Posted by SLS on April 1, 2010, at 19:02:07
In reply to Re: - Interesting Antipsychotic, posted by desolationrower on March 31, 2010, at 21:14:22
> i think most atypicals antagonise andrenoceptors to some extent
>
> -d/r
Life Sci. 2000 Nov 24;68(1):29-39.
Binding of antipsychotic drugs to human brain receptors focus on newer generation compounds.Richelson E, Souder T.
Department of Psychiatry and Psychology, and Pharmacology, Mayo Foundation for Medical Education and Research and Mayo Clinic, Jacksonville, FL 32224, USA. richel@mayo.edu
Using radioligand binding assays and post-mortem normal human brain tissue, we obtained equilibrium dissociation constants (K(d)s) for nine new antipsychotic drugs (iloperidone, melperone, olanzapine, ORG 5222, quetiapine, risperidone, sertindole, ziprasidone, and zotepine), one metabolite of a new drug (9-OH-risperidone), and three older antipsychotics (clozapine, haloperidol, and pimozide) at nine different receptors (alpha1-adrenergic, alpha2-adrenergic, dopamine D2, histamine H1, muscarinic, and serotonin 5-HT1A, 5-HT1D, 5-HT2A, and 5-HT2C receptors). Iloperidone was the most potent drug at the two adrenergic receptors. ORG 5222 was the most potent drug at dopamine D2 and 5-HT2c receptors, while ziprasidone was the most potent compound at three serotonergic receptors (5-HT1A, 5-HT1D, and 5-HT2A). At the remaining two receptors, olanzapine was the most potent drug at the histamine H1 receptor (Kd=0.087 nM); clozapine at the muscarinic receptor (Kd=9 nM). Certain therapeutic and adverse effects, as well as certain drug interactions can be predicted from a drug's potency for blocking a specific receptor. These data can provide guidelines for the clinician in the choice of antipsychotic drug.
poster:SLS
thread:939163
URL: http://www.dr-bob.org/babble/neuro/20100223/msgs/941675.html