| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| 5mg |
|
||
| 10mg |
|
||
| Other Sizes |
| Targets |
5-HT1A Receptor 2.3 nM (IC50) sigma 1 47 nM (IC50) sigma 2 56 mM (IC50)
sigma-1 receptor (σ1), sigma-2 receptor (σ2), 5-HT1A receptor, and serotonin transporter (SERT). OPC-14523 is a multi-target agonist with antidepressant activity mediated through combined sigma and 5-HT1A receptor stimulation. |
|---|---|
| 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].
OPC-14523 shows high affinity for sigma receptors (σ1 IC50 = 47 nM, σ2 IC50 = 56 nM), the 5-HT1A receptor (IC50 = 2.3 nM), and the 5-HT transporter (IC50 = 80 nM). The acute antidepressant-like action is achieved by combined stimulation of sigma and 5-HT1A receptors without inhibition of 5-HT reuptake in vivo. |
| 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].
OPC-14523 exhibits antidepressant-like responses in animal models through combined sigma and 5-HT1A receptor stimulation. The acute antidepressant-like action is achieved by combined stimulation of sigma and 5-HT1A receptors without requiring 5-HT reuptake inhibition in vivo. This dual mechanism may offer advantages over conventional antidepressants. The compound has shown antidepressant activity in preclinical models. |
| Enzyme Assay |
Cell-free receptor binding assays for sigma-1 and sigma-2 receptors: guinea pig brain membranes (sigma-1) or rat liver membranes (sigma-2) are incubated with [3H]-pentazocine (sigma-1) or [3H]-DTG (sigma-2) in the presence of (+)pentazocine for sigma-2 assays, and increasing concentrations of OPC-14523 (0.01-10,000 nM) in 50 mM Tris-HCl, pH 8.0, for 120 min at 25degC. Bound radioactivity is separated by GF/B filtration. IC50 values are calculated: σ1 = 47 nM, σ2 = 56 nM. For 5-HT1A binding, [3H]-8-OH-DPAT is used as radioligand. For SERT binding, [3H]-paroxetine is used.
|
| Cell Assay |
Functional assays: For 5-HT1A receptor agonism, CHO cells expressing human 5-HT1A receptors and a CRE-luciferase reporter are treated with OPC-14523 (0.01-10,000 nM) for 5 hours at 37degC. Luciferase activity is measured to determine EC50. For sigma receptor functional activity, HEK293 cells expressing sigma-1 receptors are used to assess changes in intracellular calcium or cell viability. Antidepressant activity is assessed by measuring stimulation of sigma and 5-HT1A receptors.
|
| 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. In vivo antidepressant efficacy is assessed using the forced swimming test (FST) and tail suspension test (TST) in rodents. OPC-14523 is administered orally or intraperitoneally at doses of 1-30 mg/kg. Immobility time is recorded to determine antidepressant-like effects. The effect of OPC-14523 is compared to standard antidepressants. The compound is also tested for 5-HT reuptake inhibition using the p-chloroamphetamine (PCA)-induced 5-HT depletion model in rat hypothalamus to demonstrate that its antidepressant action is independent of SERT inhibition. |
| ADME/Pharmacokinetics |
No specific PK data are reported for OPC-14523 hydrochloride. As an orally active small molecule, it is expected to have good oral bioavailability and to cross the blood-brain barrier. Molecular weight is approximately 400-500 g/mol. Standard PK parameters (t1/2, Cmax, AUC, F%) have not been published in the available literature. The compound is soluble in DMSO. Recommended storage: -20degC, protect from light.
|
| Toxicity/Toxicokinetics |
No specific toxicity data are reported for OPC-14523 hydrochloride. As a sigma and 5-HT1A receptor agonist with antidepressant activity in preclinical models, standard safety assessments would include hERG channel inhibition (cardiotoxicity), CYP inhibition (DDI potential), and general toxicology in rodents. No serious adverse events have been reported in the literature. No clinical trials have been conducted.
|
| References |
|
| Additional Infomation |
Other information: OPC-14523 hydrochloride is a research compound not approved by the FDA. It is an orally active sigma and 5-HT1A receptor agonist with antidepressant-like activity. The acute antidepressant-like action is achieved by combined stimulation of sigma and 5-HT1A receptors without inhibition of 5-HT reuptake in vivo, distinguishing it from SSRIs. CAS number: 145969-31-9. The compound is for research use only and not for clinical use. Synonyms: OPC-14523 HCl. Purity ≥98%.
|
| 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
|
| SMILES |
COC1=CC=CC2=C1CCC(=O)N2CCCN3CCN(CC3)C4=CC(=CC=C4)Cl.Cl
|
| 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)
|
| 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. View More
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. |
| 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.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
