Opioid Antagonist - Selective Antagonists

Selective Antagonists

All of the opioid antagonists used in medicine are non-selective, either blocking all three opioid receptors, or blocking the mu-opioid receptor but activating the kappa receptor. However for scientific research selective antagonists are needed which can block one of the opioid receptors but without affecting the other two. This has led to the development of antagonists which are highly selective to one of the three receptors;

  • Cyprodime is a selective mu opioid receptor antagonist
  • Naltrindole is a selective delta opioid receptor antagonist
  • Norbinaltorphimine is a selective kappa opioid receptor antagonist

Other selective antagonists are also known, but the three listed above were the first selective antagonists discovered for each respective opioid receptor, and are still the most widely used.

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Famous quotes containing the words selective and/or antagonists:

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