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E-5842 (Laboratories Dr Esteve).

S Beckett1

  • 1Neuroscience & Pharmacology Group, School of Biomedical Sciences, Faculty of Medicine & Health Sciences, Queens Medical Centre, Nottingham University, Nottingham, UK. Simon.Beckett@nottingham.ac.uk

Idrugs : the Investigational Drugs Journal
|August 13, 2005
PubMed
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Esteve is developing E-5842, a sigma1 opioid receptor ligand, for psychosis treatment. Preclinical studies show it acts as an atypical antipsychotic, potentially through phosphoinositide signaling pathways.

Area of Science:

  • Neuroscience
  • Pharmacology

Background:

  • Esteve is developing E-5842, a sigma1 opioid receptor ligand.
  • E-5842 has completed Phase I clinical trials.
  • Phase II trials for schizophrenia were scheduled to begin in the UK.

Purpose of the Study:

  • To evaluate E-5842 as a potential therapy for psychosis.
  • To investigate the preclinical neurochemical and behavioral effects of E-5842.

Main Methods:

  • Administered E-5842 acutely (40 mg/kg) and chronically (20 mg/kg).
  • Assessed E-5842's effects on phosphoinositide-specific phospholipase C (PLC) activity.
  • Determined E-5842's binding affinity (K(i)) at the sigma receptor.
  • Evaluated E-5842's antagonism of apomorphine- and amphetamine-induced behaviors in mice.

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Main Results:

  • E-5842 demonstrated atypical antipsychotic activity in preclinical tests.
  • Both acute and chronic E-5842 administration increased PLC activity.
  • E-5842 has a high affinity (4 nM K(i)) for the sigma receptor.
  • E-5842 blocked apomorphine-induced climbing and antagonized amphetamine-induced hyperactivity.

Conclusions:

  • E-5842's antipsychotic effects may involve a signaling pathway utilizing phosphoinositide second messengers.
  • E-5842 shows promise as a novel antipsychotic agent.