Content: Slate Blackcurrant Watermelon Strawberry Orange Banana Apple Emerald Chocolate Marble
Background: Slate Blackcurrant Watermelon Strawberry Orange Banana Apple Emerald Chocolate Marble
Pattern: Blank Waves Notes Sharp Wood Rockface Leather Honey Vertical Triangles

Clinical Advertisement
Sign in to follow this  
Health Reporter

Pubmed-Effect of the 5-HT4 receptor agonist tegaserod on the expression of GRK2 and GRK6 in the rat gastrointestinal tract.

1 post in this topic

Related Articles

Effect of the 5-HT4 receptor agonist tegaserod on the expression of GRK2 and GRK6 in the rat gastrointestinal tract.

BMC Res Notes. 2018 Jun 08;11(1):362

Authors: Nedi T, White PJ, Coupar IM, Irving HR

Abstract
OBJECTIVE: Tegaserod is a 5-hydroxytryptamine type 4 (5-HT4) receptor agonist, formerly used in treating constipation predominant irritable bowel syndrome, which desensitizes 5-HT4 receptors in rat oesophagus and colon in vitro. Desensitization of 5-HT4 receptors is regulated by G-protein coupled receptor kinases. This study was designed to assess the effect of 5-HT4 receptor activation on the expression of GRK2 and GRK6 in the rat oesophagus and distal colon by acute administration of tegaserod.
RESULTS: Rats were treated with a single dose of tegaserod (5 mg/kg) and tissue samples of the oesophagus and distal colon were prepared and level of GRK2 and GRK6 protein expression was determined using western blotting. The immunodensity of GRK2 and GRK6 was normalized against the loading control β-actin and compared with control animals. Acute administration of tegaserod for 1, 2, 3, 4, 6, and 8 h did not change significantly the immunodensity of GRK2 or GRK6 in the oesophagus or GRK2 in the distal colon when compared with control animals. This may indicate that the basal level of GRK2 and GRK6 expression is sufficient to regulate the desensitization of 5-HT4 receptors in acute drug treatment.

PMID: 29884229 [PubMed - in process]

View the full article

Share this post


Link to post
Share on other sites
Advertisement
Sign in to follow this