The brain-penetrating, orally bioavailable, ghrelin receptor agonist HM01 ameliorates motion-induced emesis in Suncus murinus (house musk shrew).

ABSTRACT:

Background and purpose

HM01, a novel, orally bioavailable, brain-penetrating agonist of ghrelin receptors, ameliorates emesis in Suncus murinus. This study compared HM01's activity against motion sickness with that of the less brain-penetrating ghrelin receptor agonist, HM02.

Experimental approach

The potential of HM01 and HM02 to relax isolated mesenteric arteries and to increase feeding was investigated. Radio telemetry was used to record gastric slow waves and body temperature. Plethysmography was used to measure respiratory function. HM01 and HM02 were administered p.o. 1 hr prior to provocative motion, and c-Fos expression in brain sections was assessed.

Key results

HM01 and HM02 both relaxed precontracted arteries, yielding EC₅₀ values of 2.5 ± 0.5 an

SUBMITTER: Tu L 

PROVIDER: S-EPMC7060360 | biostudies-literature | 2020 Apr

REPOSITORIES: biostudies-literature