| Identification | Back Directory | [Name]
OPC-14523 | [CAS]
145969-30-8 | [Synonyms]
OPC-14523
OPC-14523 free base
1-(3-(4-(3-chlorophenyl)-1-piperazinyl)propyl)-5-methoxy-3,4-dihydro-2-quinolinone
2(1H)-Quinolinone, 1-[3-[4-(3-chlorophenyl)-1-piperazinyl]propyl]-3,4-dihydro-5-methoxy- | [Molecular Formula]
C23H28ClN3O2 | [MDL Number]
MFCD00915596 | [MOL File]
145969-30-8.mol | [Molecular Weight]
413.94 |
| Hazard Information | Back Directory | [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.
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| 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.
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| [IC 50]
sigma 1: 47 nM (IC50); sigma 2: 56 nM (IC50); 5-HT1A 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 |
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