Screening and Assessment of the Potency of Anti-Inflammatory Drugs in vitro

Gryglewski, R. J.

doi:10.1007/978-3-642-66891-3_1

R. J. Gryglewski

Part of the book series: Handbook of Experimental Pharmacology ((HEP,volume 50 / 2))

184 Accesses
14 Citations

Abstract

Many in vitro models have been developed to predict the anti-inflammatory potency of newly synthesized compounds, but none of these methods is satisfactory. Glenn et al. (1973) stated bluntly: “All of these in vitro methods are virtually useless for a predictive assessment of drugs in vivo. They are useful only after drugs are discovered in other systems.” The above statement was justified when in vitro methods relied entirely on non-specific interactions between non-steroid anti-inflammatory agents (NSAID) and a variety of proteins. However, it has been discovered that the target biomolecule for NSAID is fatty acid cyclo-oxygenase, a component of the prostaglandin (PG) synthetase system (Vane, 1971; Smith and Willis, 1971; Ferreira et al., 1971; see also Section C.III). Consequently, in vitro assessment of the inhibition of PG synthetase seems to be the rational approach for screening of compounds for their anti-inflammatory activity. The search for new NSAID of various chemical structures has been extensively reviewed (Shen, 1972; Scherrer and Whitehouse, 1974). In this chapter, the in vitro screening procedures for acidic NSAID will mainly be discussed.

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R. J. Gryglewski
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The Wellcome Research Laboratories, Langley Court, BR3 3BS, Beckenham, Kent, UK
John R. Vane
Faculdade de Medicina de Ribeirão Preto, Universidade de São Paulo, CEP 14.100, São Paulo, Brazil
Sergio H. Ferreira

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Gryglewski, R.J. (1979). Screening and Assessment of the Potency of Anti-Inflammatory Drugs in vitro. In: Vane, J.R., Ferreira, S.H. (eds) Anti-Inflammatory Drugs. Handbook of Experimental Pharmacology, vol 50 / 2. Springer, Berlin, Heidelberg. https://doi.org/10.1007/978-3-642-66891-3_1

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DOI: https://doi.org/10.1007/978-3-642-66891-3_1
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Screening and Assessment of the Potency of Anti-Inflammatory Drugs in vitro

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CADD Approaches in Anti-inflammatory Drug Discovery

Of rodents, research and relationships: a pharmacological odyssey

Ulcerogenicity devoid novel non-steroidal anti-inflammatory agents (NSAIDS): syntheses, computational studies, and activity of 5-aryliden-2-imino-4-thiazolidinones

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