RTI-371
Encyclopedia
3β--2β-[3-(4-chlorophenyl)isoxazol-5-yl]tropane (RTI-371) is a phenyltropane
derived drug which acts as a potent and selective dopamine reuptake inhibitor
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. Recently the second of these hypotheses was suggested for this compound when it was discovered that RTI-371 also acts as a positive allosteric modulator of the hCB1
human cannabinoid receptor.
Phenyltropane
Phenyltropanes 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, they are not the only researchers that have prepared these...
derived drug which acts as a potent and selective dopamine reuptake inhibitor
Dopamine reuptake inhibitor
A dopamine reuptake inhibitor is a type of drug that acts as a reuptake inhibitor for the neurotransmitter dopamine by blocking the action of the dopamine transporter...
in vitro, yet unusually for this class of compound, both RTI-371 and the closely related compound RTI-370 failed to produce locomotor stimulation
Stimulant
Stimulants are psychoactive drugs which induce temporary improvements in either mental or physical function or both. Examples of these kinds of effects may include enhanced alertness, wakefulness, and locomotion, among others...
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
Blood-brain barrier
The blood–brain barrier is a separation of circulating blood and the brain extracellular fluid in the central nervous system . It occurs along all capillaries and consists of tight junctions around the capillaries that do not exist in normal circulation. Endothelial cells restrict the diffusion...
penetration, or interactions at alternative receptor sites. Recently the second of these hypotheses was suggested for this compound when it was discovered that RTI-371 also acts as a positive allosteric modulator of the hCB1
Cannabinoid receptor type 1
The cannabinoid receptor type 1, often abbreviated to CB1, is a G protein-coupled cannabinoid receptor located in the brain. It is activated by endocannabinoid neurotransmitters including anandamide and by the compound THC, found in the psychoactive drug cannabis.-Expression:The CB1 receptor is...
human cannabinoid receptor.