Fluciclovine (18F)
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Identification
- Summary
Fluciclovine (18F) is a radiolabelled L-leucine derivative used to image tumors, especially in the prostate.
- Brand Names
- Axumin
- Generic Name
- Fluciclovine (18F)
- DrugBank Accession Number
- DB13146
- Background
Fluciclovine is a [18F]-tagged synthetic analog of the amino acid L-leucine. It presents excellent diagnostic properties to be used in positron emission tomography (PET) imaging.2 The structure of fluciclovine allows it to be uptaken by the tumoral cells by its amino acid transporter without incorporating in the metabolism within the body.3 Fluciclovine was developed by Blue Earth Diagnostics, Ltd. and FDA approved in May 27, 2016.7
- Type
- Small Molecule
- Groups
- Approved
- Structure
- Weight
- Average: 132.125
Monoisotopic: 132.056441169 - Chemical Formula
- C5H8FNO2
- Synonyms
- (18F)FACBC
- (1R,3R)-1-amino-3(18F)fluorocyclobutane-1-carboxylic acid
- Anti-1-amino-3-(18F)fluorocyclobutane-1-carboxylic acid
- FACBC F-18
- Fluciclovine (18F)
- Fluciclovine F 18
- Fluciclovine F-18
- External IDs
- (18F)GE-148
- GE-148 (18F)
- GE-148 F-18
- NMK-36
- NMK36
Pharmacology
- Indication
Fluciclovine is indicated as a detection agent for positron emission tomography (PET) in men with suspected prostate cancer recurrence based on elevated blood prostate specific antigen (PSA) levels following prior treatment.4 The overexpression of L-type amino acid transporters such as LAT1 and LAT3 that mediate the uptake of essential amino acids has been extensively reported as a tumoral mechanism of cell growth.5
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 Diagnostic agent Prostate cancer •••••••••••• - Contraindications & Blackbox Warnings
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- Pharmacodynamics
Following intravenous administration, the tumor-to-normal tissue contrast is highest between 2 and 10 minutes after injection, with a 63% reduction in mean tumor uptake at 90 minutes after injection.6 The scanning time point should be evaluated carefully as an early scanning can present an increased blood pool and a late scanning will translate into an increased muscle uptake. These variations should always be considered in the image interpretation.8
- Mechanism of action
Fluciclovine is transported into the prostate cancer cells via ASCT2 and LAT1 transporters. The activity of LAT1 gets increased in acidic pH, condition that is developed intra-tumorally at certain size. The uptake of fluciclovine presents an androgen-dependent dynamic in hormone sensitive cells.9
Target Actions Organism ANeutral amino acid transporter B(0) binderHumans AY+L amino acid transporter 1 binderHumans ACationic amino acid transporter 3 binderHumans NGlutamate (NMDA) receptor inhibitorHumans NGlutamate receptor 1 inhibitorHumans NGlutamate receptor 2 inhibitorHumans NGlutamate receptor 3 inhibitorHumans NGlutamate receptor 4 inhibitorHumans - Absorption
After intravenous administration of fluciclovine, the major distribution happens in liver (14%), red bone marrow (12%), lung (7%), myocardium (4%) and pancreas (3%). With increasing time, the dose gets distributed into skeletal muscle.9
- Volume of distribution
The compartmental volume of distribution of fluciclovine is in prostate 0.97 L, vesicle 0.79 L, red bone marrow 0.98 L, gluteus muscle 2.13 L and obturator muscle 2.23 L.6
- Protein binding
Pre clinical studies showed that fluciclovine does not bind to plasma proteins.10
- Metabolism
Fluciclovine is not metabolized and it is not incorporated into newly synthesized proteins.9
- Route of elimination
In the first four hours post-injection, 3% of administered dose is excreted in the urine which increases to 5% after 24 hours post-injection.9
- Half-life
Fluciclovine is a cyclotron produced radionuclide that decays by positron emission (ß+ decay, 96.7%) and orbital electron capture (3.3%) to stable oxygen 18 with a physical half-life of 109.7 minutes.1
- Clearance
Fluciclovine renal clearance and excretion is minimal.6
- 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
The hasn't been long-term carcinogenity or fertility studies in animals. Even though all reports have shown no mutagenicity, fluciclovine has the potential to be mutagenic.10
- Pathways
- Not Available
- Pharmacogenomic Effects/ADRs
- Not Available
Interactions
- Drug Interactions
- 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.Not Available
- 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.
- Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Axumin Injection, solution 1600 MBq/ml Intravenous Blue Earth Diagnostics Ireland Ltd 2020-12-16 Not applicable EU Axumin Injection, solution 221 mCi/1mL Intravenous Blue Earth Diagnostics Ireland Ltd 2016-05-27 Not applicable US Axumin Injection, solution 3200 MBq/ml Intravenous Blue Earth Diagnostics Ireland Ltd 2020-12-16 Not applicable EU Axumin Injection, solution 3200 MBq/ml Intravenous Blue Earth Diagnostics Ireland Ltd 2020-12-16 Not applicable EU Axumin Injection, solution 1600 MBq/ml Intravenous Blue Earth Diagnostics Ireland Ltd 2020-12-16 Not applicable EU
Categories
- ATC Codes
- V09IX12 — Fluciclovine (18f)
- Drug Categories
- Chemical TaxonomyProvided by Classyfire
- Description
- This compound belongs to the class of organic compounds known as l-alpha-amino acids. These are alpha amino acids which have the L-configuration of the alpha-carbon atom.
- Kingdom
- Organic compounds
- Super Class
- Organic acids and derivatives
- Class
- Carboxylic acids and derivatives
- Sub Class
- Amino acids, peptides, and analogues
- Direct Parent
- L-alpha-amino acids
- Alternative Parents
- D-alpha-amino acids / Amino acids / Monocarboxylic acids and derivatives / Carboxylic acids / Organofluorides / Organic oxides / Monoalkylamines / Hydrocarbon derivatives / Carbonyl compounds / Alkyl fluorides
- Substituents
- Aliphatic homomonocyclic compound / Alkyl fluoride / Alkyl halide / Amine / Amino acid / Carbonyl group / Carboxylic acid / D-alpha-amino acid / Hydrocarbon derivative / L-alpha-amino acid
- Molecular Framework
- Aliphatic homomonocyclic compounds
- External Descriptors
- Not Available
- Affected organisms
- Humans and other mammals
Chemical Identifiers
- UNII
- 38R1Q0L1ZE
- CAS number
- 222727-39-1
- InChI Key
- NTEDWGYJNHZKQW-DGMDOPGDSA-N
- InChI
- InChI=1S/C5H8FNO2/c6-3-1-5(7,2-3)4(8)9/h3H,1-2,7H2,(H,8,9)/t3-,5-/i6-1
- IUPAC Name
- (1r,3r)-1-amino-3-(¹⁸F)fluorocyclobutane-1-carboxylic acid
- SMILES
- N[C@]1(C[C@H]([18F])C1)C(O)=O
References
- General References
- Nye JA, Schuster DM, Yu W, Camp VM, Goodman MM, Votaw JR: Biodistribution and radiation dosimetry of the synthetic nonmetabolized amino acid analogue anti-18F-FACBC in humans. J Nucl Med. 2007 Jun;48(6):1017-20. doi: 10.2967/jnumed.107.040097. Epub 2007 May 15. [Article]
- Schuster DM, Votaw JR, Nieh PT, Yu W, Nye JA, Master V, Bowman FD, Issa MM, Goodman MM: Initial experience with the radiotracer anti-1-amino-3-18F-fluorocyclobutane-1-carboxylic acid with PET/CT in prostate carcinoma. J Nucl Med. 2007 Jan;48(1):56-63. [Article]
- Schiavina R, Brunocilla E, Martorana G: The new promise of FACBC position emission tomography/computed tomography in the localization of disease relapse after radical treatment for prostate cancer: are we turning to the right radiotracer? Eur Urol. 2014 Jan;65(1):255-6. doi: 10.1016/j.eururo.2013.08.053. Epub 2013 Aug 30. [Article]
- Schuster DM, Nanni C, Fanti S: PET Tracers Beyond FDG in Prostate Cancer. Semin Nucl Med. 2016 Nov;46(6):507-521. doi: 10.1053/j.semnuclmed.2016.07.005. Epub 2016 Sep 7. [Article]
- Wang Q, Bailey CG, Ng C, Tiffen J, Thoeng A, Minhas V, Lehman ML, Hendy SC, Buchanan G, Nelson CC, Rasko JE, Holst J: Androgen receptor and nutrient signaling pathways coordinate the demand for increased amino acid transport during prostate cancer progression. Cancer Res. 2011 Dec 15;71(24):7525-36. doi: 10.1158/0008-5472.CAN-11-1821. Epub 2011 Oct 17. [Article]
- Sorensen J, Owenius R, Lax M, Johansson S: Regional distribution and kinetics of [18F]fluciclovine (anti-[18F]FACBC), a tracer of amino acid transport, in subjects with primary prostate cancer. Eur J Nucl Med Mol Imaging. 2013 Feb;40(3):394-402. doi: 10.1007/s00259-012-2291-9. Epub 2012 Dec 4. [Article]
- FDA News and Events [Link]
- Axumin [Link]
- Axumin [Link]
- FDA Reports [Link]
- FDA Approved Drug Products: AXUMIN (fluciclovine F 18) injection [Link]
- External Links
- PubChem Compound
- 450601
- PubChem Substance
- 347829262
- ChemSpider
- 23313216
- 1796118
- ChEBI
- 134703
- ChEMBL
- CHEMBL254468
- ZINC
- ZINC000101525552
- Wikipedia
- Fluciclovine_(18F)
- FDA label
- Download (265 KB)
- MSDS
- Download (116 KB)
Clinical Trials
- Clinical Trials
Clinical Trial & Rare Diseases Add-on Data Package
Explore 4,000+ rare diseases, orphan drugs & condition pairs, clinical trial why stopped data, & more. Preview package Phase Status Purpose Conditions Count Start Date Why Stopped 100+ additional columns Unlock 175K+ rows when you subscribe.View sample dataNot Available Active Not Recruiting Not Available Germ Cell Cancer, Nos / Germ Cell Neoplasm of Retroperitoneum / Germ Cell Neoplasms / Germ Cell Tumor, Testicular, Childhood / Metastatic Germ Cell Cancer / Testicular Cancer / Testicular Choriocarcinoma / Testicular Diseases / Testicular Germ Cell Tumors / Testicular Neoplasms / Testicular Yolk Sac Tumor / Testis cancer 1 somestatus stop reason just information to hide Not Available Unknown Status Not Available Adenocarcinoma of Prostate / Prostate Cancer 1 somestatus stop reason just information to hide 4 Recruiting Diagnostic Prostate Cancer 1 somestatus stop reason just information to hide 4 Terminated Diagnostic Cervical Cancer / Uterine Malignancies 1 somestatus stop reason just information to hide 4 Terminated Diagnostic Metastatic Carcinoma of the Prostate / Stage IVB Prostate Cancer AJCC v8 1 somestatus stop reason just information to hide
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Not Available
- Dosage Forms
Form Route Strength Injection, solution Intravenous 1600 MBq/ml Injection, solution Intravenous 221 mCi/1mL Injection, solution Intravenous 3200 MBq/ml Injection, solution Intravenous bolus 1600 MBq/ml Injection, solution Intravenous bolus 3200 MBq/ml - Prices
- Not Available
- Patents
Patent Number Pediatric Extension Approved Expires (estimated) Region US5808146 No 1998-09-15 2017-11-09 US US9387266 No 2016-07-12 2026-11-28 US US10010632 No 2018-07-03 2026-11-28 US US10124079 No 2018-11-13 2035-12-30 US US10716868 No 2020-07-21 2035-12-30 US US10933147 No 2021-03-02 2035-12-30 US US10967077 No 2021-04-06 2035-12-30 US US10953112 No 2021-03-23 2026-11-28 US US11980674 No 2022-04-23 2042-04-23 US
Properties
- State
- Liquid
- Experimental Properties
Property Value Source melting point (°C) 0ºC MSDS boiling point (°C) 100ºC MSDS water solubility Soluble MSDS Radioactivity (mCi/mL) 10 FDA label - Predicted Properties
Property Value Source Water Solubility 173.0 mg/mL ALOGPS logP -3 ALOGPS logP -2.9 Chemaxon logS 0.11 ALOGPS pKa (Strongest Acidic) 2.07 Chemaxon pKa (Strongest Basic) 9.42 Chemaxon Physiological Charge 0 Chemaxon Hydrogen Acceptor Count 3 Chemaxon Hydrogen Donor Count 2 Chemaxon Polar Surface Area 63.32 Å2 Chemaxon Rotatable Bond Count 1 Chemaxon Refractivity 27.75 m3·mol-1 Chemaxon Polarizability 11.65 Å3 Chemaxon Number of Rings 1 Chemaxon Bioavailability 1 Chemaxon Rule of Five Yes Chemaxon Ghose Filter No Chemaxon Veber's Rule No Chemaxon MDDR-like Rule No Chemaxon - Predicted ADMET Features
- Not Available
Spectra
- Mass Spec (NIST)
- Not Available
- Spectra
Spectrum Spectrum Type Splash Key Predicted GC-MS Spectrum - GC-MS Predicted GC-MS splash10-000l-9000000000-40609361b84eed0ac7ea Predicted MS/MS Spectrum - 10V, Positive (Annotated) Predicted LC-MS/MS splash10-000i-9100000000-10cfdfda5bd301d52b0d Predicted MS/MS Spectrum - 10V, Negative (Annotated) Predicted LC-MS/MS splash10-001i-0900000000-cd5988cd08de5aa795a6 Predicted MS/MS Spectrum - 20V, Positive (Annotated) Predicted LC-MS/MS splash10-00y1-9100000000-18b2fb07bac4d2cdba5e Predicted MS/MS Spectrum - 20V, Negative (Annotated) Predicted LC-MS/MS splash10-0159-9700000000-7bb228f93147807f66bc Predicted MS/MS Spectrum - 40V, Positive (Annotated) Predicted LC-MS/MS splash10-0007-9000000000-f52f81bef893fd7cc131 Predicted MS/MS Spectrum - 40V, Negative (Annotated) Predicted LC-MS/MS splash10-06y7-9000000000-4e230d26b14c008a646f Predicted 1H NMR Spectrum 1D NMR Not Applicable Predicted 13C NMR Spectrum 1D NMR Not Applicable - Chromatographic Properties
Collision Cross Sections (CCS)
Not Available
Targets
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Binder
- General Function
- Sodium-coupled antiporter of neutral amino acids. In a tri-substrate transport cycle, exchanges neutral amino acids between the extracellular and intracellular compartments, coupled to the inward cotransport of at least one sodium ion (PubMed:17094966, PubMed:23756778, PubMed:26492990, PubMed:29872227, PubMed:34741534, PubMed:8702519). The preferred substrate is the essential amino acid L-glutamine, a precursor for biosynthesis of proteins, nucleotides and amine sugars as well as an alternative fuel for mitochondrial oxidative phosphorylation. Exchanges L-glutamine with other neutral amino acids such as L-serine, L-threonine and L-asparagine in a bidirectional way. Provides L-glutamine to proliferating stem and activated cells driving the metabolic switch toward cell differentiation (PubMed:23756778, PubMed:24953180). The transport cycle is usually pH-independent, with the exception of L-glutamate. Transports extracellular L-glutamate coupled to the cotransport of one proton and one sodium ion in exchange for intracellular L-glutamine counter-ion. May provide for L-glutamate uptake in glial cells regulating glutamine/glutamate cycle in the nervous system (PubMed:32733894). Can transport D-amino acids. Mediates D-serine release from the retinal glia potentially affecting NMDA receptor function in retinal neurons (PubMed:17094966). Displays sodium- and amino acid-dependent but uncoupled channel-like anion conductance with a preference SCN(-) >> NO3(-) > I(-) > Cl(-) (By similarity). Through binding of the fusogenic protein syncytin-1/ERVW-1 may mediate trophoblasts syncytialization, the spontaneous fusion of their plasma membranes, an essential process in placental development (PubMed:10708449, PubMed:23492904)
- Specific Function
- amino acid transmembrane transporter activity
- Gene Name
- SLC1A5
- Uniprot ID
- Q15758
- Uniprot Name
- Neutral amino acid transporter B(0)
- Molecular Weight
- 56597.64 Da
References
- Axumin [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Binder
- General Function
- Heterodimer with SLC3A2, that functions as an antiporter which operates as an efflux route by exporting cationic amino acids from inside the cells in exchange with neutral amino acids plus sodium ions and may participate in nitric oxide synthesis via the transport of L-arginine (PubMed:10080182, PubMed:10655553, PubMed:14603368, PubMed:15756301, PubMed:15776427, PubMed:17329401, PubMed:9829974, PubMed:9878049). Also mediates arginine transport in non-polarized cells, such as monocytes, and is essential for the correct function of these cells (PubMed:15280038, PubMed:31705628). The transport mechanism is electroneutral and operates with a stoichiometry of 1:1 (By similarity). In vitro, Na(+) and Li(+), but also H(+), are cotransported with the neutral amino acids (By similarity)
- Specific Function
- basic amino acid transmembrane transporter activity
- Gene Name
- SLC7A7
- Uniprot ID
- Q9UM01
- Uniprot Name
- Y+L amino acid transporter 1
- Molecular Weight
- 55990.01 Da
References
- Axumin [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Binder
- General Function
- Uniporter that mediates the uptake of cationic L-amino acids such as L-arginine, L-lysine and L-ornithine (PubMed:11591158). The transport is sodium ions- and pH-independent, moderately trans-stimulated and is mediated by passive diffusion (PubMed:11591158)
- Specific Function
- amino acid transmembrane transporter activity
- Gene Name
- SLC7A3
- Uniprot ID
- Q8WY07
- Uniprot Name
- Cationic amino acid transporter 3
- Molecular Weight
- 67168.31 Da
References
- Axumin [Link]
- Kind
- Protein group
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Inhibitor
- General Function
- Component of NMDA receptor complexes that function as heterotetrameric, ligand-gated ion channels with high calcium permeability and voltage-dependent sensitivity to magnesium. Channel activation requires binding of the neurotransmitter glutamate to the epsilon subunit, glycine binding to the zeta subunit, plus membrane depolarization to eliminate channel inhibition by Mg(2+) (PubMed:26875626, PubMed:26919761, PubMed:28105280, PubMed:28126851, PubMed:7685113). Sensitivity to glutamate and channel kinetics depend on the subunit composition (PubMed:26919761)
- Specific Function
- amyloid-beta binding
Components:
References
- FDA Reports [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Inhibitor
- General Function
- Ionotropic glutamate receptor that functions as a ligand-gated cation channel, gated by L-glutamate and glutamatergic agonists such as alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA), quisqualic acid, and kainic acid (PubMed:1311100, PubMed:20805473, PubMed:21172611, PubMed:28628100, PubMed:35675825). L-glutamate acts as an excitatory neurotransmitter at many synapses in the central nervous system. Binding of the excitatory neurotransmitter L-glutamate induces a conformation change, leading to the opening of the cation channel, and thereby converts the chemical signal to an electrical impulse upon entry of monovalent and divalent cations such as sodium and calcium. The receptor then desensitizes rapidly and enters in a transient inactive state, characterized by the presence of bound agonist (By similarity). In the presence of CACNG2 or CACNG4 or CACNG7 or CACNG8, shows resensitization which is characterized by a delayed accumulation of current flux upon continued application of L-glutamate (PubMed:21172611). Resensitization is blocked by CNIH2 through interaction with CACNG8 in the CACNG8-containing AMPA receptors complex (PubMed:21172611). Calcium (Ca(2+)) permeability depends on subunits composition and, heteromeric channels containing edited GRIA2 subunit are calcium-impermeable. Also permeable to other divalents cations such as strontium(2+) and magnesium(2+) and monovalent cations such as potassium(1+) and lithium(1+) (By similarity)
- Specific Function
- adenylate cyclase binding
- Gene Name
- GRIA1
- Uniprot ID
- P42261
- Uniprot Name
- Glutamate receptor 1
- Molecular Weight
- 101505.245 Da
References
- FDA Reports [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Inhibitor
- General Function
- Ionotropic glutamate receptor that functions as a ligand-gated cation channel, gated by L-glutamate and glutamatergic agonists such as alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA), quisqualic acid, and kainic acid (PubMed:20614889, PubMed:31300657, PubMed:8003671). L-glutamate acts as an excitatory neurotransmitter at many synapses in the central nervous system and plays an important role in fast excitatory synaptic transmission (PubMed:14687553). Binding of the excitatory neurotransmitter L-glutamate induces a conformation change, leading to the opening of the cation channel, and thereby converts the chemical signal to an electrical impulse upon entry of monovalent and divalent cations such as sodium and calcium (PubMed:20614889, PubMed:8003671). The receptor then desensitizes rapidly and enters in a transient inactive state, characterized by the presence of bound agonist (By similarity). In the presence of CACNG4 or CACNG7 or CACNG8, shows resensitization which is characterized by a delayed accumulation of current flux upon continued application of L-glutamate (By similarity). Through complex formation with NSG1, GRIP1 and STX12 controls the intracellular fate of AMPAR and the endosomal sorting of the GRIA2 subunit toward recycling and membrane targeting (By similarity)
- Specific Function
- AMPA glutamate receptor activity
- Gene Name
- GRIA2
- Uniprot ID
- P42262
- Uniprot Name
- Glutamate receptor 2
- Molecular Weight
- 98820.32 Da
References
- FDA Reports [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Inhibitor
- General Function
- Ionotropic glutamate receptor that functions as a ligand-gated cation channel, gated by L-glutamate and glutamatergic agonists such as alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA), quisqualic acid, and kainic acid (By similarity). L-glutamate acts as an excitatory neurotransmitter at many synapses in the central nervous system and plays an important role in fast excitatory synaptic transmission by inducing long-term potentiation (By similarity). Binding of the excitatory neurotransmitter L-glutamate induces a conformation change, leading to the opening of the cation channel, and thereby converts the chemical signal to an electrical impulse upon entry of calcium (PubMed:17989220). The receptor then desensitizes rapidly and enters a transient inactive state, characterized by the presence of bound agonist (PubMed:17989220). In the presence of CACNG8, shows resensitization which is characterized by a delayed accumulation of current flux upon continued application of glutamate (PubMed:21172611)
- Specific Function
- AMPA glutamate receptor activity
- Gene Name
- GRIA3
- Uniprot ID
- P42263
- Uniprot Name
- Glutamate receptor 3
- Molecular Weight
- 101155.975 Da
References
- FDA Reports [Link]
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Inhibitor
- General Function
- Ionotropic glutamate receptor that functions as a ligand-gated cation channel, gated by L-glutamate and glutamatergic agonists such as alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA), quisqualic acid, and kainic acid (By similarity). L-glutamate acts as an excitatory neurotransmitter at many synapses in the central nervous system and plays an important role in fast excitatory synaptic transmission (By similarity). Binding of the excitatory neurotransmitter L-glutamate induces a conformation change, leading to the opening of the cation channel, and thereby converts the chemical signal to an electrical impulse upon entry of monovalent and divalent cations such as sodium and calcium. The receptor then desensitizes rapidly and enters a transient inactive state, characterized by the presence of bound agonist (By similarity). In the presence of CACNG8, shows resensitization which is characterized by a delayed accumulation of current flux upon continued application of L-glutamate (PubMed:21172611)
- Specific Function
- AMPA glutamate receptor activity
- Gene Name
- GRIA4
- Uniprot ID
- P48058
- Uniprot Name
- Glutamate receptor 4
- Molecular Weight
- 100870.085 Da
References
- FDA Reports [Link]
Transporters
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- No
- Actions
- Substrate
- General Function
- ATP-dependent transporter of the ATP-binding cassette (ABC) family that actively extrudes physiological compounds and xenobiotics from cells. Transports a range of endogenous molecules that have a key role in cellular communication and signaling, including cyclic nucleotides such as cyclic AMP (cAMP) and cyclic GMP (cGMP), bile acids, steroid conjugates, urate, and prostaglandins (PubMed:11856762, PubMed:12523936, PubMed:12835412, PubMed:12883481, PubMed:15364914, PubMed:15454390, PubMed:16282361, PubMed:17959747, PubMed:18300232, PubMed:26721430). Mediates the ATP-dependent efflux of glutathione conjugates such as leukotriene C4 (LTC4) and leukotriene B4 (LTB4) too. The presence of GSH is necessary for the ATP-dependent transport of LTB4, whereas GSH is not required for the transport of LTC4 (PubMed:17959747). Mediates the cotransport of bile acids with reduced glutathione (GSH) (PubMed:12523936, PubMed:12883481, PubMed:16282361). Transports a wide range of drugs and their metabolites, including anticancer, antiviral and antibiotics molecules (PubMed:11856762, PubMed:12105214, PubMed:15454390, PubMed:17344354, PubMed:18300232). Confers resistance to anticancer agents such as methotrexate (PubMed:11106685)
- Specific Function
- 15-hydroxyprostaglandin dehydrogenase (NAD+) activity
- Gene Name
- ABCC4
- Uniprot ID
- O15439
- Uniprot Name
- ATP-binding cassette sub-family C member 4
- Molecular Weight
- 149525.33 Da
References
- FDA Reports [Link]
Drug created at November 16, 2016 15:20 / Updated at October 01, 2021 23:55