Binding of oral contraceptive progestogens to serum proteins and cytoplasmic receptor.

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Juchem M, Pollow K

Binding of oral contraceptive progestogens to serum proteins and cytoplasmic receptor.

Am J Obstet Gynecol. 1990 Dec;163(6 Pt 2):2171-83. doi: 10.1016/0002-9378(90)90559-p.

PubMed ID

2175153 [ View in PubMed

]

Abstract

Some progesterones widely used in oral contraceptives are characterized at the level of high-affinity receptor binding as well as binding to sex hormone-binding globulin and corticosteroid-binding globulin. With regard to binding to sex hormone-binding globulin, gestodene, levonorgestrel, and to a lesser extent 3-ketodesogestrel (which is only formed from the prodrug desogestrel in the body), show a behavior that is manifested in the relatively high affinity to sex hormone-binding globulin, whereas desogestrel and norgestimate do not display any measurable affinity for this specific steroid-binding serum protein. Furthermore, levonorgestrel and gestodene dissociate very much more slowly from the binding sites of sex hormone-binding globulin than 3-ketodesogestrel. A natural affinity of all these synthetic progestogens tested for corticosteroid-binding globulin could not be established. Gestodene, levonorgestrel, and 3-ketodesogestrel bind to the progesterone, glucocorticoid, and androgen receptor with high affinity, apart from slight differences, whereas estrogen receptor affinity could not be demonstrated in any of the progestogens investigated. In relation to aldosterone, the relative binding affinity values of gestodene, levonorgestrel, and the natural progestogen progesterone are relatively high, whereas 3-ketodesogestrel does not display any measurable affinity for this receptor species.

DrugBank Data that Cites this Article

Drugs

Levonorgestrel

Drug Targets

Drug	Target	Kind	Organism	Pharmacological Action	Actions
Desogestrel	Estrogen receptor alpha	Protein	Humans	Yes	Agonist	Details
Levonorgestrel	Glucocorticoid receptor	Protein	Humans	Unknown	Binder	Details
Norgestimate	Estrogen receptor alpha	Protein	Humans	Yes	Agonist	Details