Somatostatin receptor subtypes 1, 3, 4, and 5 (SSTR1/3/4/5)

Somatostatin receptor subtypes 1, 3, 4, and 5 (SSTR1, SSTR3, SSTR4, and SSTR5) are members of the G protein-coupled receptor family that mediate the diverse physiological effects of the peptide hormone somatostatin. These receptors are widely distributed throughout the central nervous system and peripheral tissues, where they primarily exert inhibitory effects on hormone secretion, neurotransmission, and cell proliferation. SSTR1 and SSTR4 are often classified together as the SRIF-2 group, while SSTR3 and SSTR5 belong to the SRIF-1 group along with SSTR2. In therapeutic contexts, these subtypes are targeted to treat conditions such as neuroendocrine tumors, acromegaly, and Cushing's disease, often using multireceptor ligands like pasireotide which has high affinity for SSTR1, 3, and 5. SSTR4 is particularly noted for its role in modulating pain and inflammation, making it a target for novel analgesic development. SSTR5 plays a significant role in regulating insulin secretion, and its activation is associated with the side effect of hyperglycemia in some somatostatin analogs.

Other names

SSTR1SSTR3SSTR4SSTR5Somatostatin receptor 1, 3, 4, 5Somatotropin release-inhibiting factor receptor 1, 3, 4, 5

Agonism