OPC-14523 hydrochloride is an orally active sigma and 5-HT1A receptor agonist, with high affinity for sigma receptors (σ1/2 IC 50 =47/56 nM), the 5-HT1A receptor (IC 50 =2.3 nM), and the 5-HT transporter (IC 50 =80 nM). OPC-14523 hydrochloride shows antidepressant-like activity.
性状
Solid
IC50 & Target[1][2]
5-HT1A Receptor 2.3 nM (IC50) sigma 1
体外研究(In Vitro)
OPC-14523 hydrochloride inhibits the in vitro reuptake of 3 H-5-HT (IC50=27 nM), but it shows very weak inhibitory activity on H-NE and H-DA reuptake. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
OPC-14523 hydrochloride (0.3-100 mg/kg; p.o.; daily for 0, 2, 4, 7 days) produces a marked antidepressant-like effect in the forced swimming test (FST) with rats and mice without affecting the general locomotor activity. has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Mod
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
参考文献
[1]. Tottori K, et al. Antidepressant-like responses to the combined sigma and 5-HT1A receptor agonist OPC-14523. Neuropharmacology. 2001;41(8):976-988.[2]. Bermack JE, et al. Effects of the potential antidepressant OPC-14523 [1-[3-[4-(3-chlorophenyl)-1-piperazinyl]propyl]-5-methoxy-3,4-dihydro-2-quinolinone monomethanesulfonate] a combined sigma and 5-HT1A ligand: modulation of neuronal activity in the dorsa
溶解度数据
In Vitro: DMSO : 83.33 mg/mL (185.01 mM; Need ultrasonic)H2O : 5 mg/mL (11.10 mM; ultrasonic and warming and heat to 60°C)配制储备液