Screening the receptorome to discover the molecular targets for plant-derived psychoactive compounds: a novel approach for CNS drug discovery

Dopamine and Serotonin Receptor Binding and Antipsychotic Efficacy

“…In order to minimize variability in assay conditions that may lead to differences in K i value for a given receptor (Strange, 2001), drug affinity K i values determined by the NIMH Psychoactive Drug Screening Program (Roth et al, 2004) were used in our analysis. K i values selected for analysis were those listed as NIMH Psychoactive Drug Screening Program assay certified data, determined from assays using the cloned human receptors with drugs of interest as test ligands.…”

“…K i values selected for analysis were those listed as NIMH Psychoactive Drug Screening Program assay certified data, determined from assays using the cloned human receptors with drugs of interest as test ligands. For K i values for which PDSP certified assay data were not listed, the average K i value from assay data compiled on the PDSP web site (Roth et al, 2004) using the cloned human receptor with drug of interest as the test ligand was utilized. K i values from cloned human receptor for three drug/receptor combinations not listed in the PDSP database were identified from published literature.…”

Association Between Antipsychotic Use and Risk of Acute Myocardial Infarction

“…Blood concentration (molar) was estimated by multiplying the mean daily drug concentration (here total human blood volume was assumed to be 5 L) 22 of an antipsychotic by its oral bioavailability, defined as the fraction of an orally administered dose of unaltered drug that would reach systemic circulation after absorption, distribution, metabolism, and elimination. We excluded patients who had received thioridazine, trifluoperazine, loxapine, clothiapine, flupentixol, chlorprothixene, clopenthixol, zuclopenthixol, thiothixene, levomepromazine, and pipotiazine, drugs for which their K d values or bioavailability data are currently unavailable from the National Institute of Mental Health Psychoactive Drug Screening Program 23 and Micromedex Healthcare Series Internet Database (Truven Health Analytics). 24 Therefore, only the receptor-binding profiles (Table II in …”

Studies of the Biogenic Amine Transporters. 13. Identification of “Agonist” and “Antagonist” Allosteric Modulators of Amphetamine-Induced Dopamine Release

“…We note that the possible activity of these compounds at other central nervous system binding sites is currently underway via a screen of the receptorome (Roth et al, 2004). The results will be reported in due course.…”