145969-31-9
145969-31-9 structure
- Name: OPC-14523 hydrochloride
- Chemical Name: 1-{3-[4-(3-Chlorophenyl)-1-piperazinyl]propyl}-5-methoxy-3,4-dihydro-2(1H)-quinolinone hydrochloride (1:1)
- CAS Number: 145969-31-9
- Molecular Formula: C23H29Cl2N3O2
- Molecular Weight: 450.401
- Catalog: Signaling Pathways GPCR/G Protein 5-HT Receptor
- Create Date: 2018-07-02 18:35:39
- Modify Date: 2024-01-30 12:15:56
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OPC-14523 hydrochloride 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 hydrochloride shows antidepressant-like activity[1][2].
| Name | 1-{3-[4-(3-Chlorophenyl)-1-piperazinyl]propyl}-5-methoxy-3,4-dihydro-2(1H)-quinolinone hydrochloride (1:1) |
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| Synonyms |
1-{3-[4-(3-Chlorophenyl)-1-piperazinyl]propyl}-5-methoxy-3,4-dihydro-2(1H)-quinolinone hydrochloride (1:1)
2(1H)-Quinolinone, 1-[3-[4-(3-chlorophenyl)-1-piperazinyl]propyl]-3,4-dihydro-5-methoxy-, hydrochloride (1:1) |
| Description | OPC-14523 hydrochloride 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 hydrochloride shows antidepressant-like activity[1][2]. |
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| Related Catalog | |
| Target |
5-HT1A Receptor:2.3 nM (IC50) sigma 1:47 nM (IC50) sigma 2:56 mM (IC50) |
| 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 3H-NE and 3H-DA reuptake[1]. |
| 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[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. |
| References |
| Molecular Formula | C23H29Cl2N3O2 |
|---|---|
| Molecular Weight | 450.401 |
| Exact Mass | 449.163696 |