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Pharmacological profile of neuroleptics at human monoamine transporters.
M Tatsumi, K Jansen, R D Blakely, E Richelson
Mayo Clinic Jacksonville, FL 32224, USA.
European journal of pharmacology 1999 Mar 5
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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.
Citation
M Tatsumi, K Jansen, R D Blakely, E Richelson.
Pharmacological profile of neuroleptics at human monoamine transporters.
European journal of pharmacology.
1999 Mar 5;368(2-3):277-83
Mesh Tags
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
Substances
Antipsychotic Agents
Carrier Proteins
Dibenzazepines
Dibenzothiepins
Dopamine Plasma Membrane Transport Proteins
Membrane Glycoproteins
Membrane Transport Proteins
Nerve Tissue Proteins
Norepinephrine Plasma Membrane Transport Proteins
Piperazines
Recombinant Fusion Proteins
SLC6A2 protein, human
SLC6A4 protein, human
Serotonin Plasma Membrane Transport Proteins
Symporters
Thiazoles
Tritium
Triflupromazine
ziprasidone
Pimozide
zotepine
Cocaine
Imipramine
Chlorpromazine
(1R-(exo,exo))-3-(4-fluorophenyl)-8-methyl-8- azabicyclo(3.2.1)octane-2-carboxylic acid, methyl ester
Fluoxetine
nisoxetine
fluperlapine
PMID: 10193665
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