Modulation of somatostatin receptors

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Somatostatin regulates alpha- and beta-cells

Somatostatin is a hormone produced by delta cells in the pancreatic islets of Langerhans. This hormone has various functions in an organism, among others effective regulation of beta- and alpha-cells, secreting insulin and glucagon, respectively.

Somatostatin antagonist for higher insulin release

In pharmacological terms, antagonists are drugs which block a receptor from executing its function. When somatostatin binds to its receptor on beta-cells, there is a decrease in insulin production. An antagonist to somatostatin receptor will stimulate insulin release at high glucose levels.

Somatostatin agonist for lower glucagon release

In contrast to antagonist, an agonist binds to a receptor to stimulate its activity. When somatostatin binds to its receptor on alpha-cells, there is a decrease in glucagon production. An agonist to somatostatin receptor on alpha-cells will lead to prevention of glucagon release at high glucose levels.

Targeting receptors on both beta and alfa cells

It is possible to produce an attractive drug that would inhibit the beta-cell somatostatin receptor, while activating the alpha-cell somatostatin receptor. Today, Biocrine evaluates beta-cell and alpha-cell somatostatin receptor as potential novel drugable targets in the treatment of diabetes.