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Opiate Receptor Pharmacology. Donald R. Wesson, MD. Opiate Receptors and effect of Agonist. Schematic of Mu Opiate Receptor. Source: Goodman and Gillman 9 th ed, p. 526. Agonist Partial Agonist Antagonists. Morphine-like effect (e.g., heroin, weak binding except for Fentanyl)

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Opiate receptor pharmacology l.jpg

Opiate Receptor Pharmacology

Donald R. Wesson, MD

Schematic of mu opiate receptor l.jpg
Schematic of Mu Opiate Receptor

Source: Goodman and Gillman 9th ed, p. 526

Receptor binding at mu receptor l.jpg


Partial Agonist


Morphine-like effect (e.g., heroin, weak binding except for Fentanyl)

Weak morphine-like effects with strong receptor affinity (e.g., buprenorphine)

No effect in absence of an opiate or opiate dependence (e.g., naltrexone)

Receptor Binding at Mu receptor

Effect of common opiates at mu receptor l.jpg

Heroin, morphine, methadone





Partial Agonist


Effect of Common Opiates at Mu Receptor

Buprenorphine pharmacology l.jpg
Buprenorphine Pharmacology

  • Partial agonist at mu receptor

  • High affinity for mu receptor

  • Can displace full opiate agonist such as heroin or methadone

    • Displacement of heroin or methadone by buprenorphine can produce opiate withdrawal symptoms

Buprenorphine pharmacology8 l.jpg
Buprenorphine Pharmacology

  • Antagonist at kappa receptor

  • Poor bio-availability taken orally (extensive first pass metabolism)

  • Much more bio-available from sublingual mucosa (Peak 2-3 hours following sublingual dose)