Product Feature - Somatostatin Receptors

Somatostatin (also known as somatotropin release-inhibiting hormone, SRIF) is an endogenous cyclic polypeptide first identified in 1968 as an inhibitor of growth hormone (GH) release from the rat anterior pituitary. Two active forms have been identified, SRIF-14 and SRIF-28, produced by alternative cleavage of preprosomatostatin. SRIF-14 and SRIF-28 have a wide distribution in the CNS as well as in the stomach, intestines and pancreas. They exert a range of biological actions including inhibition of hormone release (GH, TSH, gastrin, CCK, secretin, motilin, VIP, insulin, glucagon), neuromodulation, angiogenesis and modulation of cell proliferation.

Somatostatin acts on five subtypes of G-protein-coupled receptors (sst₁ - sst₅) that are differentially distributed throughout the CNS and periphery.

Key somatostatin receptor compounds now available from Tocris include:

Potent and selective sst₅ agonist
1980 l L-817,818
Inhibits growth hormone release from rat pituitary cells (EC₅₀ = 3.1 nM) and insulin release from mouse pancreatic islets (EC₅₀ = 0.3 nM) in vitro.

Selective sst₄ agonist
2440 l NNC 26-9100
Displays > 100-fold selectivity over sst₂ receptors (K_i values are 6 and 621 nM for sst₄ and sst₂ receptors respectively). Potently inhibits forskolin-induced cAMP accumulation (EC₅₀ = 26 nM).

Potent and selective sst₄ agonist
1979 l L-803,087
Facilitates AMPA-mediated hippocampal synaptic responses in vitro and increases kainate-induced seizures in mice in vivo.

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