol-5-yl)-3β-(4-chlorophenyl)tropane) is a phenyltropane derivative which acts as a potent and selective dopamine reuptake inhibitor and stimulant drug. It binds to the dopamine transporter with around 20x the affinity of cocaine,[1] however it produces relatively mild stimulant effects, with a slow onset and long duration of action.[2] These characteristics make it a potential candidate for treatment of cocaine addiction, as a possible substitute drug analogous to how methadone is used for treating heroin abuse.[3][4] RTI-336 fully substitutes for cocaine in addicted monkeys and supports self-administration,[5][6] and significantly reduces rates of cocaine use, especially when combined with SSRIs,[7] and research is ongoing to determine whether it could be a viable substitute drug in human cocaine addicts.

See also


  1. ^ Carroll, F.; Pawlush, N.; Kuhar, M.; Pollard, G.; Howard, J. (2004). "Synthesis, monoamine transporter binding properties, and behavioral pharmacology of a series of 3beta-(substituted phenyl)-2beta-(3'-substituted isoxazol-5-yl)tropanes". Journal of medicinal chemistry 47 (2): 296–302. doi:10.1021/jm030453p. PMID 14711303.  edit
  2. ^ Carroll, F.; Fox, B.; Kuhar, M.; Howard, J.; Pollard, G.; Schenk, S. (2006). "Effects of dopamine transporter selective 3-phenyltropane analogs on locomotor activity, drug discrimination, and cocaine self-administration after oral administration". European journal of pharmacology 553 (1-3): 149–156. doi:10.1016/j.ejphar.2006.09.024. PMID 17067572.  edit
  3. ^ Carroll, F.; Howard, J.; Howell, L.; Fox, B.; Kuhar, M. (2006). "Development of the dopamine transporter selective RTI-336 as a pharmacotherapy for cocaine abuse". The AAPS journal 8 (1): E196–E203. doi:10.1208/aapsj080124. PMID 16584128.  edit
  4. ^ Sofuoglu M, Kosten TR. Emerging pharmacological strategies in the fight against cocaine addiction. Expert Opinion on Emerging Drugs. 2006 Mar;11(1):91-98. doi:10.1517/14728214.11.1.91
  5. ^ Kimmel, H.; O'Connor, J.; Carroll, F.; Howell, L. (2007). "Faster onset and dopamine transporter selectivity predict stimulant and reinforcing effects of cocaine analogs in squirrel monkeys". Pharmacology, biochemistry, and behavior 86 (1): 45–54. doi:10.1016/j.pbb.2006.12.006. PMID 17258302.  edit
  6. ^ Kimmel, H.; Negus, S.; Wilcox, K.; Ewing, S.; Stehouwer, J.; Goodman, M.; Votaw, J.; Mello, N. et al. (2008). "Relationship between rate of drug uptake in brain and behavioral pharmacology of monoamine transporter inhibitors in rhesus monkeys". Pharmacology, biochemistry, and behavior 90 (3): 453–462. doi:10.1016/j.pbb.2008.03.032. PMID 18468667.  edit
  7. ^ Howell, L.; Carroll, F.; Votaw, J.; Goodman, M.; Kimmel, H. (2007). "Effects of combined dopamine and serotonin transporter inhibitors on cocaine self-administration in rhesus monkeys". The Journal of pharmacology and experimental therapeutics 320 (2): 757–765. doi:10.1124/jpet.106.108324. PMID 17105829.  edit


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