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The inhibition of COX-2 is paramount for the anti-inflammatory and analgesic function of the selective COX-2 inhibitor celecoxib. However, with regard to this drug's promise for the therapy of advanced cancers, it is unclear whether the inhibition of COX-2 plays a dominant role, and this has become a controversial and intensely researched issue.
Rofecoxib is a selective COX-2 inhibitor, or "coxib". Though the class of coxibs includes several agents, degrees of COX-2 selectivity vary among them, with celecoxib (Celebrex) being the least COX-2 selective, and rofecoxib (Vioxx), valdecoxib (Bextra), and etoricoxib (Arcoxia), being highly COX-2 selective. [10]
Pages in category "COX-2 inhibitors" The following 24 pages are in this category, out of 24 total. This list may not reflect recent changes. * Cyclooxygenase-2 ...
Once the COX-2 enzyme was identified, Dup-697 became the building-block for synthesis of COX-2 inhibitors. Celecoxib and rofecoxib, the first COX-2 inhibitors to reach market, were based on DuP-697. [ 5 ] [ 6 ] It took less than eight years to develop and market the first COX-2 inhibitor, with Celebrex ( celecoxib ) launched in December 1998 ...
Drug nomenclature is the systematic naming of drugs, especially pharmaceutical drugs.In the majority of circumstances, drugs have 3 types of names: chemical names, the most important of which is the IUPAC name; generic or nonproprietary names, the most important of which are international nonproprietary names (INNs); and trade names, which are brand names. [1]
Parecoxib, sold under the brand name Dynastat among others, is a water-soluble and injectable prodrug of valdecoxib. Parecoxib is a COX2 selective inhibitor. It is injectable. It is approved in the European Union for short term perioperative pain control. It was patented in 1996 and approved for medical use in 2002. [3]
5743 19225 Ensembl ENSG00000073756 ENSMUSG00000032487 UniProt P35354 Q05769 RefSeq (mRNA) NM_000963 NM_011198 RefSeq (protein) NP_000954 NP_035328 Location (UCSC) Chr 1: 186.67 – 186.68 Mb Chr 1: 149.98 – 149.98 Mb PubMed search Wikidata View/Edit Human View/Edit Mouse Cyclooxygenase-2 (COX-2), also known as prostaglandin-endoperoxide synthase 2 (HUGO PTGS2), is an enzyme that in humans is ...
The smaller Val 523 residue in COX-2 allows access to a hydrophobic side-pocket in the enzyme (which Ile 523 sterically hinders). Drug molecules, such as DuP-697 and the coxibs derived from it, bind to this alternative site and are considered to be selective inhibitors of COX-2. [2]