title: [(125)I]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 (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.
authors: Russell H. Morgan Department of Radiology and Radiological Science, Johns Hopkins School of Medicine, Baltimore, MD.
authors: Yongjun
authors: Y
authors: Gao
authors: Russell H. Morgan Department of Radiology and Radiological Science, Johns Hopkins School of Medicine, Baltimore, MD.
authors: Ronnie C
authors: RC
authors: Mease
authors: Department of Pharmacology & Physiology, Georgetown University School of Medicine, Washington, DC.
authors: Thao T
authors: TT
authors: Olson
authors: Department of Pharmacology & Physiology, Georgetown University School of Medicine, Washington, DC.
authors: Kenneth J
authors: KJ
authors: Kellar
authors: Russell H. Morgan Department of Radiology and Radiological Science, Johns Hopkins School of Medicine, Baltimore, MD.
authors: Robert F
authors: RF
authors: Dannals
authors: Russell H. Morgan Department of Radiology and Radiological Science, Johns Hopkins School of Medicine, Baltimore, MD.
authors: Martin G
authors: MG
authors: Pomper
authors: Russell H. Morgan Department of Radiology and Radiological Science, Johns Hopkins School of Medicine, Baltimore, MD. Electronic address: ahorti1@jhmi.edu.
authors: Andrew G
authors: AG
authors: Horti
mesh_terms: D000818:Animals; D053961:Azabicyclo Compounds / Q000737:chemistry* / Q000378:metabolism*; D001921:Brain / Q000378:metabolism; D003499:Cyclic S-Oxides / Q000737:chemistry* / Q000378:metabolism*; D057809:HEK293 Cells; D006801:Humans; D007457:Iodine Radioisotopes / Q000737:chemistry*; D008024:Ligands; D008297:Male; D051379:Mice; D011854:Radiochemistry; D011978:Receptors, Nicotinic / Q000378:metabolism; D044406:Receptors, Serotonin, 5-HT3 / Q000378:metabolism; D013379:Substrate Specificity; D064569:alpha7 Nicotinic Acetylcholine Receptor / Q000378:metabolism*
chemical_list: C585155:3-(1,4-diazabicyclo(3.2.2)nonan-4-yl)-6-fluorodibenzo(b,d)thiophene 5,5-dioxide; D053961:Azabicyclo Compounds; D003499:Cyclic S-Oxides; D007457:Iodine Radioisotopes; D008024:Ligands; D011978:Receptors, Nicotinic; D044406:Receptors, Serotonin, 5-HT3; D064569:alpha7 Nicotinic Acetylcholine Receptor; C403531:nicotinic receptor alpha4beta2
keywords: Nicotinic acetylcholine receptor; SPECT; iodo-ASEM; α7-nAChR