SERTINDOLE

Names

[ Name ]:
SERTINDOLE

[Synonym ]:
1-[2-[4-[5-chloro-1-(4-fluorophenyl)indol-3-yl]piperidin-1-yl]ethyl]imidazolidin-2-one
1-(2-{4-[5-Chloro-1-(4-fluorophenyl)-1H-indol-3-yl]-1-piperidinyl}ethyl)-2-imidazolidinone
1-[2-[4-[5-chloro-1-(p-fluorophenyl)indol-3-yl]piperidino]ethyl]-2-imidazolidinone
1-[2-[4-[5-chloro-1-(4-fluorophenyl)-1h-indol-3-yl]-1-piperidinyl]ethyl]-2-imidazolidinone
2-Imidazolidinone, 1-[2-[4-[5-chloro-1-(4-fluorophenyl)-1H-indol-3-yl]-1-piperidinyl]ethyl]-
2-Imidazolidinone, 1-[2-[4-[5-chloro-1-(4-fluorophenyl)-1H-indol-3-yl]-1-piperidinyl]ethyl]
1-(2-{4-[5-Chloro-1-(4-fluorophenyl)-1H-indol-3-yl]piperidin-1-yl}ethyl)imidazolidin-2-one
MFCD00867749
Sertindole

Biological Activity

[Description]:

Sertindole, a neuroleptic, is one of the newer antipsychotic medications available.Target: Multi-targetIn vitro studies showed that sertindole exerts a potent antagonism at serotonin 5-HT2A, 5-HT2C, dopamine D2, and αl adrenergic receptors. Sertindole offers an alternative treatment option for refractory patients given its good EPS profile, favorable metabolic profile, and comparable efficacy to risperidone. Due to cardiovascular safety concerns, sertindole is available as a second-line choice for patients intolerant to other antipsychotic agents [1]. Sertindole should prove to be a very useful addition to the therapeutic options available for the treatment of psychotic disorders [2]. Sertindole improves negative symptoms, and is also effective for the treatment of neuroleptic-resistant schizophrenia. Sertindole is generally well tolerated and is associated with a low rate of extrapyramidal symptoms (EPS). Thus, sertindole is a useful option in the treatment of patients with schizophrenia [3].

[Related Catalog]:

Signaling Pathways >> GPCR/G Protein >> 5-HT Receptor

Signaling Pathways >> Neuronal Signaling >> 5-HT Receptor

Signaling Pathways >> Autophagy >> Autophagy

Signaling Pathways >> GPCR/G Protein >> Dopamine Receptor

Signaling Pathways >> Neuronal Signaling >> Dopamine Receptor

Research Areas >> Neurological Disease

[References]

[1]. Juruena, M.F., E.P. de Sena, and I.R. de Oliveira, Sertindole in the management of schizophrenia. J Cent Nerv Syst Dis, 2011. 3: p. 75-85.

[2]. Kane, J.M. and C.A. Tamminga, Sertindole (Serdolect): preclinical and clinical findings of a new atypical antipsychotic. Expert Opin Investig Drugs, 1997. 6(11): p. 1729-41.

[3]. Murdoch, D. and G.M. Keating, Sertindole : a review of its use in schizophrenia. CNS Drugs, 2006. 20(3): p. 233-55.

[Related Small Molecules]

Chemical & Physical Properties

[ Density]:
1.4±0.1 g/cm3

[ Boiling Point ]:
592.1±50.0 °C at 760 mmHg

[ Melting Point ]:
95-100ºC

[ Molecular Formula ]:
C₂₄H₂₆ClFN₄O

[ Molecular Weight ]:
440.941

[ Flash Point ]:
311.9±30.1 °C

[ Exact Mass ]:
440.177917

[ PSA ]:
40.51000

[ LogP ]:
5.26

[ Appearance of Characters ]:
off-white

[ Vapour Pressure ]:
0.0±1.7 mmHg at 25°C

[ Index of Refraction ]:
1.671

[ Storage condition ]:
2-8°C

[ Water Solubility ]:
DMSO: >10mg/mL

Safety Information

[ Symbol ]:

GHS07

[ Signal Word ]:
Warning

[ Hazard Statements ]:
H315-H319-H335-H413

[ Precautionary Statements ]:
P261-P305 + P351 + P338

[ Personal Protective Equipment ]:
dust mask type N95 (US);Eyeshields;Gloves

[ Hazard Codes ]:
Xi: Irritant;

[ Risk Phrases ]:
36/37/38

[ Safety Phrases ]:
26

[ RIDADR ]:
NONH for all modes of transport

[ RTECS ]:
NJ0621100

Synthetic Route

Click to get detail synthetic route

Precursor & DownStream

Precursor

DownStream

Articles

An investigation of the stability of emerging new psychoactive substances.

Drug Test. Anal. 6(7-8) , 696-704, (2014)

The evolving nature of new psychoactive substances (NPS) - often referred to as 'legal highs', 'designer drugs' or 'bath salts' - presents an evolving challenge for toxicologists. Apart from the detec...

Differential effects of blockade of ERG channels on gamma oscillations and excitability in rat hippocampal slices.

Eur. J. Neurosci. 36(12) , 3628-35, (2012)

Agents such as sertindole and astemizole affect heart action by inducing long-QT syndrome, suggesting that apart from their neuronal actions through histamine receptors, 5-HT2 serotonin receptors and ...

Risperidone versus other atypical antipsychotics for schizophrenia.

Cochrane Database Syst. Rev. (1) , CD006626, (2011)

In many countries of the industrialised world second-generation ("atypical") antipsychotics (SGAs) have become the first line drug treatment for people with schizophrenia. The question as to whether a...