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

John R. Lever, Robert F. Dannals, Alan A. Wilson, Hayden T. Ravert, Ursula Scheffel, Beth J. Hoffman, Paul R. Hartig, Dean F. Wong, Henry N. Wagner

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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.

Original languageEnglish (US)
Pages (from-to)697-704
Number of pages8
JournalInternational Journal of Radiation Applications and Instrumentation.
Volume16
Issue number7
DOIs
StatePublished - 1989

ASJC Scopus subject areas

  • Medicine(all)

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