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Related Experiment Videos

Piperidinyltetralin sigma ligands

P J Gilligan1, A A Kergaye, B M Lewis

  • 1DuPont Merck Pharmaceutical Company, Wilmington, Delaware 19880-0353.

Journal of Medicinal Chemistry
|February 4, 1994
PubMed
Summary
This summary is machine-generated.

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New tetralin derivatives show promise as antipsychotic drugs. Compound 14, a sigma-1 and serotonin 5HT2 receptor antagonist, demonstrated high affinity and efficacy in animal models without causing catalepsy.

Area of Science:

  • Neuroscience
  • Pharmacology
  • Medicinal Chemistry

Background:

  • Sigma receptor ligands are investigated as potential antipsychotic agents due to their influence on dopaminergic pathways.
  • Compound 15 (DuP 734), a dual sigma-1 and serotonin 5HT2 receptor antagonist, is in clinical trials for antipsychotic treatment.

Purpose of the Study:

  • To synthesize and evaluate novel tetralin derivatives, including compound 14, to explore conformational restriction's impact on sigma-1 and 5HT2 receptor binding and in vivo antipsychotic activity.
  • To establish structure-activity relationships for these novel compounds.

Main Methods:

  • Synthesis of tetralin analogs, including a reduced derivative (compound 14).
  • Assessment of binding affinity for sigma-1 and serotonin 5HT2 receptors.

Related Experiment Videos

  • Evaluation of in vivo antipsychotic activity and catalepsy in animal models.

    • Main Results:

    • Compound 14 exhibited high affinity for both sigma-1 and serotonin 5HT2 receptors.
    • Compound 14 demonstrated excellent oral activity in animal models predictive of antipsychotic efficacy.
    • Compound 14 did not induce catalepsy in rats at doses up to 90 mg/kg (oral).

    Conclusions:

    • Conformationally restricted tetralin derivatives, such as compound 14, represent a promising class of potential antipsychotic drugs.
    • Compound 14's profile suggests a favorable therapeutic window, combining receptor antagonism with a lack of motor side effects.