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https://www.um.edu.mt/library/oar/handle/123456789/23743
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. |
URI: | https://www.um.edu.mt/library/oar//handle/123456789/23743 |
Appears in Collections: | Scholarly Works - FacM&SPsy |
Files in This Item:
File | Description | Size | Format | |
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10.10072Fs00213-004-1817-7.pdf Restricted Access | 299.6 kB | Adobe PDF | View/Open Request a copy |
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