3β-(4-Methylphenyl)-2β-
-(4-chlorophenyl)isoxazol-5-ylropane (RTI-''4229''-371) is a
phenyltropane
Phenyltropanes (PTs) were originally developed to reduce cocaine addiction and dependency. In general these compounds act as inhibitors of the plasmalemmal monoamine reuptake transporters. Although RTI holds a strong position in this field, ...
derived drug which acts as a potent and selective
dopamine reuptake inhibitor
A dopamine reuptake inhibitor (DRI) is a class of drug which acts as a reuptake inhibitor of the monoamine neurotransmitter dopamine by blocking the action of the dopamine transporter (DAT). Reuptake inhibition is achieved when extracellular dop ...
''in vitro'', yet unusually for this class of compound, both RTI-371 and the closely related compound
RTI-370 failed to produce
locomotor stimulation in mice. In addition to this, in drug substitution tests RTI-370 weakly generalized to cocaine whereas RTI-371 did not generalize at all.
This phenomenon has also been observed for other dopamine reuptake inhibitors from other classes. It may be caused by lack of
BBB penetration, or interactions at alternative receptor sites.
See also
*
List of cocaine analogues
This is a list of cocaine analogues. A cocaine analogue is an (usually) artificial construct of a novel chemical compound from (often the starting point of natural) cocaine's molecular structure, with the result product sufficiently similar to co ...
*
List of phenyltropanes
References
{{Dopaminergics
Chloroarenes
Tropanes
RTI compounds
Dopamine reuptake inhibitors
Sympathomimetic amines
Isoxazoles