Сертиндол

Описание

Serdolect was launched in the UK for acute and chronic schizophrenia and schizoaffective psychoses. It is synthetically available in three steps from 5chloro-l- (4-fluorophenyl)-l H-indole. Sertindole is selective for the limbic areas of the brain and has a high affinity for the serotinin 5-HT₂ receptor where it behaves as an antagonist. It has weak affinity for the α₁-adrenergic receptor and no affinity for dopamine D₂ receptors. It is as effective as haloperidol but without the extrapyramidal symptoms. This may be a consequence of the fact that it expresses the c-fos protein in a manner different for haloperidol but similar to clozapine. It is non-sedating, long lasting (several days after a single dose) and has an atypical mode of action.

Химические свойства

Off-White to Pale Yellow Solid

Использование

Antipsychotic used in the treatment of schizophrenia.

Определение

ChEBI: A phenylindole that is 1H-indole which is substituted on the nitrogen by a p-chlorophenyl group, at position 5 by chlorine, and at position 3 by a piperidin-4-yl group, which is itself substituted on the nitrogen by a 2-(2-o oimidazolidin-1-yl)ethyl group.

Побочные эффекты

Sertindole is an indole-containing compound that behaves as a high-affinity serotonin 5-HT2 receptor antagonist, with weak affinity for adrenergic α1 receptors and almost no affinity for dopaminergic D2 receptors. It is about as effective as haloperidol in the treatment of acute and chronic schizophrenia, but with much lower incidence of extrapyramidal side effects. Sertindole is relatively nonsedating, and its effects are long lasting (several days).