Synthesis, dopamine and serotonin transporter binding affinities of novel analogues of meperidine.

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Citation

Lomenzo SA, Izenwasser S, Gerdes RM, Katz JL, Kopajtic T, Trudell ML

Synthesis, dopamine and serotonin transporter binding affinities of novel analogues of meperidine.

Bioorg Med Chem Lett. 1999 Dec 6;9(23):3273-6.

PubMed ID
10612583 [ View in PubMed
]
Abstract

A series of meperidine analogues was synthesized and the binding affinities for the dopamine and serotonin transporters were determined. The substituents on the phenyl ring greatly influenced the potency and selectivity of these compounds for the transporter binding sites. In general, meperidine (3) and its analogues were more selective for serotonin transporter binding sites and the esters 9 were more potent than the corresponding nitriles 8. The 3,4-dichloro derivative 9e was the most potent ligand of the series for dopamine transporter binding sites while the 2-naphthyl derivative 9g exhibited the most potent binding affinity and was highly selective for serotonin transporter binding sites.

DrugBank Data that Cites this Article

Drug Targets
DrugTargetKindOrganismPharmacological ActionActions
MeperidineSodium-dependent dopamine transporterProteinHumans
Unknown
Inhibitor
Details