Synthesis and in vivo characterization of d-(+)-(N1-[11C]methyl)-2-Br-LSD: a radioligand for positron emission tomographic studies of serotonin 5-HT2 receptors |
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Institution: | 1. Synaptic Transmission In Vivo, Neuroscience Drug Discovery, H. Lundbeck A/S, Ottiliavej 9, DK-2500 Valby, Denmark;2. Sunred Pharma Consulting ApS, Svend Gønges Vej 11ADK, 2680 Solrød Strand, Denmark |
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Abstract: | d-(+)-Nl-Methyl-2-Br-LSD (MBL), which displays high affinity and selectivity for serotonin receptors in vitro, has been labeled with carbon-11 for localization of cerebral serotonin 5-HT2 receptors by positron emission tomography. 11C]MBL was prepared from 11C]iodomethane and d-(+)-2-Br-LSD within 20 min from end of bombardment. The average specific activity of 11C]MBL was 2300 mCi/μ mol and the average radiochemical yield was 17%, both at end of synthesis. The in vivo regional distribution of radioactivity in brain after i.v. administration of 11C]MBL to mice paralleled the known density of serotonin 5-HT2 receptors. The maximum specific binding, defined by a frontal cortex to cerebellum radioactivity concentration ratio of 5.4 to 1, was reached 30 min postinjection. Administration of ketanserin, a potent serotonin 5-HT2 receptor antagonist, markedly blocked radioligand binding in all brain regions examined except cerebellum. |
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