Pasireotide is a stable cyclohexapeptide somatostatin mimic.

SST5:9.9(pki), SST2:9 (pki), SST1:pki:8.2 , SST4:<7.0 (pki), SST3:9.1(pki)

SOM230, a novel, stable cyclohexapeptide somatostatin mimic that exhibits unique high-affinity binding to human somatostatin receptors (subtypes sst1-sst5).?SOM230 has potent, long-lasting inhibitory effects on growth hormone and insulin-like growth factor-1 release[1]

Untreated SSTR2(-/-) mice with AIA displayed joint swelling and mechanical hyperalgesia similar to that seen in SSTR2(+/+) mice.?In wild-type mice, both octreotide and pasireotide significantly attenuated knee joint swelling and histopathologic manifestations of arthritis to an extent comparable to that of dexamethasone.?In SSTR2(-/-) mice, the antiinflammatory effects of both octreotide and pasireotide were completely abrogated.?Prolonged administration of pasireotide also inhibited joint swelling and protected against joint destruction during AIA flare reactions.?In addition, both octreotide and pasireotide reduced inflammatory hyperalgesia.?The antinociceptive actions of octreotide were abolished in SSTR2(-/-) mice, but those of pasireotide were retained.?In dorsal root ganglia of naive wild-type mice, only SSTR1 and SSTR2A, but not SSTR3 or SSTR5, were detected in a subset of small- and medium-diameter neurons[1].