Pharmacological MRI responses of raclopride in rats: The relationship with D2 receptor occupancy and cataleptic behavior

Synapse ◽  
2020 ◽  
Vol 74 (12) ◽  
Author(s):  
Yukiko Masaki ◽  
Yuto Kashiwagi ◽  
Takemi Rokugawa ◽  
Miwa Ito ◽  
Hitoshi Iimori ◽  
...  
Keyword(s):  
D2 Receptor ◽  
Receptor Occupancy ◽  
Pharmacological Mri ◽  
The Relationship

Antipsychotic efficacy: Relationship to optimal D2-receptor occupancy

2007 ◽  
Vol 22 (5) ◽  
pp. 267-275 ◽  
Author(s):  
Luca Pani ◽  
Luigi Pira ◽  
Giorgio Marchese
Keyword(s):  
Atypical Antipsychotics ◽  
D2 Receptor ◽  
Receptor Occupancy ◽  
Antipsychotic Agents ◽  
Therapeutic Window ◽  
Therapeutic Effects ◽  
Preclinical Models ◽  
Biochemical Interaction ◽  
The Relationship ◽  
The Brain

AbstractClinically important differences exist between antipsychotic agents and formulations in terms of safety and tolerability. Features of the biochemical interaction between the antipsychotic and the D2-receptor may underlie these differences. This article reviews current information on the relationship between antipsychotic receptor occupancy and clinical response. A literature search was performed using the keywords ‘antipsychotic or neuroleptic’, ‘receptor’ and ‘occupancy’ and ‘dopamine’ and ‘D2’ supplemented by the authors’ knowledge of the literature. Imaging and clinical data have generally supported the hypotheses that optimal D2-receptor occupancy in the striatum lies in a ‘therapeutic window’ between ∼65 and ∼80%, however, pharmacokinetic and pharmacodynamic properties of a drug should also be taken into account to fully evaluate its therapeutic effects. Additional research, perhaps in preclinical models, is needed to establish D2-receptor occupancy in various regions of the brain and the optimal duration of D2-receptor blockade in order to maximise efficacy and tolerability profiles of atypical antipsychotics and thereby improve treatment outcomes for patients with schizophrenia.

A cross-validation study on the relationship between central D2 receptor occupancy and serum perphenazine concentration

2004 ◽  
Vol 175 (2) ◽  
pp. 148-153 ◽  
Author(s):  
Mirjam Talvik ◽  
Anna-Lena Nordström ◽  
Niels-Erik Larsen ◽  
Aurelija Jucaite ◽  
Simon Červenka ◽  
...  
Keyword(s):  
Validation Study ◽  
Cross Validation ◽  
D2 Receptor ◽  
Receptor Occupancy ◽  
The Relationship

Risperidone and the relationship between D2 receptor occupancy and plasma levels

1996 ◽  
Vol 6 ◽  
pp. 74 ◽  
Author(s):  
G. Remington ◽  
S. Kapur ◽  
C. Jones ◽  
R. Zipursky ◽  
S. Houle
Keyword(s):  
Plasma Levels ◽  
D2 Receptor ◽  
Receptor Occupancy ◽  
The Relationship

scholarly journals High dose antipsychotic polypharmacy and dopamine partial agonists - time to rethink guidelines?

2021 ◽  
pp. 026988112110264
Author(s):  
Gavin P Reynolds
Keyword(s):  
Side Effects ◽  
Dopamine D2 Receptor ◽  
D2 Receptor ◽  
Receptor Site ◽  
Receptor Occupancy ◽  
Antipsychotic Agents ◽  
High Dose ◽  
Partial Agonists ◽  
Favourable Side Effect Profile ◽  
Different Characteristics

Guidelines for the treatment of schizophrenia limit the use of antipsychotic agents to clinically-established maximum doses. This acknowledges both the absence of additional efficacy of dopamine D2 receptor antagonists above a receptor occupancy threshold, and the increases in side effects that can occur at higher doses. These limits restrict the dosing of combinations of antipsychotics as they do single agents; drugs sharing the major antipsychotic mechanism of D2 receptor antagonism will act additively in blocking these receptors. Several newer antipsychotic drugs, including aripiprazole and cariprazine, act as partial agonists at the D2 receptor site and avoid action at several other receptors, effects at which are responsible for some non-dopaminergic adverse effects. This pharmacology imparts different characteristics to the drugs resulting often in a more favourable side effect profile. Their partial agonism, along with high affinities for the D2 receptor, also means that these drugs given adjunctively may in part replace, rather than enhance, the D2 antagonism of other antipsychotic agents. This can result in an improvement in certain side effects without loss of antipsychotic efficacy. This article makes the case for distinguishing the D2 partial agonists from antagonists in defining maximum doses of combined treatments, which would increase the options available to the prescriber, emphasising that pharmacological mechanisms need to be understood in identifying optimal treatments for psychotic illness.

Striatal D2 receptor occupancy in bipolar patients treated with olanzapine

2007 ◽  
Vol 17 (2) ◽  
pp. 102-107 ◽  
Author(s):  
Trawat Attarbaschi ◽  
Julia Sacher ◽  
Thomas Geiss-Granadia ◽  
Nikolas Klein ◽  
Nilufar Mossaheb ◽  
...  
Keyword(s):  
D2 Receptor ◽  
Receptor Occupancy ◽  
Bipolar Patients

Dopamine D2 Receptor Occupancy as a Predictor of Catalepsy in Rats: A Pharmacokinetic-Pharmacodynamic Modeling Approach

2014 ◽  
Vol 31 (10) ◽  
pp. 2605-2617 ◽  
Author(s):  
Martin Johnson ◽  
Magdalena Kozielska ◽  
Venkatesh Pilla Reddy ◽  
An Vermeulen ◽  
Hugh A. Barton ◽  
...  
Keyword(s):  
Dopamine D2 Receptor ◽  
D2 Receptor ◽  
Receptor Occupancy ◽  
Pharmacodynamic Modeling ◽  
Modeling Approach ◽  
Dopamine D2 ◽  
Dopamine D2 Receptor Occupancy

The relationship between D 2 receptor occupancy and plasma levels on low dose oral haloperidol: a PET study

1997 ◽  
Vol 131 (2) ◽  
pp. 148-152 ◽  
Author(s):  
Shitij Kapur ◽  
Robert Zipursky ◽  
Paul Roy ◽  
Corey Jones ◽  
Gary Remington ◽  
...  
Keyword(s):  
Plasma Levels ◽  
Low Dose ◽  
Receptor Occupancy ◽  
Dose Oral ◽  
The Relationship
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