| Identification | Back Directory | [Name]
4-(2-(2,4,6-Trifluorophenoxymethyl)phenyl)piperidine | [CAS]
1227056-84-9 | [Synonyms]
TD9855
TD-9855
4-(2-(2,4,6-Trifluorophenoxymethyl)phenyl)piperidine
Piperidine, 4-[2-[(2,4,6-trifluorophenoxy)methyl]phenyl]- | [Molecular Formula]
C18H18F3NO | [MOL File]
1227056-84-9.mol | [Molecular Weight]
321.34 |
| Hazard Information | Back Directory | [Uses]
Ampreloxetine (TD-9855) is a potent and orally active norepinephrine (NE) and serotonin 5-HT inhibitor. Ampreloxetine has the potential for the research of neurogenic orthostatic hypotension[1][2]. | [in vivo]
Ampreloxetine (0.3, 1, 5, 10, 30, 60 mg/kg; p.o.; single dose) shows a plasma EC50s of 11.7ng/mL and 50.8ng/mL in rat, respectively[1]. | Animal Model: | Male Sprague Dawley rats[1] | | Dosage: | 0.3, 1, 5, 10, 30, 60 mg/kg | | Administration: | P.o.; single dose | | Result: | Showed good PK and PD parameter with Emax of 79%, 92% for SERT and NET, respectively; EC50 values of 50.8, 11.7 ng/mL for SERT, NET, respectively. |
| [IC 50]
5-HT Receptor | [References]
[1] Smith JA, et al. Preclinical to clinical translation of CNS transporter occupancy of TD-9855, a novel norepinephrine and serotonin reuptake inhibitor. Int J Neuropsychopharmacol. 2014 Dec 13;18(2):pyu027. DOI:10.1093/ijnp/pyu027
[2] Kaufmann H, et al. Safety and efficacy of ampreloxetine in symptomatic neurogenic orthostatic hypotension: a phase 2 trial. Clin Auton Res. 2021 Dec;31(6):699-711. DOI:10.1007/s10286-021-00827-0 |
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