145969-30-8

145969-30-8 structure

Name: OPC-14523 free base
Chemical Name: 1-(3-(4-(3-chlorophenyl)-1-piperazinyl)propyl)-5-methoxy-3,4-dihydro-2-quinolinone
CAS Number: 145969-30-8
Molecular Formula: C₂₃H₂₈ClN₃O₂
Molecular Weight: 413.94000
Catalog: Signaling Pathways GPCR/G Protein 5-HT Receptor
Create Date: 2017-07-07 07:32:33
Modify Date: 2024-01-11 12:23:21
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].

Name	1-(3-(4-(3-chlorophenyl)-1-piperazinyl)propyl)-5-methoxy-3,4-dihydro-2-quinolinone
Synonyms	1-[3-[4-(3-chlorophenyl)-1-piperazinyl]propyl]-5-methoxy-3,4-dihydro-2(1H)-quinolone 5-methoxy-1-{3-[4-(3-chlorophenyl)-1-piperazinyl]propyl}-3,4-dihydrocarbostyril

Description	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].
Related Catalog	Research Areas >> Neurological Disease Signaling Pathways >> GPCR/G Protein >> Sigma Receptor Signaling Pathways >> GPCR/G Protein >> 5-HT Receptor Signaling Pathways >> Neuronal Signaling >> 5-HT Receptor
Target	5-HT1A Receptor:2.3 nM (IC50) sigma 1:47 nM (IC50) sigma 2:56 nM (IC50)
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.
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. [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 dorsal raphe nucleus. J Pharmacol Exp Ther. 2004;310(2):578-583.

Molecular Formula	C₂₃H₂₈ClN₃O₂
Molecular Weight	413.94000
Exact Mass	413.18700
PSA	36.02000
LogP	3.90800

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