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

A researcher is studying the effects of clonidine at presynaptic alpha-2 receptors on a sympathetic nerve terminal. Activation of these receptors will:

  • A Increase cAMP via Gs coupling and augment norepinephrine release
  • B Decrease cAMP via Gi coupling and inhibit norepinephrine release
  • C Activate phospholipase C, increasing IP3 and intracellular calcium
  • D Open potassium channels causing membrane depolarization
Correct answer: B. Decrease cAMP via Gi coupling and inhibit norepinephrine release

Explanation

Presynaptic alpha-2 receptors are coupled to Gi proteins; their activation inhibits adenylyl cyclase, lowers cAMP, and reduces norepinephrine exocytosis (negative feedback autoreceptor). Clonidine acts at both central (locus coeruleus) and peripheral presynaptic alpha-2 sites to diminish sympathetic outflow. Alpha-2 does not signal through Gq/phospholipase C, and its channel effects (opening K+ channels) cause hyperpolarization, not depolarization.

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

High-yield for: NEET PGINI-CETNExTFMGEUSMLEPLABMRCP

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