1. GPCR/G Protein
    Neuronal Signaling
  2. Sigma Receptor
    5-HT Receptor
  3. OPC-14523 hydrochloride

OPC-14523 hydrochloride 

Cat. No.: HY-116594A Purity: 99.90%
Handling Instructions

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.

For research use only. We do not sell to patients.

OPC-14523 hydrochloride Chemical Structure

OPC-14523 hydrochloride Chemical Structure

CAS No. : 145969-31-9

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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].

IC50 & Target[1]

sigma 1

47 nM (IC50)

sigma 2

56 mM (IC50)

5-HT1A Receptor

2.3 nM (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.
Molecular Weight

450.40

Formula

C₂₃H₂₉Cl₂N₃O₂

CAS No.

145969-31-9

SMILES

O=C1N(CCCN2CCN(C3=CC=CC(Cl)=C3)CC2)C4=C(C(OC)=CC=C4)CC1.[H]Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 83.33 mg/mL (185.01 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.2202 mL 11.1012 mL 22.2025 mL
5 mM 0.4440 mL 2.2202 mL 4.4405 mL
10 mM 0.2220 mL 1.1101 mL 2.2202 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (4.62 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (4.62 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (4.62 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Keywords:

OPC-14523OPC14523OPC 14523Sigma Receptor5-HT ReceptorSerotonin Receptor5-hydroxytryptamine ReceptorantidepressantaffinityreuptakeimmobilityswimmingsubtypeoralInhibitorinhibitorinhibit

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OPC-14523 hydrochloride
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HY-116594A
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