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 ant
Storage Temp
Store at 2-8°C,Desiccated
Shipped In
Wet ice
This product requires cold chain shipping. Ground and other economy services are not available.
Product Description
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
In Vitro
OPC-14523 hydrochloride inhibits the in vitro reuptake of 3 H-5-HT (IC 50 =27 nM), but it shows very weak inhibitory activity on 3 H-NE and 3 H-DA reuptake. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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 . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Wistar strain of rats (140-245 g) Dosage: 0.3-100 mg/kg Administration: P.o.; daily for 0, 2, 4, 7 days Result: A single doses of 1 mg/kg and higher of OPC-14523 reduced immobility time in the FST with an ED 50 value of 27 mg/kg. The ED 50 value for OPC-14523 on day 7 was 18 mg/kg. Animal Model: ICR strain of mice (25-45 g) Dosage: 0.3-100 mg/kg Administration: P.o.; daily for 0, 2, 4, 7 days Result: A single oral dose of OPC-14523 produced a marked reduction in immobility time during the FST at oral doses of 1 mg/kg and higher, with an ED 50 value of 20 mg/kg. The potency of OPC-14523 in decreasing immobility time was greater after treatment for seven consecutive days, producing an ED50 value of 2 mg/kg.
This compound belongs to the class of organic compounds known as phenylpiperazines. These are compounds containing a phenylpiperazine skeleton, which consists of a piperazine bound to a phenyl group.
External Descriptors
Not available
1. Djoumbou Feunang Y, Eisner R, Knox C, Chepelev L, Hastings J, Owen G, Fahy E, Steinbeck C, Subramanian S, Bolton E, Greiner R, and Wishart DS. ClassyFire: Automated Chemical Classification With A Comprehensive, Computable Taxonomy. Journal of Cheminformatics, 2016, 8:61.
