Female Sex Hormones Decrease Constitutive Endothelin-1 Release via Endothelial Sigma-1/Cocaine Receptors: An Action Independent of the Steroid Hormone Receptors
| Autor: | Andrea Plasse, Ute Wilbert-Lampen, Florian Straube, Anja Trapp, Christian Seliger |
|---|---|
| Rok vydání: | 2005 |
| Předmět: |
Receptors
Steroid medicine.medical_specialty Swine Physiology medicine.drug_class Receptors Drug medicine.medical_treatment Down-Regulation Pharmacology Sex hormone-binding globulin Internal medicine medicine Animals Humans Receptors sigma Testosterone Receptor Progesterone Dose-Response Relationship Drug Endothelin-1 Estradiol biology Chemistry Endothelial Cells Cell Biology General Medicine Sex hormone receptor Receptor antagonist Steroid hormone Endocrinology Hormone receptor biology.protein Female Carrier Proteins Hormone |
| Zdroj: | Endothelium. 12:185-191 |
| ISSN: | 1029-2373 1062-3329 |
| DOI: | 10.1080/10623320500227275 |
| Popis: | Cardiovascular disease is rare in premenopausal women compared to men. The authors investigate sex hormone-induced endothelin-1 (ET-1) release and the involvement of classic sex hormone receptors as well as the ability of sigma-1/cocaine receptors to respond to sex hormones. ET-1 release was measured in the supernatant of endothelial cells after treatment with beta-estradiol, progesterone, testosterone, or combined with their antagonists, and with the sigma-1 receptor ligand ditolylguanidine (DTG), or haloperidol, a sigma-1 receptor antagonist. Binding assays were performed using 2.5 x 10(-8) M [3H]DTG. Female sex hormones decreased ET-1 release whereas testosterone increased it, sex hormone antagonists only slightly attenuated or had no effect on the respective hormone's effect. DTG totally blocked the female sex hormone-induced inhibition on ET-1 release, whereas testosterone-induced stimulation was not affected. However, haloperidol blocked both. [3H]DTG binding was displaced by beta -estradiol but not by testosterone. DTG-binding sites account for 513 +/- 114 per cell, KD 8.79 nM. These data suggest that besides classic steroid hormone receptors, sigma-1/cocaine receptors mediate the effects of female sex hormones on ET-1 release, an up to now unknown signalling pathway. Results also suggest that female and male sex hormones may bind to different sites on sigma-1 receptors, exerting opposite pharmacological effects. |
| Databáze: | OpenAIRE |
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