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Phenyltropanes (PTs) are a class of cocaine-like psychoactive stimulants.
Phenyltropane compounds comprise a large family of related molecules, developed during research into the mechanism of action of certain kinds of drugs such as cocaine and other dopamine reuptake inhibitors, which in general act as inhibitors of the monoamine reuptake transporters. Different molecules in this family may be selective for a particular transporter such as the dopamine, noradrenaline or serotonin transporter, or may be non-selective and inhibit reuptake of all three monoamines.
Uses
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.
Phenyltropanes are also widely used in animal studies of drug addiction as they share the stimulant properties and reinforcing effects of cocaine, but with higher potency, less non-specific binding which avoids the cardiotoxicity associated with cocaine, and are legal in most jurisdictions which avoids the complex licensing issues involved with the legal use of cocaine in scientific research.
Some phenyltropane derivatives have also been researched for medical use in the treatment of conditions such as Parkinson's Disease and depression, or as potential substitute drugs in the treatment of cocaine addiction, and their strong appetite suppressant effects makes them promising candidates for facilitating weight loss in the treatment of obesity.
Examples
Prominent examples of phenyltropane derived drugs used in scientific research (and with some medical applications) include;
- β-CFT (WIN 35,428)
- β-CIT (RTI-55)
- Dichloropane (RTI-111)
- RTI-121 (IPCIT)
- Tesofensine (relatively weak stimulant but retains strong appetite suppressant effects, currently in clinical trials for weight loss)
- Troparil (β-CPT, WIN 35,065-2)
Wikipedia content modification information:
- This page was last modified on 1 July 2008, at 03:10.
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