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Characterization of Two [ 3 H]Ketanserin Recognition Sites in Rat Striatum
Author(s) -
Roth B. L.,
McLean S.,
Zhu X.Z.,
Chuang D.M.
Publication year - 1987
Publication title -
journal of neurochemistry
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.75
H-Index - 229
eISSN - 1471-4159
pISSN - 0022-3042
DOI - 10.1111/j.1471-4159.1987.tb02444.x
Subject(s) - ketanserin , striatum , binding site , dopaminergic , chemistry , serotonin , neuroscience , 5 ht receptor , biology , dopamine , biochemistry , receptor
Two [ 3 H]ketanserin recognition sites are present in the rat striatum. The high‐affinity site ( K d , 0.39 n M ) is similar to the 5‐hydroxytryptamine 2 (5‐HT 2 ) site previously characterized by various investigators. The low‐affinity site ( K d , 21.8 n M ) has a unique pharmacologic specificity and is preferentially localized to rat striatum and septum. Conventional 5‐HT 2 antagonists as well as 5‐HT and 5‐HT uptake inhibitors are ineffective at inhibiting [ 3 H]ketanserin binding to this low‐affinity site. Also, chronic treatment with p ‐chlorophenylalanine, which depletes brain 5‐HT, upregulates only the high‐affinity site. Thus, in the striatum and septum, [ 3 H]ketanserin labels a unique recognition site. This site has recently been shown to be associated with dopaminergic nerve endings and may regulate biogenic amine release.