| Identification | Back Directory | [Name]
CX-1632 | [CAS]
1038984-31-4 | [Synonyms]
S47445 S-47445 CX-1632 S 47445 Tulrampator (CX-1632) Tulrampator 1038984-31-4 Tulrampator (Synonyms: CX-1632) TULRAMPATOR; S-47445; S 47445; S47445; CX-1632; CX 1632; CX1632; 3H-[1,3]Oxazino[6,5-g]-1,2,3-benzotriazine-4,9-dione, 8-cyclopropyl-3-[2-(3-fluorophenyl)ethyl]-7,8-dihydro- | [Molecular Formula]
C20H17FN4O3 | [MDL Number]
MFCD31807599 | [MOL File]
1038984-31-4.mol | [Molecular Weight]
380.37 |
| Chemical Properties | Back Directory | [storage temp. ]
Store at -20°C | [solubility ]
DMSO:21.67(Max Conc. mg/mL);56.97(Max Conc. mM) | [form ]
Solid | [color ]
Light yellow to yellow |
| Hazard Information | Back Directory | [Uses]
Tulrampator (S-47445) is an orally active selective AMPA receptor modulator. Tulrampator possesses procognitive, enhancing synaptic plasticity, anti-depressant-anxiolytic-like, procognitive and potential neuroprotective properties. Tulrampator can be used for research of alzheimer’s disease and in major depressive disorder[1][2][3]. | [in vivo]
Tulrampator (0.3-10 mg/kg, Oral gavage, once a day for 4-5 weeks) has anxiolytic-like and antidepressant-like effects in the CORT Mice Model[2].
Tulrampator (1-10 mg/kg, Intraperitoneal injection, once a day for 4 weeks) reverts olfactory bulbectomy (OB)-induced hyperactivity and anxiety in bilateral olfactory bulbectomy mice model[3]. | Animal Model: | chronic corticosterone administration (CORT) mice[2] | | Dosage: | 0.3 mg/kg, 1 mg/kg, 3 mg/kg, 10 mg/kg | | Administration: | Oral gavage (p.o.) | | Result: | Reversed anxio-depressive phenotype in a neurogenesis-dependent task.
Decreased the corticosterone-induced increase in emotionality.
Had a rapid onset of effect on anhedonia in the rat Chronic Mild Stress (CMS) model.
Stimulated cell proliferation, survival and neuronal maturation in the dentate gyrusof the hippocampus.
|
| Animal Model: | bilateral olfactory bulbectomy mice model[3] | | Dosage: | 1 mg/kg, 3 mg/kg, 10 mg/kg | | Administration: | Intraperitoneal injection (i.p.) | | Result: | Significantly reverted OB-induced hyperactivity after 28 days.
Increased open field central activity in OB mice.
|
| [References]
[1] Bretin S, et al. Pharmacological characterisation of S 47445, a novel positive allosteric modulator of AMPA receptors [J]. PLoS One, 2017, 12(9): e0184429. [2] Mendez-David I, et al. S 47445 produces antidepressant-and anxiolytic-like effects through neurogenesis dependent and independent mechanisms [J]. Frontiers in pharmacology, 2017, 8: 462. [3] Pilar-Cuellar F, et al. S 47445 counteracts the behavioral manifestations and hippocampal neuroplasticity changes in bulbectomized mice [J]. Progress in Neuro-Psychopharmacology and Biological Psychiatry, 2019, 93: 205-213. [4] Wilkinson ST, et al. A new generation of antidepressants: an update on the pharmaceutical pipeline for novel and rapid-acting therapeutics in mood disorders based on glutamate/GABA neurotransmitter systems. Drug Discov Today. 2018 Nov 14. pii: S1359-6446(18)30376-3. DOI:10.1016/j.drudis.2018.11.007 |
|
|