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Title: EMD 281014, a specific and potent 5HT2 antagonist in humans : a dose-finding PET study
Authors: Mamo, David
Sedman, Ewen
Tillner, Joachim
Sellers, Edward M.
Romach, Myroslava K.
Kapur, Shitij
Keywords: Tomography, Emission
Clinical trials
Issue Date: 2004
Publisher: Springer
Citation: Mamo, D., Sedman, E., Tillner, J., Sellers, E. M., Romach, M. K., & Kapur, S. (2004). EMD 281014, a specific and potent 5HT2 antagonist in humans: a dose-finding PET study. Psychopharmacology, 175(3), 382-388.
Abstract: While serotonin 5HT2-receptors have been im- plicated in the etiology and pharmacological treatment of a number of neuropsychiatric conditions, there are few potent and specific agents available for use in human clinical studies. EMD 281014 is a highly specific 5HT2- receptor antagonist that is currently under development. To find optimal doses for early clinical studies, we conducted a PET study using [18F]setoperone in nine healthy subjects scanned at baseline and following the administration of 1, 3, and 7 mg EMD 281014. The study drug was well tolerated by all study participants, and all doses resulted in 70% occupancy at frontal 5HT2- receptors 3 h after drug administration. The data suggest that daily dosing of 3 mg EMD 281014 should be sufficient to provide sustained high levels of 5HT2- receptor occupancy in future clinical trials.
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