TAK-653
TAK-653 Basic information
- Product Name:
- TAK-653
- Synonyms:
-
- Pyrazino[2,1-c][1,2,4]thiadiazine, 9-[4-(cyclohexyloxy)phenyl]-3,4-dihydro-7-methyl-, 2,2-dioxide
- TAK-653
- Osavampator
- 9-(4-(Cyclohexyloxy)phenyl)-7-methyl-3,4-dihydropyrazino[2,1-c][1,2,4]thiadiazine 2,2-dioxide
- 9-[4-(cyclohexyloxy)phenyl]-7-methyl-3H,4H-2λ?-pyrazino[2,1-c][1,2,4]thiadiazine-2,2-dione
- NBI-1065845)
- Osavampator(TAK-653
- CAS:
- 1358751-06-0
- MF:
- C19H23N3O3S
- MW:
- 373.47
- Mol File:
- 1358751-06-0.mol
TAK-653 Chemical Properties
- Boiling point:
- 540.8±52.0 °C(Predicted)
- Density
- 1.38±0.1 g/cm3(Predicted)
- storage temp.
- Store at -20°C
- solubility
- DMSO: Slightly soluble: 0.1-1 mg/ml
- pka
- 1.71±0.40(Predicted)
- form
- Solid
- color
- White to yellow
- InChI
- InChI=1S/C19H23N3O3S/c1-14-13-22-11-12-26(23,24)21-19(22)18(20-14)15-7-9-17(10-8-15)25-16-5-3-2-4-6-16/h7-10,13,16H,2-6,11-12H2,1H3
- InChIKey
- PXJBHEHFVQVDDS-UHFFFAOYSA-N
- SMILES
- S1(=O)(=O)CCN2C=C(C)N=C(C3=CC=C(OC4CCCCC4)C=C3)C2=N1
TAK-653 Usage And Synthesis
Uses
Osavampator (TAK-653) is a AMPA receptor positive allosteric modulator. Osavampator selectively binds to AMPA-R in a glutamate-dependent manner and induces Ca2+ influx in hGluA1i CHO cells (EC50 = 3.3 μM). Osavampator improves learning and memory in many models. Osavampator is can be used for the research of depressive disorders[1][2].
Biological Functions
TAK-653 is a selective positive allosteric modulator (PAM) of AMPA receptors exhibiting minimal agonistic activity, elicits an antidepressant-like response while maintaining a favorable safety profile in rat models.
in vivo
Osavampator (0.03-0.3 mg/kg, p.o., single dose) enhances visual learning and memory in normal rats[2].
Osavampator (0.3 mg/kg, p.o., single dose) enhances sustained attention in the poor performing rats[2].
Osavampator (0.06 mg/kg, p.o., single dose) improves working memory in monkeys[2].
Osavampator (1 mg/kg, p.o., single dose) produces antidepressant-like effects in the rat RSBM (reduction of submissive behavior model)[1].
| Animal Model: | Normal rats[2] |
| Dosage: | 0.03 mg/kg, 0.1 mg/kg, 0.3 mg/kg |
| Administration: | Oral gavage (p.o.) |
| Result: | Improved the novelty discrimination index (NDI). |
| Animal Model: | Poor performing rats[2] |
| Dosage: | 0.3 mg/kg |
| Administration: | Oral gavage (p.o.) |
| Result: | Increased correct responses and decreased omissions in the poor performing rats. |
| Animal Model: | Fasted monkey[2] |
| Dosage: | 0.06 mg/kg |
| Administration: | Oral gavage (p.o.) |
| Result: | Significantly increased delayed match-to-sample (DMTS) accuracy at a 16-s delay interval. Maintained the beneficial effect 24 h after administration. |
| Animal Model: | submissive behavior model [1] |
| Dosage: | 0.1 mg/kg, 1 mg/kg |
| Administration: | Oral gavage (p.o.) |
| Result: | Led to a significant reduction in dominance levels compared with vehicle treatment starting from the seventh day of treatment and maintained throughout the study period. Had a significant effect in reducing dominance levels at 0.1 and 1 mg/kg. |
IC 50
5-LO
References
[1] Hara H, et al. TAK-653, an AMPA receptor potentiator with minimal agonistic activity, produces an antidepressant-like effect with a favorable safety profile in rats [J]. Pharmacology Biochemistry and Behavior, 2021, 211: 173289. DOI:10.1016/j.pbb.2021.173289
[2] Suzuki A, et al. Strictly regulated agonist-dependent activation of AMPA-R is the key characteristic of TAK-653 for robust synaptic responses and cognitive improvement [J]. Scientific Reports, 2021, 11(1): 14532. DOI:10.1038/s41598-021-93888-0
TAK-653Supplier
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