Details
| Stereochemistry | ABSOLUTE |
| Molecular Formula | C14H14O3.C6H14N2O2 |
| Molecular Weight | 376.4467 |
| Optical Activity | UNSPECIFIED |
| Defined Stereocenters | 2 / 2 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
NCCCC[C@H](N)C(O)=O.COC1=CC=C2C=C(C=CC2=C1)[C@H](C)C(O)=O
InChI
InChIKey=YZESAGKBHWTAET-LMECJBHSSA-N
InChI=1S/C14H14O3.C6H14N2O2/c1-9(14(15)16)10-3-4-12-8-13(17-2)6-5-11(12)7-10;7-4-2-1-3-5(8)6(9)10/h3-9H,1-2H3,(H,15,16);5H,1-4,7-8H2,(H,9,10)/t9-;5-/m00/s1
| Molecular Formula | C14H14O3 |
| Molecular Weight | 230.2592 |
| Charge | 0 |
| Count |
|
| Stereochemistry | ABSOLUTE |
| Additional Stereochemistry | No |
| Defined Stereocenters | 1 / 1 |
| E/Z Centers | 0 |
| Optical Activity | UNSPECIFIED |
| Molecular Formula | C6H14N2O2 |
| Molecular Weight | 146.1876 |
| Charge | 0 |
| Count |
|
| Stereochemistry | ABSOLUTE |
| Additional Stereochemistry | No |
| Defined Stereocenters | 1 / 1 |
| E/Z Centers | 0 |
| Optical Activity | UNSPECIFIED |
DescriptionSources: http://www.accessdata.fda.gov/drugsatfda_docs/label/2016/017581s112,018164s062,020067s019lbl.pdfCurator's Comment: description was created based on several sources, including
https://www.ncbi.nlm.nih.gov/mesh/68009288
Sources: http://www.accessdata.fda.gov/drugsatfda_docs/label/2016/017581s112,018164s062,020067s019lbl.pdf
Curator's Comment: description was created based on several sources, including
https://www.ncbi.nlm.nih.gov/mesh/68009288
Naproxen (naproxen sodium, NAPROSYN®) is a propionic acid derivative related to the arylacetic acid group of nonsteroidal anti-inflammatory drugs (NSAIDs). It is an anti-inflammatory agent with analgesic and antipyretic properties. Both the acid and its sodium salt are used in the treatment of rheumatoid arthritis and other rheumatic or musculoskeletal disorders, dysmenorrhea, and acute gout. The mechanism of action of the naproxen (naproxen sodium, NAPROSYN®), like that of other NSAIDs, is not completely understood but involves inhibition of cyclooxygenase (COX-1 and COX-2).
CNS Activity
Sources: http://www.accessdata.fda.gov/drugsatfda_docs/label/2016/017581s112,018164s062,020067s019lbl.pdf
Curator's Comment: Naproxen is a potent inhibitor of prostaglandin synthesis in vitro. Naproxen concentrations reached during therapy have produced in vivo effects. Prostaglandins sensitize afferent nerves and potentiate the action of bradykinin in inducing pain in animal models.
Approval Year
Targets
| Primary Target | Pharmacology | Condition | Potency |
|---|---|---|---|
Target ID: CHEMBL221 |
0.11 µM [IC50] | ||
Target ID: CHEMBL230 |
0.19 µM [IC50] |
Conditions
| Condition | Modality | Targets | Highest Phase | Product |
|---|---|---|---|---|
| Primary | NAPROSYN Approved UseNAPROSYN is indicated:
For the relief of the signs and symptoms of rheumatoid arthritis.
For the relief of the signs and symptoms of osteoarthritis.
For the relief of the signs and symptoms of ankylosing spondylitis.
For the relief of the signs and symptoms of juvenile arthritis.
NAPROSYN is also indicated:
For relief of the signs and symptoms of tendonitis.
For relief of the signs and symptoms of bursitis.
For relief of the signs and symptoms of acute gout.
For the management of pain.
For the management of primary dysmenorrhea. Launch Date1976 |
|||
| Primary | NAPROSYN Approved UseNAPROSYN is indicated:
For the relief of the signs and symptoms of rheumatoid arthritis.
For the relief of the signs and symptoms of osteoarthritis.
For the relief of the signs and symptoms of ankylosing spondylitis.
For the relief of the signs and symptoms of juvenile arthritis.
NAPROSYN is also indicated:
For relief of the signs and symptoms of tendonitis.
For relief of the signs and symptoms of bursitis.
For relief of the signs and symptoms of acute gout.
For the management of pain.
For the management of primary dysmenorrhea. Launch Date1976 |
|||
| Primary | NAPROSYN Approved UseNAPROSYN is indicated:
For the relief of the signs and symptoms of rheumatoid arthritis.
For the relief of the signs and symptoms of osteoarthritis.
For the relief of the signs and symptoms of ankylosing spondylitis.
For the relief of the signs and symptoms of juvenile arthritis.
NAPROSYN is also indicated:
For relief of the signs and symptoms of tendonitis.
For relief of the signs and symptoms of bursitis.
For relief of the signs and symptoms of acute gout.
For the management of pain.
For the management of primary dysmenorrhea. Launch Date1976 |
|||
| Primary | NAPROSYN Approved UseNAPROSYN is indicated:
For the relief of the signs and symptoms of rheumatoid arthritis.
For the relief of the signs and symptoms of osteoarthritis.
For the relief of the signs and symptoms of ankylosing spondylitis.
For the relief of the signs and symptoms of juvenile arthritis.
NAPROSYN is also indicated:
For relief of the signs and symptoms of tendonitis.
For relief of the signs and symptoms of bursitis.
For relief of the signs and symptoms of acute gout.
For the management of pain.
For the management of primary dysmenorrhea. Launch Date1976 |
|||
| Primary | NAPROSYN Approved UseNAPROSYN is indicated:
For the relief of the signs and symptoms of rheumatoid arthritis.
For the relief of the signs and symptoms of osteoarthritis.
For the relief of the signs and symptoms of ankylosing spondylitis.
For the relief of the signs and symptoms of juvenile arthritis.
NAPROSYN is also indicated:
For relief of the signs and symptoms of tendonitis.
For relief of the signs and symptoms of bursitis.
For relief of the signs and symptoms of acute gout.
For the management of pain.
For the management of primary dysmenorrhea. Launch Date1976 |
Cmax
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
95 μg/L |
500 mg 2 times / day steady-state, oral dose: 500 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
NAPROXEN plasma | Homo sapiens population: UNKNOWN age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
94 μg/mL |
1000 mg 1 times / day steady-state, oral dose: 1000 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
NAPROXEN plasma | Homo sapiens population: UNKNOWN age: ADULT sex: UNKNOWN food status: UNKNOWN |
AUC
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
1446 μg × h/mL |
500 mg 2 times / day steady-state, oral dose: 500 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
NAPROXEN plasma | Homo sapiens population: UNKNOWN age: ADULT sex: UNKNOWN food status: UNKNOWN |
|
1448 μg × h/mL |
1000 mg 1 times / day steady-state, oral dose: 1000 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
NAPROXEN plasma | Homo sapiens population: UNKNOWN age: ADULT sex: UNKNOWN food status: UNKNOWN |
T1/2
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
15 h |
500 mg 2 times / day steady-state, oral dose: 500 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
NAPROXEN plasma | Homo sapiens population: UNKNOWN age: ADULT sex: UNKNOWN food status: UNKNOWN |
Funbound
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
1% |
500 mg 2 times / day steady-state, oral dose: 500 mg route of administration: Oral experiment type: STEADY-STATE co-administered: |
NAPROXEN plasma | Homo sapiens population: UNKNOWN age: ADULT sex: UNKNOWN food status: UNKNOWN |
Doses
| Dose | Population | Adverse events |
|---|---|---|
12.5 g single, oral Overdose Dose: 12.5 g Route: oral Route: single Dose: 12.5 g Sources: Page: 1102/129 |
healthy, 15 n = 1 Health Status: healthy Age Group: 15 Sex: F Population Size: 1 Sources: Page: 1102/129 |
Disc. AE: Abdominal pain, Nausea... AEs leading to discontinuation/dose reduction: Abdominal pain Sources: Page: 1102/129Nausea Dizziness Seizures Metabolic acidosis (severe) |
4 g single, oral Highest studied dose Dose: 4 g Route: oral Route: single Dose: 4 g Sources: Page: p.272 |
healthy, 20 n = 4 Health Status: healthy Age Group: 20 Sex: M Population Size: 4 Sources: Page: p.272 |
|
70.4 g single, oral Overdose Dose: 70.4 g Route: oral Route: single Dose: 70.4 g Co-administed with:: alcohol, p.o Sources: Page: p.103 |
healthy, 28 n = 1 Health Status: healthy Age Group: 28 Sex: M Population Size: 1 Sources: Page: p.103 |
Disc. AE: Sinus tachycardia, Drowsiness... AEs leading to discontinuation/dose reduction: Sinus tachycardia Sources: Page: p.103Drowsiness Metabolic acidosis Seizures |
26 g single, oral Overdose Dose: 26 g Route: oral Route: single Dose: 26 g Sources: Page: p.458 |
unhealthy, 58 n = 1 Health Status: unhealthy Condition: Depressive syndrome|Anxiety Age Group: 58 Sex: F Population Size: 1 Sources: Page: p.458 |
Disc. AE: Thrombopenia... AEs leading to discontinuation/dose reduction: Thrombopenia Sources: Page: p.458 |
550 mg 2 times / day multiple, oral Recommended Dose: 550 mg, 2 times / day Route: oral Route: multiple Dose: 550 mg, 2 times / day Sources: Page: p.1 |
unhealthy Health Status: unhealthy Condition: Pain|Primary Dysmenorrhea| Acute Tendonitis| Acute Bursitis Sources: Page: p.1 |
Disc. AE: Cardiac thrombosis, Myocardial infarction... AEs leading to discontinuation/dose reduction: Cardiac thrombosis (grade 3-5) Sources: Page: p.1Myocardial infarction (grade 3-5) Stroke (grade 3-5) Gastrointestinal disorder NOS (grade 3-5) Gastrointestinal bleeding (grade 3-5) Gastrointestinal ulcer (grade 3-5) Perforation stomach (grade 3-5) |
AEs
| AE | Significance | Dose | Population |
|---|---|---|---|
| Abdominal pain | Disc. AE | 12.5 g single, oral Overdose Dose: 12.5 g Route: oral Route: single Dose: 12.5 g Sources: Page: 1102/129 |
healthy, 15 n = 1 Health Status: healthy Age Group: 15 Sex: F Population Size: 1 Sources: Page: 1102/129 |
| Dizziness | Disc. AE | 12.5 g single, oral Overdose Dose: 12.5 g Route: oral Route: single Dose: 12.5 g Sources: Page: 1102/129 |
healthy, 15 n = 1 Health Status: healthy Age Group: 15 Sex: F Population Size: 1 Sources: Page: 1102/129 |
| Nausea | Disc. AE | 12.5 g single, oral Overdose Dose: 12.5 g Route: oral Route: single Dose: 12.5 g Sources: Page: 1102/129 |
healthy, 15 n = 1 Health Status: healthy Age Group: 15 Sex: F Population Size: 1 Sources: Page: 1102/129 |
| Seizures | Disc. AE | 12.5 g single, oral Overdose Dose: 12.5 g Route: oral Route: single Dose: 12.5 g Sources: Page: 1102/129 |
healthy, 15 n = 1 Health Status: healthy Age Group: 15 Sex: F Population Size: 1 Sources: Page: 1102/129 |
| Metabolic acidosis | severe Disc. AE |
12.5 g single, oral Overdose Dose: 12.5 g Route: oral Route: single Dose: 12.5 g Sources: Page: 1102/129 |
healthy, 15 n = 1 Health Status: healthy Age Group: 15 Sex: F Population Size: 1 Sources: Page: 1102/129 |
| Drowsiness | Disc. AE | 70.4 g single, oral Overdose Dose: 70.4 g Route: oral Route: single Dose: 70.4 g Co-administed with:: alcohol, p.o Sources: Page: p.103 |
healthy, 28 n = 1 Health Status: healthy Age Group: 28 Sex: M Population Size: 1 Sources: Page: p.103 |
| Metabolic acidosis | Disc. AE | 70.4 g single, oral Overdose Dose: 70.4 g Route: oral Route: single Dose: 70.4 g Co-administed with:: alcohol, p.o Sources: Page: p.103 |
healthy, 28 n = 1 Health Status: healthy Age Group: 28 Sex: M Population Size: 1 Sources: Page: p.103 |
| Seizures | Disc. AE | 70.4 g single, oral Overdose Dose: 70.4 g Route: oral Route: single Dose: 70.4 g Co-administed with:: alcohol, p.o Sources: Page: p.103 |
healthy, 28 n = 1 Health Status: healthy Age Group: 28 Sex: M Population Size: 1 Sources: Page: p.103 |
| Sinus tachycardia | Disc. AE | 70.4 g single, oral Overdose Dose: 70.4 g Route: oral Route: single Dose: 70.4 g Co-administed with:: alcohol, p.o Sources: Page: p.103 |
healthy, 28 n = 1 Health Status: healthy Age Group: 28 Sex: M Population Size: 1 Sources: Page: p.103 |
| Thrombopenia | Disc. AE | 26 g single, oral Overdose Dose: 26 g Route: oral Route: single Dose: 26 g Sources: Page: p.458 |
unhealthy, 58 n = 1 Health Status: unhealthy Condition: Depressive syndrome|Anxiety Age Group: 58 Sex: F Population Size: 1 Sources: Page: p.458 |
| Cardiac thrombosis | grade 3-5 Disc. AE |
550 mg 2 times / day multiple, oral Recommended Dose: 550 mg, 2 times / day Route: oral Route: multiple Dose: 550 mg, 2 times / day Sources: Page: p.1 |
unhealthy Health Status: unhealthy Condition: Pain|Primary Dysmenorrhea| Acute Tendonitis| Acute Bursitis Sources: Page: p.1 |
| Gastrointestinal bleeding | grade 3-5 Disc. AE |
550 mg 2 times / day multiple, oral Recommended Dose: 550 mg, 2 times / day Route: oral Route: multiple Dose: 550 mg, 2 times / day Sources: Page: p.1 |
unhealthy Health Status: unhealthy Condition: Pain|Primary Dysmenorrhea| Acute Tendonitis| Acute Bursitis Sources: Page: p.1 |
| Gastrointestinal disorder NOS | grade 3-5 Disc. AE |
550 mg 2 times / day multiple, oral Recommended Dose: 550 mg, 2 times / day Route: oral Route: multiple Dose: 550 mg, 2 times / day Sources: Page: p.1 |
unhealthy Health Status: unhealthy Condition: Pain|Primary Dysmenorrhea| Acute Tendonitis| Acute Bursitis Sources: Page: p.1 |
| Gastrointestinal ulcer | grade 3-5 Disc. AE |
550 mg 2 times / day multiple, oral Recommended Dose: 550 mg, 2 times / day Route: oral Route: multiple Dose: 550 mg, 2 times / day Sources: Page: p.1 |
unhealthy Health Status: unhealthy Condition: Pain|Primary Dysmenorrhea| Acute Tendonitis| Acute Bursitis Sources: Page: p.1 |
| Myocardial infarction | grade 3-5 Disc. AE |
550 mg 2 times / day multiple, oral Recommended Dose: 550 mg, 2 times / day Route: oral Route: multiple Dose: 550 mg, 2 times / day Sources: Page: p.1 |
unhealthy Health Status: unhealthy Condition: Pain|Primary Dysmenorrhea| Acute Tendonitis| Acute Bursitis Sources: Page: p.1 |
| Perforation stomach | grade 3-5 Disc. AE |
550 mg 2 times / day multiple, oral Recommended Dose: 550 mg, 2 times / day Route: oral Route: multiple Dose: 550 mg, 2 times / day Sources: Page: p.1 |
unhealthy Health Status: unhealthy Condition: Pain|Primary Dysmenorrhea| Acute Tendonitis| Acute Bursitis Sources: Page: p.1 |
| Stroke | grade 3-5 Disc. AE |
550 mg 2 times / day multiple, oral Recommended Dose: 550 mg, 2 times / day Route: oral Route: multiple Dose: 550 mg, 2 times / day Sources: Page: p.1 |
unhealthy Health Status: unhealthy Condition: Pain|Primary Dysmenorrhea| Acute Tendonitis| Acute Bursitis Sources: Page: p.1 |
Overview
| CYP3A4 | CYP2C9 | CYP2D6 | hERG |
|---|---|---|---|
Drug as perpetrator
| Target | Modality | Activity | Metabolite | Clinical evidence |
|---|---|---|---|---|
| yes [IC50 4.67 uM] | ||||
| yes [IC50 486 uM] | ||||
| yes [IC50 5.67 uM] | ||||
| yes [IC50 85.4 uM] |
Drug as victim
| Target | Modality | Activity | Metabolite | Clinical evidence |
|---|---|---|---|---|
| major | ||||
| minor | ||||
| minor | ||||
| yes | ||||
| yes | ||||
| yes | ||||
| yes | ||||
| yes | ||||
| yes | ||||
| yes | ||||
| yes |
PubMed
| Title | Date | PubMed |
|---|---|---|
| Recurrent aseptic meningitis following non- steroidal anti-inflammatory drugs--a reminder. | 1999 Dec |
|
| Renal effects of selective cyclooxygenase-2 inhibition in normotensive salt-depleted subjects. | 1999 Jul |
|
| Low-dose diclofenac, naproxen, and ibuprofen cohort study. | 1999 Jul |
|
| Long-term followup of naproxen-induced pseudoporphyria in juvenile rheumatoid arthritis. | 1999 Oct |
|
| [Aspirin-induced angioedema of the nape of the neck with naproxen cross-reaction: a case report]. | 2000 May |
|
| Absence of pharmacokinetic interaction between orally co-administered naproxen sodium and diphenhydramine hydrochloride. | 2000 Sep |
|
| Synthesis of some new 1-acylthiosemicarbazides, 1,3,4-oxadiazoles, 1,3,4-thiadiazoles and 1,2,4-triazole-3-thiones and their anti-inflammatory activities. | 2001 |
|
| Rofecoxib: a review of its use in the management of osteoarthritis, acute pain and rheumatoid arthritis. | 2001 |
|
| Naproxen particle design using porous starch. | 2001 Apr |
|
| Reduced incidence of gastroduodenal ulcers with celecoxib, a novel cyclooxygenase-2 inhibitor, compared to naproxen in patients with arthritis. | 2001 Apr |
|
| Celecoxib and rofecoxib. The role of COX-2 inhibitors in dental practice. | 2001 Apr |
|
| Pharmacokinetic/pharmacodynamic modeling of antipyretic and anti-inflammatory effects of naproxen in the rat. | 2001 Apr |
|
| [Acupuncture contra antiphlogistics in acute lumbago]. | 2001 Apr 20 |
|
| Directly coupled HPLC-NMR and HPLC-MS approaches for the rapid characterisation of drug metabolites in urine: application to the human metabolism of naproxen. | 2001 Feb |
|
| A look at the safety profile of over-the-counter naproxen sodium: a meta-analysis. | 2001 Feb |
|
| [Chronic recurrent multifocal osteomyelitis]. | 2001 Feb |
|
| Analgesic and anti-inflammatory effects of Mangifera indica L. extract (Vimang). | 2001 Feb |
|
| Etoricoxib (MK-0663): preclinical profile and comparison with other agents that selectively inhibit cyclooxygenase-2. | 2001 Feb |
|
| Determination of drug residues in water by the combination of liquid chromatography or capillary electrophoresis with electrospray mass spectrometry. | 2001 Feb 23 |
|
| Efficacy of single-dose and multidose rofecoxib in the treatment of post-orthopedic surgery pain. | 2001 Jan |
|
| Successful use of propranolol in migraine associated with electroconvulsive therapy. | 2001 Jan |
|
| Slow-release tramadol for treatment of chronic malignant pain--an open multicenter trial. | 2001 Jan |
|
| Review article: the gastrointestinal safety profile of rofecoxib, a highly selective inhibitor of cyclooxygenase-2, in humans. | 2001 Jan |
|
| Prostaglandin H synthase-2 inhibitors interfere with prostaglandin H synthase-1 inhibition by nonsteroidal anti-inflammatory drugs. | 2001 Jan 19 |
|
| Alendronate and naproxen are synergistic for development of gastric ulcers. | 2001 Jan 8 |
|
| New issues about nitric oxide and its effects on the gastrointestinal tract. | 2001 Jul |
|
| Dapsone activation of CYP2C9-mediated metabolism: evidence for activation of multiple substrates and a two-site model. | 2001 Jul |
|
| In vitro evaluation and intra-articular administration of biodegradable microspheres containing naproxen sodium. | 2001 Jul-Aug |
|
| Determination of naproxen in pharmaceutical preparations by room-temperature phosphorescence. A comparative study of several organized media. | 2001 Jun |
|
| By the way, doctor. Which drugs cause problems in the sun? | 2001 Jun |
|
| [Treatment of pain due to unwanted lactation with a homeopathic preparation given in the immediate post-partum period]. | 2001 Jun |
|
| Fixed drug eruption due to naproxen; lack of cross-reactivity with other propionic acid derivatives. | 2001 Jun |
|
| [The lack of awareness of the Israeli population regarding gastrointestinal complications from non-steroidal anti-inflammatory drugs]. | 2001 Jun |
|
| Treatment of de Quervain's disease:role of conservative management. | 2001 Jun |
|
| Immune thrombocytopenia resulting from sensitivity to metabolites of naproxen and acetaminophen. | 2001 Jun 15 |
|
| Peroxisomal proliferator-activated ligand therapy for HIV lipodystrophy. | 2001 Mar |
|
| Interleukin-6 (IL-6) producing phaeochromocytoma: direct IL-6 suppression by non-steroidal anti-inflammatory drugs. | 2001 Mar |
|
| High-performance liquid chromatographic method development and validation for the simultaneous quantitation of naproxen sodium and pseudoephedrine hydrochloride impurities. | 2001 Mar |
|
| Effect of lipophilicity on in vivo iontophoretic delivery. I. NSAIDs. | 2001 Mar |
|
| Functional status and health-related quality of life of elderly osteoarthritic patients treated with celecoxib. | 2001 Mar |
|
| Rofecoxib, a COX-2 inhibitor, does not inhibit human gastric mucosal prostaglandin production. | 2001 Mar |
|
| Analysis of nonsteroidal antiinflammatory drugs in meconium and its relation to persistent pulmonary hypertension of the newborn. | 2001 Mar |
|
| Selective inhibition of COX-2 in humans is associated with less gastrointestinal injury: a comparison of nimesulide and naproxen. | 2001 Mar |
|
| Effect of cyclodextrin charge on complexation of neutral and charged substrates: comparison of (SBE)7M-beta-CD to HP-beta-CD. | 2001 May |
|
| Severe reversible renal failure due to naproxen-associated acute interstitial nephritis. | 2001 May |
|
| Effect of nonsteroidal anti-inflammatory drug use on the rate of gastrointestinal hospitalizations among people living in long-term care. | 2001 May |
|
| The influence of polyvinylpyrrolidone on naproxen complexation with hydroxypropyl-beta-cyclodextrin. | 2001 May |
|
| Upper gastrointestinal toxicity of rofecoxib and naproxen. | 2001 May 3 |
|
| Isotachophoretic determination of naproxen in the presence of its metabolite in human serum. | 2001 May 4 |
|
| Screening procedure for detection of non-steroidal anti-inflammatory drugs and their metabolites in urine as part of a systematic toxicological analysis procedure for acidic drugs and poisons by gas chromatography-mass spectrometry after extractive methylation. | 2001 May-Jun |
Patents
Sample Use Guides
Rheumatoid Arthritis, Osteoarthritis and Ankylosing Spondylitis:
1 tablet of NAPROSYN® (250 mg or 375 mg or 500 mg) twice daily.
Acute Gout:
The recommended starting dose is 750 mg of NAPROSYN® followed by 250 mg every 8
hours until the attack has subsided.
Route of Administration:
Oral
There are data on the N-(3-methylpyridin-2-yl)amide derivatives of flurbiprofen and naproxen (Flu-AM1 and Nap-AM1, respectively) with respect to their properties towards fatty acid amide hydrolase (FAAH). Flu-AM1 and Nap-AM1 inhibited FAAH-catalysed hydrolysis of [(3)H]anandamide by rat brain homogenates with IC50 values of 0.44 and 0.74 uM. The corresponding values for flurbiprofen and naproxen were 29 and >100 uM, respectively.
| Substance Class |
Chemical
Created
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admin
on
Edited
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by
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| Record UNII |
15X32OGO88
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| Record Status |
Validated (UNII)
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| Record Version |
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PARENT -> SALT/SOLVATE |
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ACTIVE MOIETY |