BIM 23056

Biological Activity

somatostatin (srif) is a cyclic tetradecapeptide that was originally isolated from mammalian hypothalamus and characterized as a physiological regulator of gh secretion from the anterior pituitary. bim 23056 is a novel linear peptide of srif sstr3 antagnist.

Safety Profile

A poison by intracerebral route. When heated to decomposition it emits toxic vapors of NOx.

in vitro

bim 23056 bound to sstr3 with subnanomolar affinities. bim 23056 displayed remarkable selectivity for sstr3, not interacting significantly with either sstr1 or sstr2 at concentrations as high as 1 μm. bim 23056 was 30,000-fold selective for sstr3, which maks it a ligand of choice for future studies on sstr3 [1]. in addition, it has been found that bim 23056 behaves as a potent and surmountable antagonist at the human recombinant sst5 receptor. such antagonism was specific for the sst5 receptor as bim 23056 did not inhibit [ca2+], or ins(1,4,5)p3 increases in response to utp [2].

IC 50

0.02 nm for sstr3

References

[1] raynor k, murphy wa, coy dh, taylor je, moreau jp, yasuda k, bell gi, reisine t. cloned somatostatin receptors: identification of subtype-selective peptides and demonstration of high affinity binding of linear peptides. mol pharmacol. 1993 jun;43(6):838-44.
[2] wilkinson gf, thurlow rj, sellers la, coote je, feniuk w, humphrey pp. potent antagonism by bim-23056 at the human recombinant somatostatin sst5 receptor. br j pharmacol. 1996 jun;118(3):445-7.