Pagoclone是有活性的(+)-RP59037，为GABA(A) receptor的局部激活剂，常用于恐慌和焦虑等疾病的研究。

Pagoclone is an active (+)-enantiomer of the racemate RP 59037. Pagoclone is a partial GABA(A) receptor agonist used for the treatment of panic and anxiety disorders.

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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. has not independently confirmed the accuracy of these methods. They are for reference only.

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. has not independently confirmed the accuracy of these methods. They are for reference only.

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[1]. Atack JR, et al. The in vivo properties of pagoclone in rat are most likely mediated by 5-hydroxy pagoclone. Neuropharmacology. 2006 May;50(6):677-89.

In Vitro: DMSO : 10 mg/mL (24.52 mM; Need ultrasonic)配制储备液