Regulation of renal peripheral benzodiazepine receptors by anion transport inhibitors
The in vitro and in vivo regulation of (/sup 3/H)Ro 5-4864 binding to peripheral benzodiazepine receptors (PBR) by ion transport/exchange inhibitors was studied in the kidney. The potencies of 9-anthroic acid, furosemide, bumetanide, hydrochlorothiazide and SITS as inhibitors of (/sup 3/H)Ro 5-4864 binding to renal membranes were consistent with their actions as anion transport inhibitors (Ki approx. = 30 - 130 ..mu..M). In contrast, spironolactone, amiloride, acetazolamide, and ouabain were less potent (Ki=100-1000 ..mu..M). Administration of furosemide to rats for five days resulted in a profound diuresis accompanied by a significant increase in PBR density (43%) that was apparent by the fifth day of treatment. Administration of hydrochlorothiazide or Ro 5-4864 for five days also caused diuresis and increased renal PBR density. Both the diuresis and increased density of PBR produced by Ro 5-4864 were blocked by coadministration of PK 11195, which alone had no effect on either PBR density or urine volume. The equilibrium binding constants of (/sup 3/H)Ro 5-4864 to cardiac membranes were unaffected by administration of any of these drugs. These findings suggest that renal PBR may be selectively modulated in vivo and in vitro by administration of ion transport/exchange inhibitors. 36 references, 4 tables.
- Research Organization:
- National Institutes of Health, Bethesda, MD
- OSTI ID:
- 5403569
- Journal Information:
- Life Sci.; (United States), Vol. 42:6
- Country of Publication:
- United States
- Language:
- English
Similar Records
Subcellular localization and displacement by diuretics of the peripheral benzodiazepine binding site (PBS) from rat kidney
Aldosterone-reversible decrease in the density of renal peripheral benzodiazepine receptors in the rat after adrenalectomy
Related Subjects
ANIONS
MEMBRANE TRANSPORT
DIURETICS
BIOCHEMICAL REACTION KINETICS
TRANQUILIZERS
RECEPTORS
CELL MEMBRANES
EXPERIMENTAL DATA
IN VITRO
IN VIVO
ION EXCHANGE
KIDNEYS
TRACER TECHNIQUES
TRITIUM COMPOUNDS
BODY
CELL CONSTITUENTS
CENTRAL NERVOUS SYSTEM AGENTS
CHARGED PARTICLES
DATA
DRUGS
INFORMATION
IONS
ISOTOPE APPLICATIONS
KINETICS
LABELLED COMPOUNDS
MEMBRANE PROTEINS
MEMBRANES
NUMERICAL DATA
ORGANIC COMPOUNDS
ORGANS
PROTEINS
PSYCHOTROPIC DRUGS
REACTION KINETICS
550201* - Biochemistry- Tracer Techniques