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Binding and uptake studies with [ 3 H]CP‐93, 129, a radiolabeled selective 5‐HT 1B receptor ligand
Author(s) -
Koe B. Kenneth,
Lebel Lorraine A.,
Fox Carol B.,
Macor John E.
Publication year - 1992
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.430250107
Subject(s) - desipramine , agonist , chemistry , ligand (biochemistry) , serotonin , receptor , 5 ht receptor , binding site , pharmacology , stereochemistry , biochemistry , endocrinology , biology , antidepressant , hippocampus
3‐(1,2,5,6‐Tetrahydro‐4‐pyridyl)‐5‐pyrrolo[3,2‐b]pyridone, CP‐93, 129, is a selective agonist ligand for 5‐HT 1B receptors. High affinity binding sites of [ 3 H]CP‐93, 129 were found in rat whole brain membranes, which showed K D and B max values similar to those for 5‐HT 1B sites labeled by [ 3 H]5‐HT. Uptake of [ 3 H]CP‐93, 129 in crude rat synaptosomes was also observed, which was potently inhibited by 5‐HT uptake blockers and 5‐HT but not by desipramine (NE uptake blocker) or tametraline (NE and DA uptake blocker). Because of this sensitivity to 5‐HT uptake inhibitors and the structural similarity of CP‐93, 129 to serotonin, [ 3 H]CP‐93, 129 uptake probably occurred in 5‐HT neurons.