Pharmacology · Autonomic Nervous System (Cholinergic, Anticholinergic, Sympathomimetics, Sympatholytics)

A researcher studies the effect of a drug that selectively blocks presynaptic α2-adrenoreceptors at noradrenergic terminals. Which of the following best describes the expected physiological consequence?

  • A Decreased norepinephrine release from the terminal due to loss of autoreceptor-mediated inhibition
  • B Increased norepinephrine release because autoinhibitory feedback is removed
  • C Activation of postsynaptic Gi protein leading to decreased cAMP in target cells
  • D Selective blockade of α2 postsynaptic heteroreceptors causing vasodilation
Correct answer: B. Increased norepinephrine release because autoinhibitory feedback is removed

Explanation

Presynaptic α2-adrenoreceptors act as autoreceptors that sense ambient norepinephrine and, when activated, inhibit further neurotransmitter release via Gi-protein-coupled reduction in cAMP. Blocking these receptors removes autoinhibitory feedback, increasing norepinephrine release. Option A reverses the physiology. Option C describes what happens when α2 receptors are activated, not blocked. Option D confuses presynaptic autoreceptors with heteroreceptors on non-noradrenergic terminals.

Reference: KD Tripathi, Essentials of Medical Pharmacology, 8th ed.

High-yield for: NEET PGINI-CETNExTFMGEUSMLEPLABMRCP

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