The β3-Adrenoceptor Agonist GW427353 (Solabegron) Decreases Excitability of Human Enteric Neurons via Release of Somatostatin

Maternal separation as a model of brain–gut axis dysfunction

“…Recent evidence suggests that local adrenergic regulation of enteric nerve or adipose tissue-derived somatostatin release in human colonic biopsies (Cellek et al 2007;Schemann et al 2010) may be exploited in the treatment of functional brain-gut disorders.…”

Relaxation by β3-adrenoceptor agonists of the isolated human internal anal sphincter

“…Thus, β 3 -AR may be expressed not only in the smooth muscle but also in the enteric neurons and adipocytes as recently demonstrated for human colon (Cellek et al 2007;Schemann et al 2009), and their activation could inhibit excitatory cholinergic activity and enhance release of somatostatin (Cellek et al 2007). Furthermore, activation of β 3 -AR reduces excitability in most of the human submucous neurons indirectly by the activation of non neuronal cells, most likely adipocytes, to release mediators such as somatostatin which reduces neuronal activity (Schemann et al 2010).…”

Leptin modulates enteric neurotransmission in the rat proximal colon: An in vitro study

“…If leptin is produced locally, for instance by adipocytes in colonic submucosa [33,37] its receptors may be desensitized, which might explain the weak but significant effect of exogenous leptin on enteric neurons. Indeed, our results were consistent with those from previous studies showing that leptin modulates GI tract motility [24], hyperpolarizes glucoresponsive enteric neurons [31] and excites enteric neurons of submucous and myenteric plexus [33].…”