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The pharmacological profile of BAM 18

D E Hurlbut1, C J Evans, J D Barchas

  • 1Department of Pharmacology, University of California, Irvine 92715.

NIDA Research Monograph
|January 1, 1986
PubMed

Insights

BAM 18 exhibits high selectivity for the mu opioid receptor over kappa and delta opioid receptors. Its opioid receptor binding profile is comparable to metorphamide, suggesting potential therapeutic applications.

Area of Science:

  • Pharmacology
  • Neuroscience
  • Medicinal Chemistry

Background:

  • Opioid receptors are critical targets for pain management.
  • Understanding ligand selectivity is key to developing targeted therapeutics with reduced side effects.

Purpose of the Study:

  • To determine the opioid receptor selectivity of the novel compound BAM 18.
  • To compare the pharmacological profile of BAM 18 with known opioid ligands.

Main Methods:

  • Radioligand binding assays were used to quantify BAM 18's affinity for mu, kappa, and delta opioid receptors.
  • Peripheral tissue bioassays, specifically naloxone antagonism in guinea pig ileum and mouse vas deferens, were employed.

Main Results:

  • BAM 18 demonstrated a high affinity for the mu opioid receptor (Ki = 0.29 nM).
  • Its affinity for the kappa opioid receptor was twice that of mu (Ki = 0.84 nM), and for the delta opioid receptor, it was over 10 times lower (Ki = 3.9 nM).
  • The compound's activity profile was similar to metorphamide.

Conclusions:

  • BAM 18 displays significant selectivity for the mu opioid receptor.
  • The findings suggest BAM 18 could be a valuable tool compound or a lead for developing new analgesics.

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