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
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
Written and medically reviewed by the StethoPrep medical team.