51803-78-2 Usage
Description
Different sources of media describe the Description of 51803-78-2 differently. You can refer to the following data:
1. Nimesulide is a relatively COX-2 selective, non-steroidal anti-inflammatory drug (NSAID) with analgesic and antipyretic properties. It is indicated for the treatment of acute pain, symptomatic treatment of osteoarthritis and primary dysmenorrhoea in adolescents and adults. However, due to the risk of causing hepatotoxicity, it should not be taken long-term. It has also been withdrawn from the markets in many countries. It mechanism of action is through targeting on various key mediators in the inflammatory process such as COX-2 mediated prostaglandins, free radicals, proteolytic enzymes and histamine.
2. Nimesulide is a non-steroidal anti-inflammatory drug (NSAID) and COX-2 inhibitor (IC50s = 1.27 and 0.03 μM for the human and ovine enzymes, respectively). It is selective for COX-2 over COX-1 (IC50s = 70 and 22 μM for the human and ovine enzymes, respectively). Nimesulide also inhibits sodium-dependent neutral amino acid transporter (B0AT1) with an IC50 value of 23 μM for the rat kidney transporter. It inhibits infection-induced increases in brain prostaglandin E2 (PGE2; ) levels, as well as reduces pyresis (ED50 = 0.3 mg/kg), in yeast-infected rats. Nimesulide (2.9 mg/kg) inhibits formalin-induced hindpaw thermal hyperalgesia in rats.
Originator
Riker (USA)
Uses
Different sources of media describe the Uses of 51803-78-2 differently. You can refer to the following data:
1. Antiinflammatory agent. Preferentially inhibits COX-2 over COX-1. Suppresses chemical-induced carcinogenesis in mice and rats. Inhibits LPS-induced TNF-alpha production
2. Labelled Nimesulide (N477500). Antiinflammatory agent. Preferentially inhibits COX-2 over COX-1. Suppresses chemical-induced carcinogenesis in mice and rats. Inhibits LPS-induced TNF-α production.
3. Antiinflammatory;'Cyclooxygenase 2 inhibitor
4. For the treatment of acute pain, the symptomatic treatment of osteoarthritis and primary dysmenorrhoea in adolescents and adults above 12 years old.
5. Labelled Nimesulide . Antiinflammatory agent. Preferentially inhibits COX-2 over COX-1. Suppresses chemical-induced carcinogenesis in mice and rats. Inhibits LPS-induced TNF-α production.;Labeled Nimesulide, intended for use as an internal standard for th
6. Nimesulide is a selective inhibitor of COX-2. The IC50 values are 70 and 1.27 μM for human recombinant COX-1 and -2 (at 20 μM arachidonic acid), respectively, and 22 and 0.03 μM for ovine COX-1 and -2 (at 100 μM arachidonic acid), respectively.[Cayman Chemical]
Brand name
Nimulid.
General Description
Nimesulide, a nonsteroidal anti-inflammatory drug (NSAID) belongs to the sulfonanilide class.
Biological Activity
Selective, orally active cyclooxygenase-2 (COX-2) inhibitor. Produces potent analgesic, anti-inflammatory and antipyretic activities in vivo . Reported to produce fewer gastrointestinal side effects than standard NSAIDs.
Biochem/physiol Actions
Highly selective cyclooxygenase-2 inhibitor.
Clinical Use
Nimesulide is a nonsteroidal antiinflammatory/analgesic agent useful in the
treatment of rheumatoid arthritis, as well as acute inflammation such as that
induced by periodontal surgery or urinary tract infections.
References
https://en.wikipedia.org/wiki/Nimesulide
https://www.drugbank.ca/drugs/DB04743
Check Digit Verification of cas no
The CAS Registry Mumber 51803-78-2 includes 8 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 5 digits, 5,1,8,0 and 3 respectively; the second part has 2 digits, 7 and 8 respectively.
Calculate Digit Verification of CAS Registry Number 51803-78:
(7*5)+(6*1)+(5*8)+(4*0)+(3*3)+(2*7)+(1*8)=112
112 % 10 = 2
So 51803-78-2 is a valid CAS Registry Number.
InChI:InChI=1/C13H12N2O5S/c1-21(18,19)14-12-8-7-10(15(16)17)9-13(12)20-11-5-3-2-4-6-11/h2-9,14H,1H3
51803-78-2Relevant articles and documents
Identification of the decomposition products in an industrial nitration process under thermal runaway conditions
Lunghi, Angelo,Alos, Miquel A.,Gigante, Lucia,Feixas, Joan,Sironi, Eugenio,Feliu, Josep A.,Cardillo, Paolo
, p. 926 - 932 (2002)
Directive 96/82/EC on the control of major-accident hazards involving dangerous substances, so-called Seveso II Directive, requires inventorying of dangerous substances which are believed might be generated during loss of control of an industrial chemical process. In the present work a nitration process that has underlined a potential risk of thermal runaway has been studied. A kinetic model has been developed and validated using the calorimetric data from a Mettler RC1 and a differential scanning calorimeter, along with the commercial software BatchCAD. The model has been later used to simulate the behavionr of an industrial reactor under abnormal conditions and to evaluate their consequences. Finally, the conditions that lead to thermal runaway scenarios have been reproduced to identify the decomposition products, as Seveso II Directive requires, using thermogravimetry and adiabatic calorimetry coupled with FTIR gas analyser.
Isomeric methoxy analogs of nimesulide for development of brain cyclooxygense-2 (COX-2)-targeted imaging agents: Synthesis, in vitro COX-2-inhibitory potency, and cellular transport properties
Yamamoto, Yumi,Hisa, Takuya,Arai, Jun,Saito, Yohei,Yamamoto, Fumihiko,Mukai, Takahiro,Ohshima, Takashi,Maeda, Minoru,Ohkubo, Yasuhito
, p. 6807 - 6814 (2015/11/11)
Nimesulide analogs bearing a methoxy substituent either at the ortho-, meta- or para-position on the phenyl ring, were designed, synthesized, and evaluated for potential as radioligands for brain cyclooxygenase-2 (COX-2) imaging. The synthesis of nimesulide and regioisomeric methoxy analogs was based on the copper-mediated arylation of phenolic derivatives for the construction of diaryl ethers. These isomeric methoxy analogs displayed lipophilicity similar to that of nimesulide itself, as evidenced by their HPLC log P7.4 values. In vitro inhibition studies using a colorimetric COX (ovine) inhibitor-screening assay demonstrated that the para-methoxy substituted analog retains the inhibition ability and selectivity observed for parent nimesulide toward COX-2 enzyme, whereas the meta- and ortho-methoxy substituents detrimentally affected COX-2-inhibition activity, which was further supported by molecular docking studies. Bidirectional transport cellular studies using Caco-2 cell culture model in the presence of the P-glycoprotein (P-gp) inhibitor, verapamil, showed that P-gp did not have a significant effect on the efflux of the para-methoxy substituted analog. Further investigations using the radiolabeled form of the para-methoxy substituted analog is warranted for in vivo characterization.
Method for the treatment and prevention of cachexia
-
, (2008/06/13)
Cachexia, including anorexia and other forms of weight loss, is a frequent complication of acute and chronic infections, and result from induction of cytokines, prostaglandins, and other inflammatory mediators that are critical for pathogen elimination. The present invention includes methods for the treatment or prevention of cachexic conditions while maintaining the production of factors essential for infection control through the administration of an effective amount of a cyclooxygenase-2 selective inhibiting compound.
