| Autor: |
Ryosuke, Arakawa, Akihiro, Takano, Sangram, Nag, Zhisheng, Jia, Nahid, Amini, Kevin P, Maresca, Lei, Zhang, Edmund J, Keliher, Christopher R, Butler, Justin R, Piro, Tarek A, Samad, Deborah, Smith, Deane, Nason, Steve, O'Neil, Patrick, Trapa, Kari R, Fonseca, John, Litchfield, Timothy, McCarthy, Richard E, Carson, Christer, Halldin |
| Rok vydání: |
2021 |
| Zdroj: |
EJNMMI research. 12(1) |
| ISSN: |
2191-219X |
| Popis: |
Monoacylglycerol lipase (MAGL) is a key serine hydrolase which terminates endocannabinoid signaling and regulates arachidonic acid driven inflammatory responses within the central nervous system. To develop [Seven cynomolgus monkeys were enrolled for brain PET measurements. Two PET measurements along with arterial blood sampling were performed in each NHP: one baseline and one pretreatment condition with intravenous administration of PF-06818883, a pro-drug of a selective MAGL inhibitor (total of seven doses between 0.01 and 1.27 mg/kg). Kinetic parameters KRadioactivity retention was decreased in all brain regions following pretreatment with PF-06818883. Occupancy was measured as 25.4-100.5% in a dose dependent manner. Whole-body PET showed high radioactivity uptake values in the liver, small intestine, kidney, and brain. The effective dose of [[ |
| Databáze: |
OpenAIRE |
| Externí odkaz: |
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