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The development of additional radioligands of varying pharmacokinetics for the 5‐HT 1A receptor
Author(s) -
Lang L.,
Jagoda E. M.,
Eckelman W. C.
Publication year - 2001
Publication title -
journal of labelled compounds and radiopharmaceuticals
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.432
H-Index - 47
eISSN - 1099-1344
pISSN - 0362-4803
DOI - 10.1002/jlcr.2580440108
Subject(s) - chemistry , pharmacokinetics , pyrimidine , moiety , stereochemistry , ligand (biochemistry) , receptor , combinatorial chemistry , pharmacology , biochemistry , medicine
Six compounds have been prepared to further probe the structure activity relationships based on the 5‐HT 1A receptor ligand, WAY 100635. The goal is to obtain a series of radiotracers with varying pharmacokinetic properties. Substitution of a pyrimidine for a pyridine moiety, increased the specific binding ratio in the phenylcarboxamide series, but decreased the ratio in the cyclohexanecarboxamide series. A series of compounds with varying pharmacokinetic properties are now available to study a range of properties involving 5‐HT 1A receptor binding.