Pharmacological profile of neuroleptics at human monoamine transporters.

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Tatsumi M, Jansen K, Blakely RD, Richelson E

Pharmacological profile of neuroleptics at human monoamine transporters.

Eur J Pharmacol. 1999 Mar 5;368(2-3):277-83.

PubMed ID

10193665 [ View in PubMed

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Abstract

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.

DrugBank Data that Cites this Article

Drug Targets

Drug	Target	Kind	Organism	Pharmacological Action	Actions
Imipramine	Sodium-dependent noradrenaline transporter	Protein	Humans	Yes	Inhibitor	Details