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| | OPC-14523 Basic information |
| Product Name: | OPC-14523 | | Synonyms: | OPC-14523;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-;OPC-14523 free base;VPI 013;VPI013;VPI-013;OPC 14523 free base,OPC14523 free base | | CAS: | 145969-30-8 | | MF: | C23H28ClN3O2 | | MW: | 413.94 | | EINECS: | | | Product Categories: | | | Mol File: | 145969-30-8.mol |  |
| | OPC-14523 Chemical Properties |
| | OPC-14523 Usage And Synthesis |
| 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 |
| | OPC-14523 Preparation Products And Raw materials |
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