Sertindole was used to study the role of 5-HT2C receptor in antipsychotic-induced body weight gain in rats.3
生物化学的／生理学的作用
5-HT2 セロトニンおよびD2 ド-パミンレセプタ-アンタゴニストで、統合失調症治療薬です。
Sertindole readily passes the blood-brain barrier and is metabolized into compounds that show greater affinity for 5-HT2 receptors and less for D2 receptors. It is an effective treatment agent for schizophrenia as it improves cognitive impairment.1 Sertindole also acts as antagonist to human cardiac potassium channel, HERG and produces prolonged QT interval.2
特徴および利点
This compound is featured on the Dopamine Receptors page of the Handbook of Receptor Classification and Signal Transduction. To browse other handbook pages, click here.
This compound was developed by Abbott. To browse the list of other pharma-developed compounds and Approved Drugs/Drug Candidates, click here.
International clinical psychopharmacology, 13 Suppl 3, S65-S70 (1998-08-05)
The safety and efficacy of sertindole have been established in three double-blind randomized controlled studies conducted in the United States, North America and Europe. In these three studies the tendency for sertindole to cause extrapyramidal side effects (EPS), a critical
The synthesis and in vitro preclinical profile of a series of 5-heteroaryl substituted analogs of the antipsychotic drug sertindole are presented. Compounds 1-(4-fluorophenyl)-3-(1-methylpiperidin-4-yl)-5-(pyrimidin-5-yl)-1H-indole (Lu AA27122, 3i) and 1-(4-fluorophenyl)-5-(1-methyl-1H-1,2,4-triazol-3-yl)-3-(1-methylpiperidin-4-yl)-1H-indole (3l) were identified as high affinity α(1A)-adrenoceptor ligands with K(i) values of
Journal of clinical psychopharmacology, 32(2), 173-178 (2012-03-01)
Clozapine augmentation with antipsychotic drugs is widely used despite sparse evidence supporting this strategy. Sertindole is a nonsedating atypical antipsychotic drug with low affinity for cholinergic receptors, which makes it potentially suitable for augmentation of clozapine. The study design was
International clinical psychopharmacology, 12 Suppl 1, S29-S35 (1997-02-01)
Evidence from clinical trials supports the claim that sertindole is a potent antipsychotic drug at a dose of 12-24 mg/day. Its action against positive symptoms is as potent as that of the traditional antipsychotic haloperidol. Its action against negative symptoms
Journal of psychopharmacology (Oxford, England), 25(12), 1600-1613 (2011-09-06)
Sensory gating, indexed by P50 suppression, and sensorimotor gating, indexed by prepulse inhibition (PPI), are impaired in schizophrenia spectrum disorders. There is considerable evidence that schizophrenia patients treated with atypical antipsychotics exhibit relatively less gating deficits than do other patients
