OPC-14523 free base
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.
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- CAS No.: 145969-30-8
- 화학식: C23H28ClN3O2
- 분자량:413.94
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보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- 순도&문서
- References
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Help & FAQs
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Biological Activity
제품 설명
IC50 & Target
[1]|
5-HT1A Receptor |
sigma 1 47 nM (IC50) |
sigma 2 56 nM (IC50) |
5-HT1A Receptor 2.3 nM (IC50) |
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Wistar strain of rats (140-245 g)[1]
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Dosage:0.3-100 mg/kg
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Administration:P.o.; daily for 0, 2, 4, 7 days
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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]
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Dosage:0.3-100 mg/kg
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Administration:P.o.; daily for 0, 2, 4, 7 days
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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.
Chemical Information
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CAS No. 145969-30-8
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분자량 413.94
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화학식 C23H28ClN3O2
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SMILES
O=C1N(CCCN2CCN(C3=CC=CC(Cl)=C3)CC2)C4=C(C(OC)=CC=C4)CC1
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
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. [Content Brief]
[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. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
OPC-14523 free base Related Classifications
HY-116594 Related Classifications
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