1. Dear Drugs-Forum readers: We are a small non-profit that runs one of the most read drug information & addiction help websites in the world. We serve over 4 million readers per month, and have costs like all popular websites: servers, hosting, licenses and software. To protect our independence we do not run ads. We take no government funds. We run on donations which average $25. If everyone reading this would donate $5 then this fund raiser would be done in an hour. If Drugs-Forum is useful to you, take one minute to keep it online another year by donating whatever you can today. Donations are currently not sufficient to pay our bills and keep the site up. Your help is most welcome. Thank you.
    PLEASE HELP

Pharmacological Profile of Neuroleptics at Human Monoamine Transporters

Pharmacological Profile of Neuroleptics at Human Monoamine Transporters

  1. Bajeda
    Tatsumi M, Jansen K, Blakely RD, Richelson E. Eur J Pharmacol. 1999 Mar 5;368(2-3):277-83.

    Using radioligand binding techniques, we determined the equilibrium dissociation constants (KD) 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 (KD 24–39 nM); and at the norepinephrine transporter, chlorpromazine, zotepine, chlorprothixene, and promazine (KD 19–25 nM). At the human dopamine transporter, only pimozide (KD=69±3) ziprasidone (KD=76±5) had notable potency. These data may be useful in predicting therapeutic and adverse effects, including drug interactions of neuroleptics.