OPC-14523 CAS#: 145969-30-8

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Uses

OPC-14523 free base is an orally active sigma and 5-HT1A receptor agonist, with high affinity for sigma receptors (σ1/2 IC50=47/56 nM), the 5-HT1A receptor (IC50=2.3 nM), and the 5-HT transporter (IC50=80 nM). OPC-14523 free base shows antidepressant-like activity[1][2].

in vivo

OPC-14523 free base (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^[1].

Animal Model:	Wistar strain of rats (140-245 g)^[1]
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 ED₅₀ value of 27 mg/kg. The ED₅₀ value for OPC-14523 on day 7 was 18 mg/kg.

Animal Model:	ICR strain of mice (25-45 g)^[1]
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 ED₅₀ 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.

IC 50

sigma 1: 47 nM (IC₅₀); sigma 2: 56 nM (IC₅₀); 5-HT_1A Receptor: 2.3 nM (IC₅₀)

References

[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. DOI:10.1016/s0028-3908(01)00147-2
[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 DOI:10.1124/jpet.104.066472

OPC-14523

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