Mofezolac acts via selective inhibition of the cyclooxygenaseCOX-1 and consequent suppression of prostaglandin synthesis.[5] It is the most potent and selective reversible COX-1 inhibitor.[6] Studies of ovine COX-1 in complex with mofezolac indicate that the drug forms a combination of electrostatic, H-bond, hydrophobic, and van der Waals contacts with the enzyme active site channel, contributing to mofezolac's high binding affinity.[7]
Mofezolac belongs to the class of isoxazoles and is a substrate of CYP2C9.[8]
It is manufactured and marketed by Nipro ES Pharma Co., Ltd.[1]
Referencesedit
^ abc"Kusuri-no-Shiori (Drug Information Sheet)". RAD-AR Council, Japan. June 2018. Retrieved 2021-10-18.
^Calvello R, Lofrumento DD, Perrone MG, Cianciulli A, Salvatore R, Vitale P, et al. (2017). "Highly Selective Cyclooxygenase-1 Inhibitors P6 and Mofezolac Counteract Inflammatory State both In Vitro and In Vivo Models of Neuroinflammation". Frontiers in Neurology. 8: 251. doi:10.3389/fneur.2017.00251. PMC5465243. PMID 28649222.
^"Pharmaceuticals and Medical Devices Safety Information" (381). Translated by Pharmaceuticals and Medical Devices Agency. Japan Ministry of Health, Labour and Welfare. March 2021. {{cite journal}}: Cite journal requires |journal= (help)
^Ono N, Yamamoto N, Sunami A, Yamasaki Y, Miyake H (February 1990). "[Pharmacological profile of mofezolac, a new non-steroidal analgesic anti-inflammatory drug]". Nihon Yakurigaku Zasshi. Folia Pharmacologica Japonica (in Japanese). 95 (2): 63–81. doi:10.1254/fpj.95.2_63. PMID 2109726.
^Pati ML, Vitale P, Ferorelli S, Iaselli M, Miciaccia M, Boccarelli A, et al. (February 2019). "Translational impact of novel widely pharmacological characterized mofezolac-derived COX-1 inhibitors combined with bortezomib on human multiple myeloma cell lines viability". European Journal of Medicinal Chemistry. 164: 59–76. doi:10.1016/j.ejmech.2018.12.029. hdl:11586/227733. PMID 30590258. S2CID 58648199.
^Cingolani G, Panella A, Perrone MG, Vitale P, Di Mauro G, Fortuna CG, et al. (September 2017). "Structural basis for selective inhibition of Cyclooxygenase-1 (COX-1) by diarylisoxazoles mofezolac and 3-(5-chlorofuran-2-yl)-5-methyl-4-phenylisoxazole (P6)". European Journal of Medicinal Chemistry. 138: 661–668. doi:10.1016/j.ejmech.2017.06.045. PMC5992922. PMID 28710965.
mofezolac, sold, under, name, disopain, japan, nonsteroidal, anti, inflammatory, drug, nsaid, used, analgesic, anti, inflammatory, actions, often, prescribed, rheumatoid, arthritis, lower, back, pain, frozen, shoulder, pain, management, after, surgery, trauma,. Mofezolac INN sold under the name Disopain in Japan is a nonsteroidal anti inflammatory drug NSAID used for its analgesic and anti inflammatory actions It is often prescribed for rheumatoid arthritis lower back pain frozen shoulder and pain management after surgery or trauma 1 It is also being investigated for potential use in the treatment of neuroinflammation 2 3 MofezolacClinical dataAHFS Drugs comInternational Drug NamesRoutes ofadministrationOralATC codenoneLegal statusLegal statusIn general Prescription only IdentifiersIUPAC name 3 4 bis 4 methoxyphenyl isoxazol 5 yl acetic acidCAS Number78967 07 4 YPubChem CID4237ChemSpider4089UNIIRVJ0BV3H3YKEGGD01718 YCompTox Dashboard EPA DTXSID1046716Chemical and physical dataFormulaC 19H 17N O 5Molar mass339 347 g mol 13D model JSmol Interactive imageSMILES COC1 CC C C C1 C2 C ON C2C3 CC C C C3 OC CC O OInChI InChI 1S C19H17NO5 c1 23 14 7 3 12 4 8 14 18 16 11 17 21 22 25 20 19 18 13 5 9 15 24 2 10 6 13 h3 10H 11H2 1 2H3 H 21 22 Key DJEIHHYCDCTAAH UHFFFAOYSA N verify Common side effects include abdominal pain stomach discomfort nausea sleepiness itch hives rash erythema and edema Serious side effects include peptic ulcers gastrointestinal bleeding asthma attack jaundice acute liver failure and thrombocytopenia 1 Use is not recommended during pregnancy or breastfeeding 4 Mofezolac acts via selective inhibition of the cyclooxygenase COX 1 and consequent suppression of prostaglandin synthesis 5 It is the most potent and selective reversible COX 1 inhibitor 6 Studies of ovine COX 1 in complex with mofezolac indicate that the drug forms a combination of electrostatic H bond hydrophobic and van der Waals contacts with the enzyme active site channel contributing to mofezolac s high binding affinity 7 Mofezolac belongs to the class of isoxazoles and is a substrate of CYP2C9 8 It is manufactured and marketed by Nipro ES Pharma Co Ltd 1 References edit a b c Kusuri no Shiori Drug Information Sheet RAD AR Council Japan June 2018 Retrieved 2021 10 18 Calvello R Panaro MA Carbone ML Cianciulli A Perrone MG Vitale P et al January 2012 Novel selective COX 1 inhibitors suppress neuroinflammatory mediators in LPS stimulated N13 microglial cells Pharmacological Research 65 1 137 148 doi 10 1016 j phrs 2011 09 009 hdl 11586 117804 PMID 22001217 Calvello R Lofrumento DD Perrone MG Cianciulli A Salvatore R Vitale P et al 2017 Highly Selective Cyclooxygenase 1 Inhibitors P6 and Mofezolac Counteract Inflammatory State both In Vitro and In Vivo Models of Neuroinflammation Frontiers in Neurology 8 251 doi 10 3389 fneur 2017 00251 PMC 5465243 PMID 28649222 Pharmaceuticals and Medical Devices Safety Information 381 Translated by Pharmaceuticals and Medical Devices Agency Japan Ministry of Health Labour and Welfare March 2021 a href Template Cite journal html title Template Cite journal cite journal a Cite journal requires journal help Ono N Yamamoto N Sunami A Yamasaki Y Miyake H February 1990 Pharmacological profile of mofezolac a new non steroidal analgesic anti inflammatory drug Nihon Yakurigaku Zasshi Folia Pharmacologica Japonica in Japanese 95 2 63 81 doi 10 1254 fpj 95 2 63 PMID 2109726 Pati ML Vitale P Ferorelli S Iaselli M Miciaccia M Boccarelli A et al February 2019 Translational impact of novel widely pharmacological characterized mofezolac derived COX 1 inhibitors combined with bortezomib on human multiple myeloma cell lines viability European Journal of Medicinal Chemistry 164 59 76 doi 10 1016 j ejmech 2018 12 029 hdl 11586 227733 PMID 30590258 S2CID 58648199 Cingolani G Panella A Perrone MG Vitale P Di Mauro G Fortuna CG et al September 2017 Structural basis for selective inhibition of Cyclooxygenase 1 COX 1 by diarylisoxazoles mofezolac and 3 5 chlorofuran 2 yl 5 methyl 4 phenylisoxazole P6 European Journal of Medicinal Chemistry 138 661 668 doi 10 1016 j ejmech 2017 06 045 PMC 5992922 PMID 28710965 DRUG Mofezolac KEGG Retrieved 2021 10 18 nbsp This drug article relating to the musculoskeletal system is a stub You can help Wikipedia by expanding it vte Retrieved from https en wikipedia org w index php title Mofezolac amp oldid 1214900166, wikipedia, wiki, book, books, library,
