Document Detail

What are the optimal pharmacokinetic properties of antipsychotic medications?
MedLine Citation:
PMID:  21896301     Owner:  NLM     Status:  Publisher    
Sensitization of the dopaminergic system has been proposed as a pathogenic mechanism of psychosis. It has been reported in sensitized animals that the proportion of high-affinity dopamine 2 (D(2)) receptors is increased, without changes in the total amount of D(2) receptors. This increase induces an exaggerated postsynaptic transmission of the dopamine signal, which is attenuated by antipsychotic D(2) antagonists. In this report, I simulated D(2) receptor binding of dopamine and antipsychotics under pathologic state, and investigated pharmacological conditions that would return the increased dopamine binding back to normal levels in both resting and burst dopamine concentrations. I found that D(2) antagonists with small Koff values at a concentration 2.5 times the Ki closely mimicked normal dopamine binding. Under these conditions, the apparent receptor occupancy of the drug was calculated as 70%.
Ung Gu Kang
Publication Detail:
Type:  JOURNAL ARTICLE     Date:  2011-8-28
Journal Detail:
Title:  Progress in neuro-psychopharmacology & biological psychiatry     Volume:  -     ISSN:  1878-4216     ISO Abbreviation:  -     Publication Date:  2011 Aug 
Date Detail:
Created Date:  2011-9-7     Completed Date:  -     Revised Date:  -    
Medline Journal Info:
Nlm Unique ID:  8211617     Medline TA:  Prog Neuropsychopharmacol Biol Psychiatry     Country:  -    
Other Details:
Languages:  ENG     Pagination:  -     Citation Subset:  -    
Copyright Information:
Copyright © 2011 Elsevier Inc. All rights reserved.
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