Phenyltropane

The phenyltropane compounds were initially discovered by R. Clarke et al. during research to try and dissociate the stimulant properties of cocaine from its abuse and dependence liability.

[9] Animal studies on monkeys and rats have tried to assess the self-administration propensity of phenyltropane analogs alongside cocaine.

Frequently the analogs are administered prior to the start of a session to see if they can suppress cocaine lever responding.

In particular, they tend to stimulate locomotor activity, and cause nonselective reductions in cocaine intake relative to food.

Most of the analogs will readily substitute for cocaine, although most do not elicit as many lever responses per session because of pharmacokinetic factors.

Most modern research suggests that 5-HT is negatively correlated with the addiction forming potential of psychostimulants, this is not saying that SRI properties cannot be considered beneficial.

What was somewhat interesting is that although the reason for the lack of reinforcement of RTI-112 is now well established, closely related RTI-111 was able to behave in ways that might be typical for a nonselective SNDRI such as cocaine.

Hence, it should be borne in mind that these neurotransmitters are unlikely to be involved in the addiction forming properties of cocaine and related stimulants.

Hence, selective NRIs such as atomoxetine are able to increase the concentration of supracellular (synaptic) DA in this brain region via NET blockade.

[16] Weeding out SERT and NET affinity is desirable in the context that these molecular targets are less relevant to the goals of the treatment program, which is to reduce cocaine intake.

These compounds are primarily used in scientific research, as their high binding affinity for monoamine transporters, and the wide range of radiolabelled phenyltropane compounds available with different binding specificities makes them very useful for mapping the distribution of the various monoamine transporters in the brain.