Somatostatin receptors

Overview

Somatostatin (somatotropin release inhibiting factor) is an abundant neuropeptide, which acts on five subtypes of somatostatin receptor (SST1-SST5; nomenclature as agreed by the NC-IUPHAR Subcommittee on Somatostatin Receptors [1]). Activation of these receptors produces a wide range of physiological effects throughout the body including the inhibition of secretion of many hormones. Endogenous ligands for these receptors are somatostatin-14 (SRIF-14) and somatostatin-28 (SRIF-28). cortistatin-14 has also been suggested to be an endogenous ligand for somatostatin receptors [2].

References

  1. Günther T, Tulipano G, Dournaud P, et al. International Union of Basic and Clinical Pharmacology. CV. Somatostatin Receptors: Structure, Function, Ligands, and New Nomenclature. Pharmacol Rev 2018;70:763-835.
  2. de Lecea L, Criado JR, Prospero-Garcia O, et al. A cortical neuropeptide with neuronal depressant and sleep-modulating properties. Nature 1996;381:242-5.
Excerpt from IUPHAR/BPS Guide to Pharmacology
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Human
Available
Assay modes:
Agonist
Inverse agonist
Antagonist
PAM
NAM
Panels:
Human non-orphan GPCRs
Oncology
Endocrinology/Metabolism
Neurology
Gastrointestinal
à la carte
Reference agonist:
somatostatin‐14
EC50:
23 nM
Human
Available
Assay modes:
Agonist
Inverse agonist
Antagonist
PAM
NAM
Panels:
Human non-orphan GPCRs
Oncology
Endocrinology/Metabolism
Neurology
Gastrointestinal
à la carte
Reference agonist:
somatostatin‐14
EC50:
3.1 nM
Human
Available
Assay modes:
Agonist
Inverse agonist
Antagonist
PAM
NAM
Panels:
Human non-orphan GPCRs
Neurology
Gastrointestinal
à la carte
Reference agonist:
somatostatin‐14
EC50:
3.2 nM
Human
Available
Assay modes:
Agonist
Inverse agonist
Antagonist
PAM
NAM
Panels:
Human non-orphan GPCRs
Immunology/Infection
Oncology
Hematology
Neurology
Ophthalmology
Respiratory
Dermatology
Musculoskeletal
Urology/Reproduction
à la carte
Reference agonist:
somatostatin‐14
EC50:
290 pM
Human
Available
Assay modes:
Agonist
Inverse agonist
Antagonist
PAM
NAM
Panels:
Human non-orphan GPCRs
Neurology
à la carte
Reference agonist:
somatostatin‐14
EC50:
1.7 nM
Mouse
Available
Assay modes:
Agonist
Inverse agonist
Antagonist
PAM
NAM
Panels:
Mouse non-orphan GPCRs
à la carte
Reference agonist:
somatostatin‐14
EC50:
8.0 nM
Mouse
Available
Assay modes:
Agonist
Inverse agonist
Antagonist
PAM
NAM
Panels:
Mouse non-orphan GPCRs
à la carte
Reference agonist:
somatostatin‐14
EC50:
7.0 nM
Mouse
Available
Assay modes:
Agonist
Inverse agonist
Antagonist
PAM
NAM
Panels:
Mouse non-orphan GPCRs
à la carte
Reference agonist:
somatostatin‐14
EC50:
8.1 nM
Mouse
Available
Assay modes:
Agonist
Inverse agonist
Antagonist
PAM
NAM
Panels:
Mouse non-orphan GPCRs
à la carte
Reference agonist:
somatostatin‐14
EC50:
1.3 nM
Mouse
Available
Assay modes:
Agonist
Inverse agonist
Antagonist
PAM
NAM
Panels:
Mouse non-orphan GPCRs
à la carte
Reference agonist:
somatostatin‐14
EC50:
13 nM