Piroxicam, a potent inhibitor of prostaglandin production in cell culture. Structure-activity study
- PMID: 7384538
- DOI: 10.1016/0090-6980(80)90153-7
Piroxicam, a potent inhibitor of prostaglandin production in cell culture. Structure-activity study
Abstract
The new non-steroidal antiinflammatory (NSAI)2 agent, piroxicam [4-hydroxy-2-methyl-N-(2-pyridyl)-2H-1,2-benzothiazine-3-carboxamide 1,1-dioxide], is a highly active inhibitor of prostaglandin (PG) synthesis by methylcholanthrene transformed mouse fibroblasts (MC5-5) and rabbit synovial cells in culture. Comparison of the PG biosynthesis inhibitory activity of piroxicam with other NSAI drugs in these experiments ranks piroxicam as among the most potent agents of this type now known. Some specific modifications of piroxicam's structure result in significant loss in PG synthesis blocking activity.
Similar articles
-
Piroxicam: a review of its pharmacological properties and therapeutic efficacy.Drugs. 1981 Sep;22(3):165-87. doi: 10.2165/00003495-198122030-00001. Drugs. 1981. PMID: 7021122 Review.
-
Piroxicam, a structurally novel anti-inflammatory compound. Mode of prostaglandin synthesis inhibition.Prostaglandins. 1980 May;19(5):671-82. doi: 10.1016/0090-6980(80)90166-5. Prostaglandins. 1980. PMID: 6775350
-
Inhibition of prostaglandin E synthesis by steroidal and nonsteroidal antiinflammatory drugs in human synovial fibroblast cultures.J Rheumatol. 1984 Aug;11(4):488-92. J Rheumatol. 1984. PMID: 6481721
-
Piroxicam pharmacologic activity and gastrointestinal damage by oral and rectal route. Comparison with oral indometacin and phenylbutazone.Arzneimittelforschung. 1981;31(1):87-92. Arzneimittelforschung. 1981. PMID: 6971112
-
Effect of nonsteroidal antiinflammatory drugs on immune function.Semin Arthritis Rheum. 1983 Aug;13(1 Suppl 1):134-43. doi: 10.1016/0049-0172(83)90033-1. Semin Arthritis Rheum. 1983. PMID: 6226096 Review.
Cited by
-
Predictability of the clinical potency of NSAIDs from the preclinical pharmacodynamics in rats.Inflamm Res. 1996 Nov;45(11):531-40. doi: 10.1007/BF02342223. Inflamm Res. 1996. PMID: 8951503
-
Synthesis and Antimicrobial Activity of 1,2-Benzothiazine Derivatives.Molecules. 2016 Jun 30;21(7):861. doi: 10.3390/molecules21070861. Molecules. 2016. PMID: 27376253 Free PMC article.
-
Piroxicam: a review of its pharmacological properties and therapeutic efficacy.Drugs. 1981 Sep;22(3):165-87. doi: 10.2165/00003495-198122030-00001. Drugs. 1981. PMID: 7021122 Review.
-
In vitro study of mediators of inflammation in multiple sclerosis.J Clin Immunol. 1989 Mar;9(2):84-96. doi: 10.1007/BF00916935. J Clin Immunol. 1989. PMID: 2541163
-
Inhibitory effects of anti-inflammatory drugs on type II collagen induced arthritis in rats.Ann Rheum Dis. 1987 Jul;46(7):543-8. doi: 10.1136/ard.46.7.543. Ann Rheum Dis. 1987. PMID: 3662643 Free PMC article.
MeSH terms
Substances
LinkOut - more resources
Full Text Sources