Characterization of binding of antipsychotics to muscarinic receptors using mouse cerebral cortex.
J Pharmacol Sci
; 140(2): 197-200, 2019 Jun.
Article
em En
| MEDLINE
| ID: mdl-31178327
ABSTRACT
Antipsychotics are often the first-line treatment for behavioral and psychological symptoms of dementia. However, the potential anticholinergic effects of antipsychotics could counteract the therapeutic effects of cholinesterase inhibitors used to treat dementia. We investigated the inhibitory effects of 26 antipsychotics on [N-Methyl-3H]scopolamine specific binding in mouse cerebral cortex. At 10-5 M, chlorpromazine, levomepromazine, prochlorperazine, timiperone, zotepine, pimozide, blonanserin, olanzapine, quetiapine, and clozapine inhibited [N-Methyl-3H]scopolamine binding by > 45%. Furthermore, the pKi values of chlorpromazine, levomepromazine, zotepine, olanzapine, and clozapine overlapped with their clinically achievable blood concentrations. Therefore, the anticholinergic properties of these antipsychotics could attenuate the effects of cholinesterase inhibitors.
Palavras-chave
Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Escopolamina
/
Antipsicóticos
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Córtex Cerebral
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Inibidores da Colinesterase
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Receptores Muscarínicos
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Antagonistas Colinérgicos
Limite:
Animals
Idioma:
En
Ano de publicação:
2019
Tipo de documento:
Article