Pharmacology · Pharmacokinetics and Pharmacodynamics

A full agonist and a partial agonist act at the same receptor. Which statement correctly describes a partial agonist?

  • A It produces submaximal response even at complete receptor occupancy and can antagonize a full agonist
  • B It binds the receptor but produces no intrinsic activity
  • C It shifts the full agonist curve to the left, increasing its potency
  • D It irreversibly binds the receptor, permanently reducing available receptors
Correct answer: A. It produces submaximal response even at complete receptor occupancy and can antagonize a full agonist

Explanation

B partial agonist has intrinsic activity between zero and that of a full agonist, so even at full receptor occupancy it produces a submaximal response. In the presence of a full agonist, it competes for the receptor and reduces the overall response, thus acting as a functional antagonist. Buprenorphine at the mu-opioid receptor is the classic example used in pharmacology teaching.

Reference: Goodman and Gilman's The Pharmacological Basis of Therapeutics, 14th ed.

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