OPC-14523 HCl is an orally bioactive sigma and 5-HT1A receptor agonist, targeting sigma receptor (σ1/2 IC50=47/56 nM), 5-HT1A receptor (IC50=2.3 nM) and 5 -HT transporter (IC50=80 nM) has high affinity. OPC-14523 HCl displays antidepressant-like activity.

Physicochemical Properties

Molecular Formula	C23H29CL2N3O2
Molecular Weight	450.40
Exact Mass	449.163
CAS #	145969-31-9
Related CAS #	OPC-14523 free base;145969-30-8
PubChem CID	19027727
Appearance	White to off-white solid powder
Hydrogen Bond Donor Count	1
Hydrogen Bond Acceptor Count	4
Rotatable Bond Count	6
Heavy Atom Count	30
Complexity	540
Defined Atom Stereocenter Count	0
InChi Key	SFOVXVXPFWJNBL-UHFFFAOYSA-N
InChi Code	InChI=1S/C23H28ClN3O2.ClH/c1-29-22-8-3-7-21-20(22)9-10-23(28)27(21)12-4-11-25-13-15-26(16-14-25)19-6-2-5-18(24)17-19;/h2-3,5-8,17H,4,9-16H2,1H3;1H
Chemical Name	1-[3-[4-(3-chlorophenyl)piperazin-1-yl]propyl]-5-methoxy-3,4-dihydroquinolin-2-one;hydrochloride
HS Tariff Code	2934.99.9001
Storage	Powder-20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture.
Shipping Condition	Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

Biological Activity

Targets	5-HT1A Receptor 2.3 nM (IC50) sigma 1 47 nM (IC50) sigma 2 56 mM (IC50)
ln Vitro	OPC-14523 hydrochloride has very little inhibitory action on 3H-NE and 3H-DA reuptake, however it inhibits the in vitro reuptake of 3 H-5-HT (IC50=27 nM)[1].
ln Vivo	In the forced swimming test (FST) with rats and mice, OPC-14523 hydrochloride (0.3-100 mg/kg; po; daily for 0, 2, 4, 7 days) exhibits a pronounced antidepressant-like effect without influencing the overall locomotor activity[1].
Animal Protocol	Animal/Disease Models: Wistar strain of rats (140-245 g)[1] Doses: 0.3-100 mg/kg Route of Administration: Po; daily for 0, 2, 4, 7 days Experimental Results: A single doses of 1 mg /kg and higher of OPC-14523 decreased 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/Disease Models: ICR strain of mice (25- 45 g)[1] Doses: 0.3-100 mg/kg Route of Administration: Po; daily for 0, 2, 4, 7 days Experimental Results: 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 days, producing an ED50 value of 2 mg/kg.
References	[1]. Antidepressant-like responses to the combined sigma and 5-HT1A receptor agonist OPC-14523. Neuropharmacology. 2001;41(8):976-988. [2]. 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 dorsa.

Solubility Data

Solubility (In Vitro)

DMSO: 83.33 mg/mL (185.01 mM) H2O: 5 mg/mL (11.10 mM)

Solubility (In Vivo)

Solubility in Formulation 1: ≥ 2.08 mg/mL (4.62 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (4.62 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Solubility in Formulation 3: ≥ 2.08 mg/mL (4.62 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.  (Please use freshly prepared in vivo formulations for optimal results.)

Preparing Stock Solutions		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

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.