Is AL-438 likely to have fewer side effects than the glucocorticoids?

Abstract

The glucocorticoids are effective anti-inflammatory agents but their use may be limited by systemic side effects. AL-438 and prednisolone inhibit binding to glucocorticoid and mineralcorticoid receptors with similar potency. In rat models of acute and chronic inflammation, AL-438 was effective but less potent than prednisolone. In fasted overnight rats, prednisolone was hyperglycaemic but AL-438 was not. Prednisolone also inhibited bone formation in rats, whereas AL-438 did not. The differing profile of AL-438 relative to prednisolone may be due to altered interactions between the receptor and selected co-activators. AL-438 may have lesser side effects than prednisolone.

• Authors: Sheila Doggrell
• Journal: Expert opinion on investigational drugs (Expert Opin Investig Drugs) Vol. 12 Issue 7 Pg. 1227-9 (Jul 2003) ISSN: 1354-3784 [Print] England
• PMID: 12831356 (Publication Type: Journal Article)

Chemical References

• 10-methoxy-5-(2-propenyl)-2,5-dihydro-2,2,4-trimethyl-1H-(1)benzopyrano(3,4-f)quinoline
• Anti-Inflammatory Agents
• Anti-Inflammatory Agents, Non-Steroidal
• Benzopyrans
• Glucocorticoids
• Quinolines
• Receptors, Glucocorticoid
• Prednisolone

Topics

• Animals
• Anti-Inflammatory Agents (adverse effects)
• Anti-Inflammatory Agents, Non-Steroidal (adverse effects, pharmacokinetics)
• Benzopyrans (adverse effects, pharmacokinetics)
• Drug Delivery Systems
• Gene Expression Regulation (drug effects)
• Glucocorticoids (adverse effects, pharmacokinetics)
• Inflammation (genetics, pathology)
• Prednisolone (adverse effects)
• Quinolines (adverse effects, pharmacokinetics)
• Rats
• Receptors, Glucocorticoid (genetics, metabolism)