[Pharmacologic study of the glucocorticoid activity of flunisolide compared with other steroids in the rat].
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.
Philibert
D
D
Centre de Recherches Roussel Uclaf, Romainville.
Bouchoux
F
F
Cerede
E
E
Corallo
F
F
Allaire
J M
JM
D000284:Administration, Oral; D000818:Animals; D001507:Beclomethasone / Q000031:analogs & derivatives / Q000494:pharmacology; D002478:Cells, Cultured; D004261:DNA Replication / Q000187:drug effects; D004790:Enzyme Induction / Q000187:drug effects; D005446:Fluocinolone Acetonide / Q000031:analogs & derivatives* / Q000378:metabolism / Q000494:pharmacology; D008099:Liver / Q000187:drug effects / Q000201:enzymology; D009928:Organ Specificity; D011485:Protein Binding; D051381:Rats; D011987:Receptors, Steroid / Q000378:metabolism; D013601:T-Lymphocytes / Q000187:drug effects; D014156:Transcortin / Q000378:metabolism; D014366:Tryptophan Oxygenase / Q000096:biosynthesis
D011987:Receptors, Steroid; D005446:Fluocinolone Acetonide; C065857:beclomethasone 17-monopropionate; C007734:flunisolide; D014156:Transcortin; D014366:Tryptophan Oxygenase; D001507:Beclomethasone
Etude pharmacologique de l'activité glucocorticoïde du flunisolide comparativement à d'autres stéroïdes chez le rat.