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Related Experiment Videos

[Does 'selective binding profile' result in 'selective treatment'?].

T Suzuki1

  • 1Department of Toxicology, School of Pharmacy, Hoshi University, 2-4-41, Ebara, Shinagawa-ku, Tokyo 142-8501, Japan.

Nihon Shinkei Seishin Yakurigaku Zasshi = Japanese Journal of Psychopharmacology
|June 13, 2001
PubMed
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Selective drug targeting does not guarantee selective treatment. Multi-acting-acting-receptor-targeted-antipsychotics (MARTAs) offer broader efficacy for complex conditions like schizophrenia by targeting multiple receptors, improving treatment outcomes.

Area of Science:

  • Psychopharmacology
  • Neuroscience

Context:

  • Traditional antipsychotics targeting single receptors, like dopamine D2, often cause side effects such as extrapyramidal symptoms (EPS).
  • Serotonin-dopamine antagonists show improved efficacy and reduced EPS due to combined 5-HT2A and dopamine D2 antagonism.

Purpose:

  • To evaluate the efficacy of Multi-Acting-Acting-Receptor-Targeted-Antipsychotics (MARTAs) in treating complex psychiatric conditions.
  • To challenge the 'selective binding profile' equals 'selective treatment' paradigm in drug development.

Summary:

  • MARTAs, by antagonizing multiple receptors (5-HT2A, 5-HT2C, alpha 1-adrenergic, muscarinic), disinhibit glutamatergic transmission and reduce positive symptoms.
  • MARTAs' combined receptor antagonism is linked to reduced EPS and potential improvements in negative, anxiety, depressive, and cognitive symptoms often resistant to other treatments.

Related Experiment Videos

  • Increased dopamine and norepinephrine in the prefrontal cortex by MARTAs contribute to improved negative and cognitive symptoms.

    • Impact:

    • Findings suggest that a multi-acting, multi-receptor approach is more effective for complex diseases than single-target strategies.
    • Rethinking single-receptor targeting strategies is crucial for developing breakthrough treatments for refractory diseases.