Design, synthesis, and in vitro pharmacology of new radiolabeled γ-hydroxybutyric acid analogues including photolabile analogues with irreversible binding to the high-affinity γ-hydroxybutyric acid binding sites
γ-Hydroxybutyric acid (GHB) is a psychotropic compound endogenous to the brain. Despite its potential physiological significance, the complete molecular mechanisms of action remain unexplained. To facilitate the isolation and identification of the high-affinity GHB binding site, we herein report the design and synthesis of the first 125I-labeled radioligands in the field, one of which contains a photoaffinity label which enables it to bind irreversibly to the high-affinity GHB binding sites.
Sabbatini, Paola,Wellendorph, Petrine,H?g, Signe,Pedersen, Martin H. F.,Br?uner-Osborne, Hans,Martiny, Lars,Fr?lund, Bente,Clausen, Rasmus P.
supporting information; experimental part
p. 6506 - 6510
(2010/11/18)
Synthesis of I-125 labeled photoaffinity rapamycin analogs
Two no-carrier-added 125I-labeled photoaffinity rapamycin analogs were prepared: 7-demethoxy-7-(4-azido-3-125I-benzyloxy)rapamycin (2) and its C28-C29 seco analog 3. The key reactions of the synthesis were subst
Shu, Arthur Y.L.,Yamashita, Dennis S.,Holt, Dennis A.,Heys, J. Richard
p. 227 - 237
(2007/10/03)
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