Selective agonists of somatostatin receptor subtype 1 or 2 injected peripherally induce antihyperalgesic effect in two models of visceral hypersensitivity in mice.
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Mulak A, Larauche M, Biraud M, Million M, Rivier J, Tache Y
Selective agonists of somatostatin receptor subtype 1 or 2 injected peripherally induce antihyperalgesic effect in two models of visceral hypersensitivity in mice.
Peptides. 2015 Jan;63:71-80. doi: 10.1016/j.peptides.2014.10.013. Epub 2014 Nov 5.
- PubMed ID
- 25451334 [ View in PubMed]
- Abstract
Somatostatin interacts with five G-protein-coupled receptor (sst1-5). Octreotide, a stable sst2>>3>/=5 agonist, exerts a visceral anti-hyperalgesic effect in experimental and clinical studies. Little is known on the receptor subtypes involved. We investigated the influence of the stable sst1-5 agonist, ODT8-SST and selective receptor subtype peptide agonists (3 or 10mug/mouse) injected intraperitoneally (ip) on visceral hypersensitivity in mice induced by repeated noxious colorectal distensions (four sets of three CRD, each at 55mmHg) or corticotropin-releasing factor receptor 1 agonist, cortagine given between two sets of graded CRD (15, 30, 45, and 60mmHg, three times each pressure). The mean visceromotor response (VMR) was assessed using a non-invasive manometry method and values were expressed as percentage of the VMR to the 1st set of CRD baseline or to the 60mmHg CRD, respectively. ODT8-SST (10mug) and the sst2 agonist, S-346-011 (3 and 10mug) prevented mechanically induced visceral hypersensitivity in the three sets of CRD, the sst1 agonist (10mug) blocked only the 2nd set and showed a trend at 3mug while the sst4 agonist had no effect. The selective sst2 antagonist, S-406-028 blocked the sst2 agonist but not the sst1 agonist effect. The sst1 agonist (3 and 10mug) prevented cortagine-induced hypersensitivity to CRD at each pressure while the sst2 agonist at 10mug reduced it. These data indicate that in addition to sst2, the sst1 agonist may provide a novel promising target to alleviate visceral hypersensitivity induced by mechanoreceptor sensitization and more prominently, stress-related visceral nociceptive sensitization.
DrugBank Data that Cites this Article
- Drug Targets
Drug Target Kind Organism Pharmacological Action Actions Octreotide Somatostatin receptor Group Humans YesAgonistDetails