Identification
- Summary
Somatostatin is a natural peptide hormone used to treat acute bleeding from esophageal varices, gastrointestinal ulcers, and gastritis; prevent pancreatic complications after surgery; and restrict secretions of the upper intestine, pancreas, and biliary tract.
- Generic Name
- Somatostatin
- DrugBank Accession Number
- DB09099
- Background
Somatostatin, also known as growth hormone-inhibiting hormone, is a naturally-occurring peptide hormone of 14 or 28 amino acid residues 9 that regulates the endocrine system. It is secreted by the D cells of the islets to inhibit the release of insulin and glucagon, and is also generated in the hypothalamus, where it inhibits the release of growth hormone and thyroid-stimulating hormones from the anterior pituitary 9. Somatostatin is initially secreted as a 116 amino acid precursor, preprosomatostatin, which undergoes endoproteolytic cleavage to prosomastatin. Prosomastatin is further process into two active forms, somatostatin-14 (SST-14) and somatostatin-28 (SST-28), an extended SST-14 sequence to the N-terminus 1. The actions of somatostatin are mediated via signalling pathways of G protein-coupled somatostatin receptors.
Antineoplastic effects and potential uses of somatostatin on various tumours, including pituitary adenomas, GEP-NETs, paragangliomas, carcinoids, breast cancers, malignant lymphoma and small-cell lung cancers, have been extensively investigated 1. Somatostatin has been used in the clinical setting for the diagnosis of acromegaly and gastrointestinal tract tumours. Its analogues have been developed to achieve more favourable kinetics for efficiency use in the management of acute conditions, such as esophageal varices. Octreotide is a long-acting analogue of somatostatin that inhibits the release of a number of hormones, and is clinically used to relieve symptoms of uncommon gastroenteropancreatic endocrine tumours, as well as treat acromegaly 9.
- Type
- Small Molecule
- Groups
- Approved, Investigational
- Structure
Structure for Somatostatin (DB09099)
- Weight
- Average: 1637.9
Monoisotopic: 1636.716655549 - Chemical Formula
- C76H104N18O19S2
- Synonyms
- Somatostatin
- Somatostatina
- Somatostatine
- Somatostatinum
- Synthetic growth hormone release-inhibiting hormone
- Synthetic somatostatin-14
- External IDs
- SRIF-14
Pharmacology
- Indication
For the symptomatic treatment of acute bleeding from esophageal varices. Other treatment options for long-term management of the condition may be considered if necessary, once initial control has been established.
Reduce drug development failure ratesBuild, train, & validate machine-learning modelswith evidence-based and structured datasets.Build, train, & validate predictive machine-learning models with structured datasets.- Associated Conditions
Indication Type Indication Combined Product Details Approval Level Age Group Patient Characteristics Dose Form Management of Acromegaly •••••••••••• •••••••••• ••••••• ••• •••••••• For therapy Biliary fistula •••••••••••• •••••••••• ••••••• ••• •••••••• Treatment of Bleeding caused by gastritis erosive •••••••••••• •••••••••• ••••••• ••• •••••••• Treatment of Diabetic ketoacidosis •••••••••••• ••••••• ••• •••••••• Treatment of Duodenal ulcer haemorrhage •••••••••••• •••••••••• ••••••• ••• •••••••• - Associated Therapies
- Contraindications & Blackbox Warnings
Prevent Adverse Drug Events TodayTap into our Clinical API for life-saving information on contraindications & blackbox warnings, population restrictions, harmful risks, & more.Avoid life-threatening adverse drug events with our Clinical API- Pharmacodynamics
Somatostatin is an endogenous peptide hormone that is secreted by the central nervous system, gastrointestinal tract, retina, peripheral neurons and pancreatic D cells of the islets of Langerhans. It exhibits several biological roles but predominantly exerts an inhibitory effect on secretion of other hormones and transmitters 1. While distribution of two active isoforms of somatostatin is similar, SST-14 is more predominant in the enteric neurons and peripheral nerves whereas SST-28 is more prominent in the retina and intestinal mucosal cells 1.
Anterior pituitary gland and brain: It inhibits the release of growth hormones and thyroid-stimulating hormones, such as thyroid stimulating hormone (TSH) and thyrotrophin, from the anterior pituitary while inhibiting the release of dopamine from the midbrain, norepinephrine, TRH and corticotrophin-releasing hormone in the brain 1.
Pancreas: In the pancreas, somatostatin reduces the secretion of glucagon and insulin as well as bicarbonate ions and other enzymes 1,9.
Thyroid gland: Somatosatin reduces secretion of T3, T4, and calcitonin 1. Somatostatin regulates the thyroid function by reducing basal TSH release 9.
Gastrointestinal tract: It attenuates the release of most gastrointestinal hormones such as gastrin, secretin, motilin, gastric acid, enteroglucagon, cholecystokinin (CCK), vasoactive intestinal peptide (VIP), gastric inhibitory polypeptide (GIP), intrinsic factor, pepsin, neurotensin, as well as bile secretion and colonic fluid secretion 1.
Adrenal gland: It inhibits angiotensin II-stimulated aldosterone secretion and acetylcholine-induced medullary catecholamine secretion 1.
Eye/retina: Somatostatin inhibits the production of vascular endothelial growth factor 1.
Inflammatory cells and sensory nerves: The expression of somatostatin has been found in inflammatory cells such as lymphocytes, monocytes, macrophages and endothelial cells to act as an autocrine or paracrine regulator in local immune responses. Findings suggest that somatostatin may play a role in exerting local and systemic anti-inflammatory and antinociceptive effects 1. On primary afferent neurons, somatostatin reduces the responses to thermal stimulation in C-mechanoheat sensitive fibers in a dose-dependent fashion and reduces the responses of C-mechanoheat fibers to bradykinin-induced excitation and sensitization to heat 6. Somatostatin is reported to elicit an analgesic effect when applied intrathecally; there is evidence supporting that similar effects may occur when systemically used to treat endocrine disorders 9.
Somatostatin is thought to reduce bleeding from esophageal varices by causing splanchnic vasoconstriction 2. Somatostatin elicits anti-neoplastic actions on various tumours via direct or indirect effects, or a combination of both 4.
- Mechanism of action
Somatostatin binds to 5 subtypes of somatostatin receptors (SSTRs), which are all Gi-protein-coupled transmembrane receptors that inhibits adenylyl cyclase upon activation 1. By inhibiting intracellular cyclic AMP and Ca2+ and by a receptor-linked distal effect on exocytosis, SSTRs block cell secretion 3. The common pathway shared by the receptors involve the activation of phosphotyrosine phosphatase (PTP), and modulation of mitogen-activated protein kinase (MAPK) 3. With the exception of SSTR3, activation of SSTRs lead to activation of voltage-gated potassium channels accompanied by increased K+ currents. This result in membrane hyperpolarization and inhibits depolarization-induced Ca2+ influx through voltage-sensitive Ca2+ channels 1. Depending on the receptor subtype, signalling cascades involve activation of other downstream targets such as Na+/H+ exchanger, Rho GTPase, and nitric oxide synthase (NOS) 1. SSTRs 1 to 4 bind both somatostatin isoforms with equal nanomolar binding affinity whereas SSTR5 exhibits a 5- to 10-fold higher binding affinity for SST-28 1.
Effects of SSTR1: Upon biding of somatostatin and activation, SSTR1 mediates an antisecretory effect on growth hormone, prolactin and calcitonin 1.
Effects of SSTR2: SSTR2 subtype dominates in endocrine tissues. By binding to SST2 receptors, somatostatin exerts paracrine inhibitory actions on gastrin release from G cells, histamine release from ECL cells, and directly on parietal cell acid output 9. SSTR2 receptor signalling cascades also inhibit the secretion of growth hormone and that of adrenocorticotropin, glucagon, insulin, and interferon-γ 1.
Effects of SSTR3: Activation of these receptors lead to reduction in cell proliferation 1. SSTR3 triggers PTP-dependent cell apoptosis accompanied by activation of p53 and the pro-apoptotic protein Bax 3. A study of the matrigel sponge assay suggests that through SSTR3-mediated inhibition of both NOS and MAPK activities may lead to the antitumor effects of somatostatin in inhibiting tumor angiogenesis 8.
Effects of SSTR4: The functions of SSTR4 remain largely unknown 1.
Effects of SSTR5: Like SSTR2, SSTR5 subtype also predominates in endocrine tissues. Upon activation, SSTR5 signalling cascades exert an inhibitory action on growth hormone, adrenocorticotropin, insulin, and glucagon-like peptide-1 as well as the secretion of amylase 1.
The presence of somatostatin receptors has been identified in most neuroendocrine tumours, endocrine gastroenteropancreatic (GEP) tumors, paragangliomas, pheochromocytomas, medullary thyroid carcinomas (MTC) and small cell lung carcinomas 7. The antitumor effects of somatostatin were also effective in various malignant lymphomas and breast tumours 7. Gastrointestinal hormones, such as gastrin, secretin, and cholecystokinin (CCK), as well as growth hormones and growth factors are thought to be elevated in gastrointestinal tract and neuroendocrine tumours and are inhibited by somatostatin 4. In vitro, somatostatin inhibited epidermal growth factor (EGF)-induced DNA synthesis and replication following which suggest that somatostatin may have direct anti-proliferative effects via SSTR signalling 4. Acromegaly is characterized as the endocrine disorder caused by a functioning tumour of cells that secrete growth hormone from the anterior pituitary 9. Somatostatin analogue therapies serve to normalize the elevated levels of GH and insulin-like growth factor 1 (IGF-1) and attenuate tumour growth.
In the vascular system this likely produces vasoconstriction by inhibiting adenylate cyclase leading to a lowering the concentration of cyclic adenosine monophosphate in the endothelial cells which ultimately blocks vasodilation through this pathway. This vasoconstriction is though the be responsible for reducing blood flow to the esophageal tissues and so reduces bleeding from esophageal varices 2.
Somatostatin mediates an analgesic activity by reducing vascular and nociceptive components of inflammation 6. Studies indicate that somatostatin may be present in nociceptive DRG neurons with C-fibers and primary afferent neurons to inhibit the release of transmitters at the presynaptic junctions of the sensory-efferent nerve terminals 1. Exogenous somatostatin has shown to inhibit the release of Substance P from central and peripheral nerve ending 1.
Target Actions Organism ASomatostatin receptor type 1 agonistHumans ASomatostatin receptor type 2 agonistHumans ASomatostatin receptor type 3 agonistHumans ASomatostatin receptor type 4 agonistHumans ASomatostatin receptor type 5 agonistHumans - Absorption
This pharmacokinetic data is irrelevant.
- Volume of distribution
This pharmacokinetic data is irrelevant.
- Protein binding
This pharmacokinetic data is irrelevant.
- Metabolism
Somatostatin is rapidly degraded by peptidase enzymes present in cells and plasma 1.
- Route of elimination
As a polypeptide chain, somatostatin is primarily eliminated via metabolism by peptidase enzymes 1.
- Half-life
The half-life of endogenous somatostatin is 1-3 minutes due to rapid degradation by peptidase enzymes present in the plasma and tissues 1.
- Clearance
Following intravenous administration of 3H-labeld endogenous somatostatin, the total body clearance was approximately 50 mL/min 5. In man, the value was calculated to be as high as 3000 mL/minutes, which is greatly exceeds the hepatic blood flow. This suggests that rapid enzymatic breakdown in the circulation and other tissues serves as a critical route of elimination 5.
- Adverse Effects
Improve decision support & research outcomesWith structured adverse effects data, including: blackbox warnings, adverse reactions, warning & precautions, & incidence rates. View sample adverse effects data in our new Data Library!Improve decision support & research outcomes with our structured adverse effects data.- Toxicity
Data is not available.
- Pathways
- Not Available
- Pharmacogenomic Effects/ADRs Browse all" title="About SNP Mediated Effects/ADRs" id="snp-actions-info" class="drug-info-popup" href="javascript:void(0);">
- Not Available
Interactions
- Drug Interactions Learn More" title="About Drug Interactions" id="structured-interactions-info" class="drug-info-popup" href="javascript:void(0);">
- This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
Drug Interaction Integrate drug-drug
interactions in your softwareAbemaciclib The metabolism of Abemaciclib can be decreased when combined with Somatostatin. Acalabrutinib The metabolism of Acalabrutinib can be decreased when combined with Somatostatin. Acenocoumarol The serum concentration of Acenocoumarol can be increased when it is combined with Somatostatin. Albendazole The metabolism of Albendazole can be decreased when combined with Somatostatin. Alectinib The metabolism of Alectinib can be decreased when combined with Somatostatin. - Food Interactions
- No interactions found.
Products
Drug product information from 10+ global regionsOur datasets provide approved product information including:dosage, form, labeller, route of administration, and marketing period.Access drug product information from over 10 global regions.- Product Ingredients
Ingredient UNII CAS InChI Key Somatostatin acetate F6R2N217HS 54472-66-1 GFYNCDIZASLOMM-HMAILDBGSA-N - Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Stilamin - Pws IV 3mg/amp Powder, for solution 3 mg / amp Intravenous Emd Serono, A Division Of Emd Inc., Canada 1997-11-10 2014-12-12 Canada 
- Mixture Products
Name Ingredients Dosage Route Labeller Marketing Start Marketing End Region Image Stilamin - Pws Liq IV Somatostatin acetate (250 mcg / kit) + Sodium chloride (9 mg / kit) Liquid; Powder, for solution Intravenous Emd Serono, A Division Of Emd Inc., Canada 1997-09-16 2014-12-12 Canada
Categories
- ATC Codes
- H01CB01 — Somatostatin
- Drug Categories
- Amino Acids, Peptides, and Proteins
- Cytochrome P-450 CYP3A Inhibitors
- Cytochrome P-450 CYP3A4 Inhibitors
- Cytochrome P-450 CYP3A4 Inhibitors (weak)
- Cytochrome P-450 Enzyme Inhibitors
- Hormones
- Hormones, Hormone Substitutes, and Hormone Antagonists
- Hypothalamic Hormones
- Nerve Tissue Proteins
- Neuropeptides
- P-glycoprotein substrates
- Pancreatic Hormones
- Peptide Hormones
- Peptides
- Pituitary and Hypothalamic Hormones and Analogues
- Pituitary Hormone Release Inhibiting Hormones
- Proteins
- Somatostatin and Analogues
- Somatostatin, agonists
- Systemic Hormonal Preparations, Excl. Sex Hormones and Insulins
- Classification
- Not classified
- Affected organisms
- Not Available
Chemical Identifiers
- UNII
- 6E20216Q0L
- CAS number
- 38916-34-6
- InChI Key
- NHXLMOGPVYXJNR-ATOGVRKGSA-N
- InChI
- InChI=1S/C76H104N18O19S2/c1-41(79)64(100)82-37-61(99)83-58-39-114-115-40-59(76(112)113)92-72(108)57(38-95)91-75(111)63(43(3)97)94-71(107)54(33-46-23-11-6-12-24-46)90-74(110)62(42(2)96)93-66(102)51(28-16-18-30-78)84-69(105)55(34-47-36-81-49-26-14-13-25-48(47)49)88-68(104)53(32-45-21-9-5-10-22-45)86-67(103)52(31-44-19-7-4-8-20-44)87-70(106)56(35-60(80)98)89-65(101)50(85-73(58)109)27-15-17-29-77/h4-14,19-26,36,41-43,50-59,62-63,81,95-97H,15-18,27-35,37-40,77-79H2,1-3H3,(H2,80,98)(H,82,100)(H,83,99)(H,84,105)(H,85,109)(H,86,103)(H,87,106)(H,88,104)(H,89,101)(H,90,110)(H,91,111)(H,92,108)(H,93,102)(H,94,107)(H,112,113)/t41-,42+,43+,50-,51-,52-,53-,54-,55-,56-,57-,58-,59-,62-,63-/m0/s1
- IUPAC Name
- (4R,7S,10S,13S,16S,19S,22S,25S,28S,31S,34S,37R)-19,34-bis(4-aminobutyl)-37-{2-[(2S)-2-aminopropanamido]acetamido}-13,25,28-tribenzyl-31-(carbamoylmethyl)-10,16-bis[(1R)-1-hydroxyethyl]-7-(hydroxymethyl)-22-[(1H-indol-3-yl)methyl]-6,9,12,15,18,21,24,27,30,33,36-undecaoxo-1,2-dithia-5,8,11,14,17,20,23,26,29,32,35-undecaazacyclooctatriacontane-4-carboxylic acid
- SMILES
- C[C@@H](O)[C@@H]1NC(=O)[C@H](CC2=CC=CC=C2)NC(=O)[C@@H](NC(=O)[C@H](CCCCN)NC(=O)[C@H](CC2=CNC3=C2C=CC=C3)NC(=O)[C@H](CC2=CC=CC=C2)NC(=O)[C@H](CC2=CC=CC=C2)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CSSC[C@H](NC(=O)[C@H](CO)NC1=O)C(O)=O)NC(=O)CNC(=O)[C@H](C)N)[C@@H](C)O
References
- General References
- Rai U, Thrimawithana TR, Valery C, Young SA: Therapeutic uses of somatostatin and its analogues: Current view and potential applications. Pharmacol Ther. 2015 Aug;152:98-110. doi: 10.1016/j.pharmthera.2015.05.007. Epub 2015 May 5. [Article]
- Hanisch E, Doertenbach J, Usadel KH: Somatostatin in acute bleeding oesophageal varices. Pharmacology and rationale for use. Drugs. 1992;44 Suppl 2:24-35; discussion 70-2. [Article]
- Patel YC: Somatostatin and its receptor family. Front Neuroendocrinol. 1999 Jul;20(3):157-98. [Article]
- Lamberts SW, de Herder WW, Hofland LJ: Somatostatin analogs in the diagnosis and treatment of cancer. Trends Endocrinol Metab. 2002 Dec;13(10):451-7. [Article]
- Marbach P, Briner U, Lemaire M, Schweitzer A, Terasaki T: From somatostatin to sandostatin: pharmacodynamics and pharmacokinetics. Metabolism. 1992 Sep;41(9 Suppl 2):7-10. [Article]
- Carlton SM, Du J, Davidson E, Zhou S, Coggeshall RE: Somatostatin receptors on peripheral primary afferent terminals: inhibition of sensitized nociceptors. Pain. 2001 Feb 15;90(3):233-44. [Article]
- Reubi JC, Laissue J, Krenning E, Lamberts SW: Somatostatin receptors in human cancer: incidence, characteristics, functional correlates and clinical implications. J Steroid Biochem Mol Biol. 1992 Sep;43(1-3):27-35. [Article]
- Florio T, Morini M, Villa V, Arena S, Corsaro A, Thellung S, Culler MD, Pfeffer U, Noonan DM, Schettini G, Albini A: Somatostatin inhibits tumor angiogenesis and growth via somatostatin receptor-3-mediated regulation of endothelial nitric oxide synthase and mitogen-activated protein kinase activities. Endocrinology. 2003 Apr;144(4):1574-84. doi: 10.1210/en.2002-220949. [Article]
- 29, 30, 32, 33, 41, . (2012). In Rang and Dale's Pharmacology (7th ed., pp. 362, 372, 377, 394-395, 412, 522). Edinburgh: Elsevier/Churchill Livingstone. [ISBN:978-0-7020-3471-8]
- External Links
- KEGG Drug
- D07431
- PubChem Compound
- 16129681
- PubChem Substance
- 310265025
- ChemSpider
- 17286507
- BindingDB
- 81767
- 9939
- ChEBI
- 64628
- ChEMBL
- CHEMBL1823872
- Wikipedia
- Somatostatin
- MSDS
- Download (21.9 KB)
Clinical Trials
- Clinical Trials Learn More" title="About Clinical Trials" id="clinical-trials-info" class="drug-info-popup" href="javascript:void(0);">
Phase Status Purpose Conditions Count 4 Completed Prevention Cirrhosis of the Liver / Upper Gastrointestinal Hemorrhage 1 4 Completed Treatment Acromegaly 1 4 Completed Treatment Bleeding / Varices, Esophageal 1 4 Completed Treatment Gastric Cancer After D2 Lymph Node Dissection 1 4 Completed Treatment Pancreatic Fistula 1
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Not Available
- Dosage Forms
Form Route Strength Injection, powder, lyophilized, for solution Intravenous 3 mg Powder Intravenous Injection, powder, for solution Intravenous Powder, for solution Powder, for solution Intravenous; Parenteral 3 MG Injection, solution Intravenous 3 mg Injection, powder, for solution Parenteral 3 mg Injection Intravenous 3 mg Injection, powder, for solution Parenteral Injection, powder, for solution Parenteral 6 mg Injection Intravenous 250 mcg Injection, powder, for solution; injection, powder, lyophilized, for solution Powder, for solution Intravenous; Parenteral 1 MG/2ML Powder, for solution Intravenous; Parenteral 2.5 MG/2ML Powder, for solution Intravenous; Parenteral 3 MG/2ML Injection, powder, for solution Powder, for solution Intravenous 3 mg / amp Liquid; powder, for solution Intravenous Injection, powder, for solution Intravenous 3 mg/ampoule - Prices
- Not Available
- Patents
- Not Available
Properties
- State
- Solid
- Experimental Properties
- Not Available
- Predicted Properties
Property Value Source Water Solubility 0.0205 mg/mL ALOGPS logP -1.8 ALOGPS logP -8.2 Chemaxon logS -4.9 ALOGPS pKa (Strongest Acidic) 2.88 Chemaxon pKa (Strongest Basic) 10.47 Chemaxon Physiological Charge 2 Chemaxon Hydrogen Acceptor Count 22 Chemaxon Hydrogen Donor Count 22 Chemaxon Polar Surface Area 613.23 Å2 Chemaxon Rotatable Bond Count 26 Chemaxon Refractivity 420.26 m3·mol-1 Chemaxon Polarizability 165.8 Å3 Chemaxon Number of Rings 6 Chemaxon Bioavailability 0 Chemaxon Rule of Five No Chemaxon Ghose Filter No Chemaxon Veber's Rule No Chemaxon MDDR-like Rule Yes Chemaxon - Predicted ADMET Features
- Not Available
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
- Chromatographic Properties
Collision Cross Sections (CCS)
Not Available
Targets
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Agonist
- General Function
- Somatostatin receptor activity
- Specific Function
- Receptor for somatostatin with higher affinity for somatostatin-14 than -28. This receptor is coupled via pertussis toxin sensitive G proteins to inhibition of adenylyl cyclase. In addition it stim...
- Gene Name
- SSTR1
- Uniprot ID
- P30872
- Uniprot Name
- Somatostatin receptor type 1
- Molecular Weight
- 42685.77 Da
References
- Rai U, Thrimawithana TR, Valery C, Young SA: Therapeutic uses of somatostatin and its analogues: Current view and potential applications. Pharmacol Ther. 2015 Aug;152:98-110. doi: 10.1016/j.pharmthera.2015.05.007. Epub 2015 May 5. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Agonist
- General Function
- Somatostatin receptor activity
- Specific Function
- Receptor for somatostatin-14 and -28. This receptor is coupled via pertussis toxin sensitive G proteins to inhibition of adenylyl cyclase. In addition it stimulates phosphotyrosine phosphatase and ...
- Gene Name
- SSTR2
- Uniprot ID
- P30874
- Uniprot Name
- Somatostatin receptor type 2
- Molecular Weight
- 41332.37 Da
References
- Rai U, Thrimawithana TR, Valery C, Young SA: Therapeutic uses of somatostatin and its analogues: Current view and potential applications. Pharmacol Ther. 2015 Aug;152:98-110. doi: 10.1016/j.pharmthera.2015.05.007. Epub 2015 May 5. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Agonist
- General Function
- Somatostatin receptor activity
- Specific Function
- Receptor for somatostatin-14 and -28. This receptor is coupled via pertussis toxin sensitive G proteins to inhibition of adenylyl cyclase.
- Gene Name
- SSTR3
- Uniprot ID
- P32745
- Uniprot Name
- Somatostatin receptor type 3
- Molecular Weight
- 45846.995 Da
References
- Rai U, Thrimawithana TR, Valery C, Young SA: Therapeutic uses of somatostatin and its analogues: Current view and potential applications. Pharmacol Ther. 2015 Aug;152:98-110. doi: 10.1016/j.pharmthera.2015.05.007. Epub 2015 May 5. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Agonist
- General Function
- Receptor for somatostatin-14. The activity of this receptor is mediated by G proteins which inhibits adenylyl cyclase. It is functionally coupled not only to inhibition of adenylate cyclase, but also to activation of both arachidonate release and mitogen-activated protein (MAP) kinase cascade. Mediates antiproliferative action of somatostatin in tumor cells.
- Specific Function
- Neuropeptide binding
- Gene Name
- SSTR4
- Uniprot ID
- P31391
- Uniprot Name
- Somatostatin receptor type 4
- Molecular Weight
- 42002.245 Da
References
- Rai U, Thrimawithana TR, Valery C, Young SA: Therapeutic uses of somatostatin and its analogues: Current view and potential applications. Pharmacol Ther. 2015 Aug;152:98-110. doi: 10.1016/j.pharmthera.2015.05.007. Epub 2015 May 5. [Article]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Agonist
- General Function
- Somatostatin receptor activity
- Specific Function
- Receptor for somatostatin 28 and to a lesser extent for somatostatin-14. The activity of this receptor is mediated by G proteins which inhibit adenylyl cyclase. Increases cell growth inhibition act...
- Gene Name
- SSTR5
- Uniprot ID
- P35346
- Uniprot Name
- Somatostatin receptor type 5
- Molecular Weight
- 39201.925 Da
References
- Rai U, Thrimawithana TR, Valery C, Young SA: Therapeutic uses of somatostatin and its analogues: Current view and potential applications. Pharmacol Ther. 2015 Aug;152:98-110. doi: 10.1016/j.pharmthera.2015.05.007. Epub 2015 May 5. [Article]
Enzymes
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Inhibitor
- General Function
- Vitamin d3 25-hydroxylase activity
- Specific Function
- Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation react...
- Gene Name
- CYP3A4
- Uniprot ID
- P08684
- Uniprot Name
- Cytochrome P450 3A4
- Molecular Weight
- 57342.67 Da
Transporters
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Unknown
- Actions
- Substrate
- General Function
- Xenobiotic-transporting atpase activity
- Specific Function
- Energy-dependent efflux pump responsible for decreased drug accumulation in multidrug-resistant cells.
- Gene Name
- ABCB1
- Uniprot ID
- P08183
- Uniprot Name
- Multidrug resistance protein 1
- Molecular Weight
- 141477.255 Da
References
- Uchiyama-Kokubu N, Naito M, Nakajima M, Tsuruo T: Transport of somatostatin and substance P by human P-glycoprotein. FEBS Lett. 2004 Sep 10;574(1-3):55-61. doi: 10.1016/j.febslet.2004.07.084. [Article]
Drug created at September 16, 2015 20:56 / Updated at December 02, 2023 07:02