2. Neuronal Signaling GPCR/G Protein
  3. Sigma Receptor 5-HT Receptor
  4. 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.

At equivalent molar concentrations, both the salt and free forms of a compound exhibit comparable biological activity. Nevertheless, the salt form (OPC-14523 hydrochloride) usually boasts enhanced water solubility and stability.

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OPC-14523 free base Chemical Structure

OPC-14523 free base Chemical Structure

CAS No. : 145969-30-8

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OPC-14523 free base Related Antibodies

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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].

IC50 & Target[1]

sigma 1

47 nM (IC50)

sigma 2

56 nM (IC50)

5-HT1A Receptor

2.3 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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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.
Molecular Weight

413.94

Formula

C23H28ClN3O2
CAS No.
SMILES

O=C1N(CCCN2CCN(C3=CC=CC(Cl)=C3)CC2)C4=C(C(OC)=CC=C4)CC1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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OPC-14523 free base Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

OPC-14523145969-30-8OPC14523OPC 14523Sigma Receptor5-HT ReceptorSerotonin Receptor5-hydroxytryptamine ReceptorantidepressantaffinityreuptakeimmobilityswimmingsubtypeInhibitorinhibitorinhibit

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