TAK-653

Research use only, not for human use.

TAK-653, 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.

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.

——

Animal Model:Normal rats 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 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 monkeyDosage: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 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.

——

Membrane Transporter/Ion Channel

iGluR

iGluR

——

——

1358751-06-0

373.47

C19H23N3O3S

>98% (HPLC)

In Vitro:?DMSO : ≥ 12.5 mg/mL (33.47 mM )

CC1=CN2CCS(=O)(=O)N=C2C(=N1)c1ccc(OC2CCCCC2)cc1

——

(-20℃)

With Ice Pack

≥ 2 years