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

Nucl Med Biol. 2015 May;42(5):488-493. doi: 10.1016/j.nucmedbio.2014.12.008. Epub 2014 Dec 20.

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.

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