Rapid tachyphylaxis of the glucagon-like peptide 1-induced deceleration of gastric emptying in humans

Diabetes. 2011 May;60(5):1561-5. doi: 10.2337/db10-0474. Epub 2011 Mar 23.

Abstract

Objective: Glucagon-like peptide (GLP)-1 lowers postprandial glycemia primarily through inhibition of gastric emptying. We addressed whether the GLP-1-induced deceleration of gastric emptying is subject to rapid tachyphylaxis and if so, how this would alter postprandial glucose control.

Research design and methods: Nine healthy volunteers (25 ± 4 years old, BMI: 24.6 ± 4.7 kg/m(2)) were examined with intravenous infusion of GLP-1 (0.8 pmol · kg(-1) · min(-1)) or placebo over 8.5 h. Two liquid mixed meals were administered at a 4-h interval. Gastric emptying was determined, and blood samples were drawn frequently.

Results: GLP-1 decelerated gastric emptying significantly more after the first meal compared with the second meal (P = 0.01). This was associated with reductions in pancreatic polypeptide levels (marker of vagal activation) after the first but not the second meal (P < 0.05). With GLP-1, glucose concentrations declined after the first meal but increased after the second meal (P < 0.05). The GLP-1-induced reductions in postprandial insulin and C-peptide levels were stronger during the first meal course (P < 0.05). Likewise, glucagon levels were lowered by GLP-1 after the first meal but increased after the second test meal (P < 0.05).

Conclusions: The GLP-1-induced delay in gastric emptying is subject to rapid tachyphylaxis at the level of vagal nervous activation. As a consequence, postprandial glucose control by GLP-1 is attenuated after its chronic administration.

Publication types

  • Randomized Controlled Trial
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Adult
  • Blood Glucose / drug effects
  • C-Peptide / blood
  • Gastric Emptying / drug effects*
  • Glucagon / blood
  • Glucagon-Like Peptide 1 / blood
  • Glucagon-Like Peptide 1 / pharmacology*
  • Humans
  • Male
  • Postprandial Period
  • Tachyphylaxis*
  • Young Adult

Substances

  • Blood Glucose
  • C-Peptide
  • Glucagon-Like Peptide 1
  • Glucagon