2-([sup 125]I) iodomelatonin binding sites in rat adrenals: Pharmacological characteristics and subcellular distribution

Journal Article · Wed Jan 01 00:00:00 EST 1992 · Life Sciences; (United States)

DOI:https://doi.org/10.1016/0024-3205(92)90237-J· OSTI ID:7160946

Persengiev, S P ^[1]

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1. Bulgarian Academy of Sciences, Sofia (Bulgaria)

Specific binding sites for 2-[[sup 125]I] iodomelatonin, a selective radiolabeled melatonin receptor ligand, were detected and characterized in rat adrenal membranes. Saturation studies demonstrated that 2-[[sup 125]I]iodomelatonin binds to a single class of sites with an affinity constant (Kd) of 541 pM and a total binding capacity (Bmax) of 3.23 fmol/mg protein. Competition experiments revealed that the relative order of potency of compounds tested was as follows: 6-chloromelatonin > 2-iodomelatonin > melatonin > 5-methoxytryptamine > 5-methoxytryptophol. The highest density of binding sites was found in membranes from nuclear and mitochondrial subcellular fractions.

• OSTI ID: 7160946
• Journal Information: Life Sciences; (United States), Vol. 51:9; ISSN 0024-3205
• Country of Publication: United States
• Language: English

Related Subjects

59 BASIC BIOLOGICAL SCIENCES
MELATONIN
RECEPTORS
SUBCELLULAR DISTRIBUTION
ADRENAL GLANDS
AFFINITY
BIOCHEMICAL REACTION KINETICS
CELL MEMBRANES
CHEMICAL COMPOSITION
LIGANDS
PHARMACOLOGY
RATS
AMINES
ANIMALS
AROMATICS
AZAARENES
AZOLES
BODY
CELL CONSTITUENTS
DISTRIBUTION
ENDOCRINE GLANDS
GLANDS
HETEROCYCLIC COMPOUNDS
INDOLES
KINETICS
MAMMALS
MEMBRANE PROTEINS
MEMBRANES
ORGANIC COMPOUNDS
ORGANIC NITROGEN COMPOUNDS
ORGANS
PROTEINS
PYRROLES
REACTION KINETICS
RODENTS
TRYPTAMINES
VERTEBRATES
550201* - Biochemistry- Tracer Techniques