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Related Experiment Videos

TIPP[psi], a highly selective delta ligand

L M Visconti1, K M Standifer, P W Schiller

  • 1Cotzias Laboratory of Neuro-Oncology, Memorial Sloan-Kettering Cancer Center, New York, NY 10021.

Neuroscience Letters
|November 7, 1994
PubMed
Summary
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TIPP[psi] is a highly delta-selective opioid peptide antagonist. Its superior selectivity over mu and kappa receptors enables development of an improved mu 1 binding assay.

Area of Science:

  • Pharmacology
  • Neuroscience
  • Biochemistry

Background:

  • Opioid receptors (mu, delta, kappa) are critical targets for pain management.
  • Developing selective antagonists is crucial for targeted therapeutic interventions.
  • TIPP[psi] is a novel delta-selective opioid peptide antagonist.

Purpose of the Study:

  • To characterize the receptor selectivity profile of TIPP[psi].
  • To compare TIPP[psi]'s selectivity with other delta-selective compounds.
  • To develop an improved mu 1 binding assay utilizing TIPP[psi]'s properties.

Main Methods:

  • Radioligand binding assays were performed using [3H]DPDPE.
  • TIPP[psi] and DPDPE were tested against delta, mu (1 and 2), and kappa (1, 2, and 3) receptor subtypes.

Related Experiment Videos

  • Inhibition constants (Ki) were determined to quantify binding affinity and selectivity.

    • Main Results:

    • TIPP[psi] demonstrated potent activity at delta receptors (Ki < 1 nM).
    • TIPP[psi] showed minimal binding to mu and kappa receptors (Ki > 5 microM).
    • TIPP[psi] exhibited a delta/mu 1 selectivity exceeding 15,000-fold, significantly higher than DPDPE.

    Conclusions:

    • TIPP[psi] possesses exceptional delta-selectivity, surpassing previously reported compounds.
    • Its high selectivity and antagonist properties offer advantages for opioid receptor research.
    • TIPP[psi] has been successfully employed to create an enhanced mu 1 binding assay.