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Unusual binding of [ 3 H] MDL 72222 in guinea pig hippocampus
Author(s) -
Meyerson Laurence R.,
Park Hyoungsup
Publication year - 1991
Publication title -
drug development research
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.582
H-Index - 60
eISSN - 1098-2299
pISSN - 0272-4391
DOI - 10.1002/ddr.430230103
Subject(s) - guinea pig , population , biology , chemistry , endocrinology , sociology , demography
Abstract [ 3 H] MDL 72222 labeled a non‐homogeneous population of sites in guinea pig hippocampal membranes (K d1 = 1 nM; K d2 = 60 nM). The binding was not sodium dependent. Competition studies with a variety of characterizing agents showed displacement of [ 3 H] MDL 72222 binding by 5‐HT uptake inhibitors. [ 3 H] MDL 72222 binding was not effectively displaced by established 5‐HT 3 antagonists. MDL 72222, fluoxetine, fluvoxamine and citalopram competitively inhibited the uptake of [ 3 H] 5‐HT into guinea pig hippocampal synaptosomes with K i values of 1.97, 0.02, 0.023, 0.049 μM, respectively. The results demonstrate that [ 3 H] MDL 72222 labels a non‐homogeneous population of sites in guinea pig brain, as well as inhibiting 5‐HT uptake into synaptosomal preparations.