( S )-5-(2'-Fluorophenyl)- N , N -dimethyl-1,2,3,4-tetrahydronaphthalen-2-amine, a Serotonin Receptor Modulator, Possesses Anticonvulsant, Prosocial, and Anxiolytic-like Properties in an Fmr1 Knockout Mouse Model of Fragile X Syndrome and Autism Spectrum Disorder.
Autor: | Armstrong JL; Department of Pharmaceutical Sciences, College of Pharmacy, Mercer University Health Sciences Center, Mercer University, 3001 Mercer University Drive, Atlanta, Georgia 30341, United States., Casey AB; Center for Drug Discovery, Department of Pharmaceutical Sciences, and Department of Chemistry and Chemical Biology, Northeastern University, Boston, Massachusetts 02131, United States., Saraf TS; Department of Pharmaceutical Sciences, College of Pharmacy, Mercer University Health Sciences Center, Mercer University, 3001 Mercer University Drive, Atlanta, Georgia 30341, United States., Mukherjee M; Center for Drug Discovery, Department of Pharmaceutical Sciences, and Department of Chemistry and Chemical Biology, Northeastern University, Boston, Massachusetts 02131, United States., Booth RG; Center for Drug Discovery, Department of Pharmaceutical Sciences, and Department of Chemistry and Chemical Biology, Northeastern University, Boston, Massachusetts 02131, United States., Canal CE; Department of Pharmaceutical Sciences, College of Pharmacy, Mercer University Health Sciences Center, Mercer University, 3001 Mercer University Drive, Atlanta, Georgia 30341, United States. |
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Jazyk: | angličtina |
Zdroj: | ACS pharmacology & translational science [ACS Pharmacol Transl Sci] 2020 Feb 21; Vol. 3 (3), pp. 509-523. Date of Electronic Publication: 2020 Feb 21 (Print Publication: 2020). |
DOI: | 10.1021/acsptsci.9b00101 |
Abstrakt: | Fragile X syndrome (FXS) is a neurodevelopmental disorder characterized by intellectual disabilities and a plethora of neuropsychiatric symptoms. FXS is the leading monogenic cause of autism spectrum disorder (ASD), which is defined clinically by repetitive and/or restrictive patterns of behavior and social communication deficits. Epilepsy and anxiety are also common in FXS and ASD. Serotonergic neurons directly innervate and modulate the activity of neurobiological circuits altered in both disorders, providing a rationale for investigating serotonin receptors (5-HTRs) as targets for FXS and ASD drug discovery. Previously we unveiled an orally active aminotetralin, ( S )-5-(2'-fluorophenyl)- N,N -dimethyl-1,2,3,4-tetrahydronaphthalen-2-amine (FPT), that exhibits partial agonist activity at 5-HT Competing Interests: The authors declare no competing financial interest. (Copyright © 2020 American Chemical Society.) |
Databáze: | MEDLINE |
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