[125I]Iodo-ASEM, a specific in vivo radioligand for α7-nAChR

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 (1600 Ci/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.