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OIDV and OBDV showed greater binding affinity to VAChT (K(i) = 20.5 ± 5.6 and 13.8 ± 1.2 nM, respectively) than did vesamicol (K(i) = 33.9 ± 18.1 nM) with low affinity to σ receptors. A saturation binding assay in rat cerebral membranes revealed that [(125)I]OIDV had a single high affinity binding site with a K(d) value of 1.73 nM and a B(max) value of 164.4 fmol/mg protein. [(125)I]OIDV revealed little competition with inhibitors, which possessed specific affinity to each σ (σ-1 and σ-2), serotonin (5-HT(1A) and 5-HT(2A)), noradrenaline, and muscarinic acetylcholine receptors. In addition, BBB penetration of [(125)I]OIDV was verified in in vivo. The results of the binding studies indicated that OIDV and OBDV had great potential to be VAChT imaging probes with high affinity and selectivity."}]}],"creator":[{"@id":"https://cir.nii.ac.jp/crid/1420564276164221952","@type":"Researcher","personIdentifier":[{"@type":"KAKEN_RESEARCHERS","@value":"50579836"},{"@type":"NRID","@value":"1000050579836"},{"@type":"NRID","@value":"9000391960075"},{"@type":"NRID","@value":"9000290381057"},{"@type":"NRID","@value":"9000415305104"},{"@type":"NRID","@value":"9000415082176"},{"@type":"NRID","@value":"9000023210972"},{"@type":"NRID","@value":"9000415082325"},{"@type":"NRID","@value":"9000020700914"},{"@type":"NRID","@value":"9000409576207"},{"@type":"NRID","@value":"9000020685103"},{"@type":"NRID","@value":"9000414112028"},{"@type":"RESEARCHMAP","@value":"https://researchmap.jp/7000007804"}],"foaf:name":[{"@value":"Takashi Kozaka"}]},{"@id":"https://cir.nii.ac.jp/crid/1380004232015198594","@type":"Researcher","foaf:name":[{"@value":"Izumi 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