. Author manuscript; available in PMC: 2012 Jul 1.

Published in final edited form as: Neurogastroenterol Motil. 2011 May 13;23(7):e294–e308. doi: 10.1111/j.1365-2982.2011.01721.x

Table 1.

Structure and receptor binding affinity of somatostatin receptor agonists.

Peptide^Reference	Structure	Receptor binding affinity (IC₅₀, nM)^a
Peptide^Reference	Structure	sst₁	sst₂	sst₃	sst₄	sst₅
ODT8-SST S-89-188²³	des-AA^{1,2,4,5,12,13}-(DTrp⁸)-SRIF	27.0 ± 3.4	41.0 ± 8.7	13.0 ± 3.2	1.8 ± 0.7	46.0 ± 27.0

sst₁ agonist S-406-062 (compound 25)³⁴	des-AA^{1,4–6,10,12,13}-[DTyr²,D-Agl(NMe,2naphtoyl)⁸,IAmp⁹]-SRIF-Thr-NH₂	0.19 ± 0.04	> 1K	158.0 ± 14.0	27.0 ± 7.5	> 1K

sst₂ agonist S-346-011 (compound 2)³⁵	des-AA^{1,4–6,11–13}-[DPhe²,Aph⁷(Cbm),DTrp⁸]-Cbm-SRIF-Thr-NH₂	> 1K	7.5 – 20	942 – 1094	872 – 957	109 – 260

sst₄ agonist S-315-297 (compound 15)³⁶	des-AA^{1,2,4,5,12,13}-[Aph⁷]-Cbm-SRIF	650 ± 115	> 1K	780 ± 62	1.5 ± 0.07	> 1K

sst₅ agonist BIM-23052³¹	D-Phe-Phe-Phe-D-Trp-Lys-Thr-Phe-Thr-NH₂	100	11.9	5.6	132	1.2

somatostatin-28 (SRIF-28)⁷⁶	Ser-Ala-Asn-Ser-Asn-Pro-Ala-Met-Ala-Pro-Arg-Glu-Arg-Lys-Ala-Gly-c[Cys-Lys-Asn-Phe-Phe-Trp-Lys-Thr-Phe-Thr-Ser-Cys]-OH	2.2	4.1	6.1	1.1	0.07

Derived from competitive radio ligand displacement assays in cells stably expressing the cloned human receptor using ¹²⁵I-[Leu⁸DTrp²²Tyr²⁵]somatostatin-28^{23, 31, 34–36} except for somatostatin-28.⁷⁶