Reinforcing effect of pseudoephedrine isomers and the mechanism of action.

Article Details

Citation

Wee S, Ordway GA, Woolverton WL

Reinforcing effect of pseudoephedrine isomers and the mechanism of action.

Eur J Pharmacol. 2004 Jun 16;493(1-3):117-25.

PubMed ID
15189772 [ View in PubMed
]
Abstract

It has been proposed that ephedrine and its isomers may have abuse potential. When made available to rhesus monkeys (n = 4) for self-administration, +-pseudoephedrine functioned as a positive reinforcer in all monkeys, as did (-)-pseudoephedrine in two of three monkeys. Pseudoephedrine isomers were 10- to 33-fold less potent than cocaine. In in vitro binding in monkey brain tissue, both isomers had low affinity for dopamine and serotonin transporters by at least 200-fold relative to cocaine, but comparable affinity for norepinephrine transporters. +-Pseudoephedrine also blocked dopamine uptake in 293 hDAT cells with low potency relative to cocaine. When given in vivo +-pseudoephedrine significantly displaced radioligand binding to dopamine transporters with a potency comparable to that in self-administration. Therefore, pseudoephedrine isomers can function as reinforcers and the mechanism at dopamine transporters may underlie this effect. However, pseudoephedrine appears to be a weak reinforcer and may have relatively low abuse potential.

DrugBank Data that Cites this Article

Drugs
Drug Targets
DrugTargetKindOrganismPharmacological ActionActions
Ephedra sinica rootSodium-dependent dopamine transporterProteinHumans
Yes
Negative modulator
Details
Ephedra sinica rootSodium-dependent noradrenaline transporterProteinHumans
Yes
Negative modulator
Details
Ephedra sinica rootSodium-dependent serotonin transporterProteinHumans
Yes
Negative modulator
Details
PseudoephedrineSodium-dependent dopamine transporterProteinHumans
Yes
Inhibitor
Details
PseudoephedrineSodium-dependent noradrenaline transporterProteinHumans
Yes
Inhibitor
Details
PseudoephedrineSodium-dependent serotonin transporterProteinHumans
Yes
Inhibitor
Details
Drug Transporters
DrugTransporterKindOrganismPharmacological ActionActions
PseudoephedrineSodium-dependent dopamine transporterProteinHumans
Unknown
Inhibitor
Details
PseudoephedrineSodium-dependent noradrenaline transporterProteinHumans
Unknown
Inhibitor
Details
PseudoephedrineSodium-dependent serotonin transporterProteinHumans
Unknown
Inhibitor
Details