[(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.
Download full-text PDF |
Source |
---|---|
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4387010 | PMC |
http://dx.doi.org/10.1016/j.nucmedbio.2014.12.008 | DOI Listing |
Molecules
March 2020
Neurobiology Research Unit, Copenhagen University Hospital, Rigshospitalet, DK-2100 Copenhagen, Denmark.
The α7 nicotinic acetylcholine receptor (α7 nAChR) is involved in several cognitive and physiologic processes; its expression levels and patterns change in neurologic and psychiatric diseases, such as schizophrenia and Alzheimer's disease, which makes it a relevant drug target. Development of selective radioligands is important for defining binding properties and occupancy of novel molecules targeting the receptor. We tested the in vitro binding properties of [I]Iodo-ASEM [(3-(1,4-diazabycyclo[3.
View Article and Find Full Text PDFNucl Med Biol
May 2015
Russell H. Morgan Department of Radiology and Radiological Science, Johns Hopkins School of Medicine, Baltimore, MD. Electronic address:
[(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).
View Article and Find Full Text PDFEnter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!