Abstract
[(125)I]Iodo-ASEM, a new radioligand with high affinity and selectivity for α7-nAChRs (K(i) = 0.5 nM; α7/α4β2 = 3414), has been synthesized in radiochemical yield of 33 ± 6% from the corresponding di-butyltriazene derivative and at high specific radioactivity (1600Ci/mmol; 59.2 MBq/μmol). [(125)I]Iodo-ASEM readily entered the brains of normal CD-1 mice and specifically and selectively labeled cerebral α7-nAChRs. [(125)I]iodo-ASEM is a new useful tool for studying α7-nAChR.
Keywords:
Nicotinic acetylcholine receptor; SPECT; iodo-ASEM; α7-nAChR.
Copyright © 2014 Elsevier Inc. All rights reserved.
Publication types
-
Research Support, N.I.H., Extramural
-
Research Support, Non-U.S. Gov't
MeSH terms
-
Animals
-
Azabicyclo Compounds / chemistry*
-
Azabicyclo Compounds / metabolism*
-
Brain / metabolism
-
Cyclic S-Oxides / chemistry*
-
Cyclic S-Oxides / metabolism*
-
HEK293 Cells
-
Humans
-
Iodine Radioisotopes / chemistry*
-
Ligands
-
Male
-
Mice
-
Radiochemistry
-
Receptors, Nicotinic / metabolism
-
Receptors, Serotonin, 5-HT3 / metabolism
-
Substrate Specificity
-
alpha7 Nicotinic Acetylcholine Receptor / metabolism*
Substances
-
3-(1,4-diazabicyclo(3.2.2)nonan-4-yl)-6-fluorodibenzo(b,d)thiophene 5,5-dioxide
-
Azabicyclo Compounds
-
Cyclic S-Oxides
-
Iodine Radioisotopes
-
Ligands
-
Receptors, Nicotinic
-
Receptors, Serotonin, 5-HT3
-
alpha7 Nicotinic Acetylcholine Receptor
-
nicotinic receptor alpha4beta2