H-p-Chloro-Phe-D-Cys-beta-(3-pyridyl)-Ala-D-Trp-Lys-tBu-Gly-Cys-2-Nal-NH2

Uses

PRL 2915 is a potent human somatostatin subtype 2 receptor (hsst2) antagonist with a Ki of 12 nM[1].

IC 50

hsst₂: 12 nM (Ki); hsst₃: 100 nM (Ki); hsst₅: 520 nM (Ki); hsst₄: 895 nM (Ki); hsst₁: >1000 nM (Ki); hsst₂: 1.8 nM (IC₅₀, rat antagonist bioassay versus somatostatin); rat urotensin II receptor: 293 nM (Ki); human urotensin II receptor: 562 nM (Ki)

References

[1] Hocart SJ, et al. Highly potent cyclic disulfide antagonists of somatostatin. J Med Chem. 1999 Jun 3;42(11):1863-71. DOI:10.1021/jm9806289
[2] Rossowski WJ, et al. Human urotensin II-induced aorta ring contractions are mediated by protein kinase C, tyrosine kinases and Rho-kinase: inhibition by somatostatin receptor antagonists. Eur J Pharmacol. 2002 Mar 8;438(3):159-70. DOI:10.1016/s0014-2999(02)01341-9