(/sup 3/H)nitrendipine binding to adrenal capsular membranes
The physiologic regulation of aldosterone secretion is dependent on extracellular calcium and appears to be mediated by increases in cytosolic free calcium concentration in the zona glomerulosa cell. A specific role for voltage-dependent calcium channels was suggested by previous studies with the calcium channel antagonist verapamil. The authors therefore studied the (/sup 3/H)nitrendipine calcium channel binding site in adrenal capsules. These studies revealed a single class of saturable, high affinity sites with K/sub D/ = .26 +/- .04 nM and B/sub max/ = 105 +/- 5.7 fmol/mg protein. Specific binding of (/sup 3/H)nitrendipine was inhibited by calcium channel antagonists with potencies nitrendipine = nifedipine >> verapamil, while diltiazem had no inhibitory effect. In the rat, binding sites for (/sup 3/H)nitrendipine were located in the adrenal capsule and medulla and were undetectable in the zona fasciculata. Physiologic studies with collagenase-dispersed adrenal glomerulosa cells demonstrated that nifedipine selectively inhibited angiotensin-II and potassium-stimulated steroidogenesis. These observations suggest both a pharmacologic and physiologic role for the nitrendipine binding site in aldosterone production. 17 references, 2 figures, 1 table.
- Research Organization:
- National Institutes of Health, Bethesda, MD
- OSTI ID:
- 5826154
- Journal Information:
- Life Sci.; (United States), Journal Name: Life Sci.; (United States) Vol. 35:8; ISSN LIFSA
- Country of Publication:
- United States
- Language:
- English
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59 BASIC BIOLOGICAL SCIENCES
ADRENAL GLANDS
ADRENAL HORMONES
AFFINITY
ALDEHYDES
ALDOSTERONE
ALKALI METALS
ALKALINE EARTH METALS
ANIMALS
AUTONOMIC NERVOUS SYSTEM AGENTS
BODY
CALCIUM
CHEMICAL BONDS
CORTICOSTEROIDS
DRUGS
ELEMENTS
ENDOCRINE GLANDS
GLANDS
HORMONES
HYDROXY COMPOUNDS
INHIBITION
ISOTOPE APPLICATIONS
KETONES
LABELLED COMPOUNDS
MAMMALS
METALS
MINERALOCORTICOIDS
ORGANIC COMPOUNDS
ORGANS
PHYSIOLOGY
POTASSIUM
PREGNANES
RATS
RODENTS
STEROID HORMONES
STEROIDS
SYMPATHOLYTICS
TRACER TECHNIQUES
TRITIUM COMPOUNDS
VERTEBRATES