Pharmacology · Antidiabetic Drugs (Oral Hypoglycemics, Insulins)

Repaglinide is a meglitinide analog used in type 2 diabetes. How does its binding site on the pancreatic beta-cell sulfonylurea receptor differ from sulfonylureas?

  • A It binds to the Kir6.2 subunit of the K-ATP channel rather than SUR1
  • B It binds to a distinct 36 kDa membrane site separate from the SUR1 sulfonylurea binding site
  • C It binds to SUR2A on cardiac myocytes instead of SUR1 on beta cells
  • D It does not bind any receptor and acts via direct membrane depolarization
Correct answer: B. It binds to a distinct 36 kDa membrane site separate from the SUR1 sulfonylurea binding site

Explanation

Repaglinide binds to a distinct 36 kDa membrane binding site on beta cells, separate from the SUR1 sulfonylurea receptor site. This explains its shorter half-life and different pharmacokinetic profile. It still closes K-ATP channels but through a different binding location. It does not bind Kir6.2 (A) or SUR2B (C), and it does require receptor binding (D).

Reference: Katzung Basic and Clinical Pharmacology, 15th ed.

High-yield for: NEET PGINI-CETNExTFMGEUSMLEPLABMRCP

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