[Pharmacologic study of the glucocorticoid activity of flunisolide compared with other steroids in the rat].

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Philibert D, Bouchoux F, Cerede E, Corallo F, Allaire JM

[Pharmacologic study of the glucocorticoid activity of flunisolide compared with other steroids in the rat].

Allerg Immunol (Paris). 1993 Feb;25(2):77-81.

PubMed ID

8466638 [ View in PubMed

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Abstract

Flunisolide (FLU), beclomethasone dipropionate (BDP) and its pulmonary metabolites beclomethasone monopropionate (BMP) and beclomethasone (B) were studied in rat for: their relative binding affinity (RBA) for the 5 classes of steroid receptors, their in vitro glucocorticoid activity on rat thymocytes, their in vivo glucocorticoid activity by oral route. These compounds displayed a strong RBA for rat lung, thymus and liver glucocorticoid receptors (FLU > or = BMP > BDP > or = B). They were also shown to have a moderate RBA for both mineralocorticoid and progestin receptors, while being devoid of any binding to androgen and oestrogen receptors. On rat thymocytes FLU exhibited the highest glucocorticoid activity (FLU > B > or = BMP > BDP). In rat oral FLU displayed a strong glucocorticoid activity with a slight first-pass metabolism as opposed to what has been reported in human.

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Drug Targets

Drug	Target	Kind	Organism	Pharmacological Action	Actions
Flunisolide	Glucocorticoid receptor	Protein	Humans	Yes	Agonist	Details