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. Copyright (C) 1999 Elsevier Science B.V.
| Original language | English (US) |
|---|---|
| Pages (from-to) | 277-283 |
| Number of pages | 7 |
| Journal | European Journal of Pharmacology |
| Volume | 368 |
| Issue number | 2-3 |
| DOIs | |
| State | Published - Mar 5 1999 |
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Keywords
- 5-HT (5-hydroxy-hyptamine, serotonin), human
- Dopamine transporter, human
- Neuroleptic
- Norepinephrine transporter, human
- Radioligand binding assay
ASJC Scopus subject areas
- Cellular and Molecular Neuroscience
- Pharmacology
Cite this
Pharmacological profile of neuroleptics at human monoamine transporters. / Tatsumi, Masahiko; Jansen, Karen; Blakely, Randy D.; Richelson, Elliott.
In: European Journal of Pharmacology, Vol. 368, No. 2-3, 05.03.1999, p. 277-283.Research output: Contribution to journal › Article
}
TY - JOUR
T1 - Pharmacological profile of neuroleptics at human monoamine transporters
AU - Tatsumi, Masahiko
AU - Jansen, Karen
AU - Blakely, Randy D.
AU - Richelson, Elliott
PY - 1999/3/5
Y1 - 1999/3/5
N2 - 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. Copyright (C) 1999 Elsevier Science B.V.
AB - 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. Copyright (C) 1999 Elsevier Science B.V.
KW - 5-HT (5-hydroxy-hyptamine, serotonin), human
KW - Dopamine transporter, human
KW - Neuroleptic
KW - Norepinephrine transporter, human
KW - Radioligand binding assay
UR - http://www.scopus.com/inward/record.url?scp=0032979135&partnerID=8YFLogxK
UR - http://www.scopus.com/inward/citedby.url?scp=0032979135&partnerID=8YFLogxK
U2 - 10.1016/S0014-2999(99)00005-9
DO - 10.1016/S0014-2999(99)00005-9
M3 - Article
C2 - 10193665
AN - SCOPUS:0032979135
VL - 368
SP - 277
EP - 283
JO - European Journal of Pharmacology
JF - European Journal of Pharmacology
SN - 0014-2999
IS - 2-3
ER -