Atypicality of several antipsychotics on the basis of in vivo dopamine-D2 and serotonin-5HT2 receptor occupancy
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Cited by (58)
Imidazopyridine-based selective and multifunctional ligands of biological targets associated with psychiatric and neurodegenerative diseases
2019, European Journal of Medicinal ChemistryCitation Excerpt :This compound contains a fully saturated imidazo[1,2-a]pyridine core. In addition to targeting dopamine receptors, it also binds to 5-HT2ARs, thus expending a concept of atypical antipsychotics [92,93]. Since the imidazopyridine-derived core is unlikely to be a key fragment for interaction with dopamine receptor, the main pharmacophore is attributed to a 7-membered nitrogen-containing ring.
In vivo 5-HT <inf>6</inf> receptor occupancy by antipsychotic drugs in the rat brain
2011, Neuroscience LettersAntipsychotic drugs dose-dependently suppress the spontaneous hyperactivity of the chakragati mouse
2010, NeuroscienceCitation Excerpt :The drugs administered were vehicle, haloperidol (0.03, 0.1, 0.3, 1 and 3 mg/kg), pimozide (0.03, 0.1, 0.3, 1 and 3 mg/kg), risperidone (0.01, 0.03, 0.1, 0.3 and 1 mg/kg), clozapine (0.1, 0.3, 1, 3 and 10 mg/kg), olanzapine (0.6, 2, 6 and 20 mg/kg), ziprasidone (1, 3, 10, 30 and 100 mg/kg), quetiapine (6, 20, 60 and 200 mg/kg) or aripiprazole (1.67, 3, 5, 10, 15 and 30 mg/kg). As the pharmacokinetics of antipsychotics differ in rodents and humans, doses of the test compounds were selected to include doses that would approximate to 60–80% maximal D2 receptor occupancy in the rodent and thus correspond to receptor occupancy on human clinical dosing (Assié et al., 2006; Kapur et al., 2003; Sumiyoshi et al., 1995): 0.03–1 mg/kg haloperidol, 3 mg/kg pimozide, 1 mg/kg risperidone, 10 mg/kg clozapine, 2 mg/kg olanzapine, 1 mg/kg ziprasidone, 20 mg/kg quetiapine and 5 mg/kg aripiprazole. Haloperidol, pimozide, risperidone and clozapine were tested in the first batch of 32 ckr mice and olanzapine, ziprasidone, quetiapine and aripiprazole were tested in the second batch of 26 ckr mice.
A new approach to antischizophrenic therapeutics: D2 dopamine receptor partial agonists
2009, Annales Pharmaceutiques Francaises
- 1
From the Department of Neuropsychiatry (TS, KS, HS, NY) of Kanazawa, University School of Medicine, Kanazawa 920, Japan
- 2
Radioisotope Center (HM, KS) of Kanazawa, University School of Medicine, Kanazawa 920, Japan
- 3
Hospitals Pharmacy (KY) of Kanazawa, University School of Medicine, Kanazawa 920, Japan