. Author manuscript; available in PMC: 2011 Mar 1.

Published in final edited form as: Trends Endocrinol Metab. 2010 Feb 9;21(3):123–133. doi: 10.1016/j.tem.2009.12.003

Table 1.

SRIF receptor subtype binding affinities.

		IC₅₀ (nM)
Ligands		hSSTR1	hSSTR2	hSSTR3	hSSTR4	hSSTR5
Endogenous	SRIF14 ^a	0.1–2.26	0.2–1.3	0.3–1.6	0.3–1.8	0.2–0.9
	SRIF28 ^a	0.1–2.2	0.2–4.1	0.3–6.1	0.3–7.9	0.05–0.4
	rCST14 ^a	1.7–5	0.09–1.8	0.3–3.8	0.2–18.2	0.3–1.9
	rCST29 ^a	2.8	7.1	0.2	3	13.7
	hCST17 ^a	0.25–7	0.6–0.9	0.4–0.6	0.5–0.6	0.3–0.4

Synthetic in clinical use or trial	BIM-23A760^b	622	0.03	160	>1000	3.7
	Lanreotide ^c	180	0.5	14	230	17
	Octreotide ^c	575	0.4	38	>1000	9
	Pasireotide ^c	9.3	1	1.5	>100	0.16

Synthetic experimental	BIM-23120 ^d	>1000	0.3	412	>1000	190
	BIM-23206 ^d	>1000	128	>1000	>1000	2
	BIM-23268 ^e	18	15	62	16	0.4

All tested in mono-receptor stable -K1, COS-7 or HEK-293 transfectants.

SRIF=somatostatin; r/hCTS=rat/human cortistatin

From:

Binding affinity to D2R is 15 nM[8],

[9],

[10].