Pagoclone

Research use only, not for human use.

A potent, orally active GABAA receptor agonist with high affinity (0.7-9.1nM) to the benzodiazepine binding site of GABAA receptors containing either an α1, α2, α3 or α5 subunit.

A potent, orally active GABAA receptor agonist with high affinity (0.7-9.1nM) to the benzodiazepine binding site of GABAA receptors containing either an α1, α2, α3 or α5 subunit; exhibits significant anxiolytic-like activity in vivo.Anxiety Phase 3 Discontinued.

Pagoclone has high and approximately equivalent affinity (Ki values=0.7-9.1 nM) for recombinant human GABAA receptors containing either an α1, α2, α3 or α5 subunit. Pagoclone has significant agonist activity at all four diazepam-sensitive GABAA receptor subtypes, with EC50 of 3.1-6.6 nM.

Pagoclone (3 mg/kg, p.o.) has significant anxiolytic-like activity, but at all three doses tested (0.3, 1 and 3 mg/kg p.o.) it produces a significant reduction in the total distance travelled. Pagoclone (3 mg/kg, p.o.) produces a dose-dependent increase in time spent on the open arms compared to control. Pagoclone (1, 3 or 10 mg/kg) lowers the cumulative chain-pulling response in the response sensitivity test. Plasma pagoclone concentrations are dose-dependent but not linear, with plasma concentrations of pagoclone being 0.4±0.1, 1.1±0.2 and 2.2±0.2 ng/mL, respectively. Pagoclone (0.3, 1 or 3 mg/kg) reduces locomotor activity in rats in a dose dependent manner.

+)-RP-59037 | IP-456 | RP-62955 | CI-1043

Membrane Transporter/Ion Channel

GAT

GAT

Neurological Disease

Anxiety

133737-32-3

407.89268

C23H22ClN3O2

>98% (HPLC)

10 mM in DMSO

O=C1N(C2=NC3=NC(Cl)=CC=C3C=C2)C(CC(CCC(C)C)=O)C4=C1C=CC=C4

1H-Isoindol-1-one, 2-(7-chloro-1,8-naphthyridin-2-yl)-2,3-dihydro-3-(5-methyl-2-oxohexyl)-, (+)-

(-20℃)

With Ice Pack

≥ 2 years