Alex Dean

Agonists and antagonists of SSTR

Discussion created by Alex Dean on Aug 29, 2019

Agonists and antagonists of SSTR / Somatostatin Receptor Inhibitor

I Octreotide acetate eight peptide is a kind of long-term growth hormone inhibin analogue, to simulate the natural growth hormone inhibin pharmacological effects.

II Octreotide is a somatostatin analog that binds to the somatostatin receptor, mainly subtypes 2, 3 and 5, increases Gi activity, and reduces intracellular cAMP production.

III Pasireotide (ditrifluoroacetate) is a stable cyclohexapeptide somatostatin mimic that exhibits unique high-affinity binding to human somatostatin receptors (subtypes sst1/2/3/4/5, pK i =8.2/9.0/9.1/<7.0/9.9, respectively).

IV MK-4256 is a potent and selective SSTR3 antagonist with IC 50s of 0.66 nM and 0.36 nM in human and mouse receptor binding assays, respectively.