CH 275 is a cyclic peptide agonist of somatostatin receptor 1 (SST1; IC50 = 30.9 nM for the human receptor).[1] It is selective for SST1 over SST2, SST3, SST4, and SST5 (IC50s = >10,000, 345, >1,000, and >10,000 nM, respectively, for the human receptors). CH 275 (500 nM) inhibits basal growth hormone secretion from primary mouse pituitary cells.[2] It inhibits glucose-induced increases in electrical activity without inducing membrane hyperpolarization in a whole-cell patch-clamp assay using MIN6 pancreatic β-cells when used at a concentration of 100 nM.[3]
References:
[1].Rivier, J.E., Hoeger, C., Erchegyi, J., et al.Potent somatostatin undecapeptide agonists selective for somatostatin receptor 1 (sst1)J. Med. Chem.44(13)2238-2246(2001).
[2].Kreienkamp, H.J., Akgün, E., Baumeister, H., et al.Somatostatin receptor subtype 1 modulates basal inhibition of growth hormone release in somatotrophsFEBS Lett.462(3)464-466(1999).
[3].Smith, P.A., Sellers, L.A., and Humphrey, P.P.Somatostatin activates two types of inwardly rectifying K+ channels in MIN-6 cellsJ. Physiol.532(Pt 1)127-142(2001).