Binding affinities of mometasone furoate and related compounds including its metabolites for the glucocorticoid receptor of rat skin tissue.

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Isogai M, Shimizu H, Esumi Y, Terasawa T, Okada T, Sugeno K

Binding affinities of mometasone furoate and related compounds including its metabolites for the glucocorticoid receptor of rat skin tissue.

J Steroid Biochem Mol Biol. 1993 Feb;44(2):141-5.

PubMed ID

8439518 [ View in PubMed

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Abstract

The binding affinities of mometasone furoate (MF), its metabolites and related compounds for the glucocorticoid receptor of rat epidermis and dermis were measured. MF and its main metabolite exhibited binding affinities higher than those of alclomethasone dipropionate (ADP) and betamethasone dipropionate (BDP), but equivalent to betamethasone 17-valerate (BMV). For compound I (metabolite of MF), ADP, BDP and BMV, the binding affinity was found to be higher in epidermis relative to dermis. This difference in the dermal/epidermal binding ratio may be a favorable sign leading to a possible reduction of dermal collagen atrophy, a known side effect of glucocorticoids. In structure-binding relationship studies, esterification of the 17-OH by furoylation and introduction of the 9 alpha-Cl caused a marked increase of the binding affinity, whereas the 6 beta-hydroxylation led to a pronounced decrease.

DrugBank Data that Cites this Article

Drug Targets

Drug	Target	Kind	Organism	Pharmacological Action	Actions
Mometasone	Glucocorticoid receptor	Protein	Humans	Yes	Agonist	Details
Mometasone furoate	Glucocorticoid receptor	Protein	Humans	Yes	Not Available	Details