European Journal of Pharmacology: Molecular Pharmacology
Deriving the therapeutic concentrations for clozapine and haloperidol: The apparent dissociation constant of a neuroleptic at the dopamine D2 or D4 receptor varies with the affinity of the competing radioligand
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Rationale and neurobiological effects of treatment with antipsychotics in patients with chronic schizophrenia considering dopamine supersensitivity
2021, Behavioural Brain ResearchCitation Excerpt :The main mechanism of clozapine action has been proposed to be either a higher affinity receptor rate of 5-HT2A/DRD2, which is an atypical profile of the most extreme nature, and/or a faster dissociation from DRD2s [8,150]. The action of its main active metabolite (norclozapine) and the blockade of DRD4 by clozapine have been also discussed [151–153]. Despite these extensive studies and discussions, it remains uncertain whether these factors are involved in the efficacy of clozapine.
In vivo temporal EPR study using a region-selected intensity determination method to estimate cerebral reducing ability in rats treated with olanzapine
2010, Magnetic Resonance ImagingCitation Excerpt :HPD shows a high affinity for D2 receptors, so HPD administration prompts dopamine turnover because of occupancy of D2 receptors by the neuroleptic [9,10,13,14]. A novel atypical neuroleptic, olanzapine (OZP), has a favorable side-effect profile, with minimal EPS, because of lower affinity for D2 receptors [14–17]. However, acute administration of OZP causes an increase in dopamine turnover, which is considered to reflect enhancement of intracerebral dopamine release [18].
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