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Characterization of central melatonin receptors using 125 I‐melatonin
Author(s) -
Laudon Moshe,
Zisapel Nava
Publication year - 1986
Publication title -
febs letters
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.593
H-Index - 257
eISSN - 1873-3468
pISSN - 0014-5793
DOI - 10.1016/0014-5793(86)80287-3
Subject(s) - melatonin , melatonin receptor , receptor , characterization (materials science) , chemistry , biochemistry , medicine , endocrinology , biology , nanotechnology , materials science
The binding of 125 I‐melatonin, a potent analog of melatonin, to rat brain synaptosomal preparations was investigated. 125 I‐melatonin bound with high affinity ( K d = 38 nM) to a single class of sites ( B max = 81 protein). Kinetic studies indicated that binding was time‐dependent and reversible. Specific 125 I‐melatonin binding was inhibited by melatonin, and was unaffected by other structurally related compounds including serotonin. Binding of 125 I‐melatonin was greatly reduced if the synaptosomal preparations were pretreated by heat or trypsin but was unaffected by freeze‐thawing. These results suggest that 125 I‐melatonin may serve as a valuable probe for studying melatonin receptors.