Pharmacological profile of neuroleptics at human monoamine transporters.

Tatsumi M, Jansen K, Blakely RD, Richelson E
Eur J Pharmacol. 1999 368 (2-3): 277-83

PMID: 10193665 · DOI:10.1016/s0014-2999(99)00005-9

Using radioligand binding techniques, we determined the equilibrium dissociation constants (K(D)) for 37 neuroleptics and one metabolite of a neuroleptic (haloperidol metabolite) for the human serotonin, norepinephrine, and dopamine transporters with [3H]imipramine, [3H]nisoxetine, and [3H]WIN35428, respectively. Among neuroleptics, the four most potent compounds at the human serotonin transporter were triflupromazine, fluperlapine, chlorpromazine, and ziprasidone (K(D) 24-39 nM); and at the norepinephrine transporter, chlorpromazine, zotepine, chlorprothixene, and promazine (K(D) 19-25 nM). At the human dopamine transporter, only pimozide (K(D) = 69+/-3) ziprasidone (K(D) = 76+/-5) had notable potency. These data may be useful in predicting therapeutic and adverse effects, including drug interactions of neuroleptics.

MeSH Terms (25)

Antipsychotic Agents Carrier Proteins Cell Line Chlorpromazine Cocaine Dibenzazepines Dibenzothiepins Dopamine Plasma Membrane Transport Proteins Fluoxetine Humans Imipramine Membrane Glycoproteins Membrane Transport Proteins Nerve Tissue Proteins Norepinephrine Plasma Membrane Transport Proteins Pimozide Piperazines Protein Binding Radioligand Assay Recombinant Fusion Proteins Serotonin Plasma Membrane Transport Proteins Symporters Thiazoles Triflupromazine Tritium

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