| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| Other Sizes |
| Targets |
Ki: 50 nM (σ receptor); IC50: 5.5 μM ([3H] DA)[1].
Opipramol targets sigma (σ) receptors as an agonist with a Ki value of 50 nM. It also interacts with histamine, serotonin, dopamine, and alpha-1 adrenergic receptors. As an atypical tricyclic antidepressant, its primary mechanism involves sigma receptor agonism rather than monoamine reuptake inhibition, which distinguishes it from classical TCAs. The compound's sigma receptor activity is believed to contribute to its anxiolytic and antidepressant effects. It is used for research of generalized anxiety disorder. |
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| ln Vitro |
With a Ki value of 50 nM, opipramol can interact with sigma recognition sites potently[1]. With an IC50 value of 5.5 μM, optramoxazole decreases the absorption of [3H] DA in crude synaptosomal preparations[1].
In vitro studies demonstrate that Opipramol acts primarily as a sigma (σ) receptor agonist and potently interacts with sigma recognition sites with a Ki value of 50 nM. The compound also interacts with histamine, serotonin, dopamine and alpha-1 adrenergic receptors. As an atypical tricyclic antidepressant, it has a unique pharmacological profile compared to classical TCAs. The compound's sigma receptor agonism is believed to mediate its anxiolytic and antidepressant effects. It can be used for the research of generalized anxiety disorder (GAD). Additional in vitro characterization may include receptor binding profiles and functional assays. |
| ln Vivo |
In vivo dopamine release is increased by opiapramol (ip; 5–50 mg/kg)[2].
In vivo studies of Opipramol have been conducted in the context of its use as an antidepressant and anxiolytic agent. The compound has been studied in animal models of anxiety and depression. Its sigma receptor agonist activity is believed to contribute to its therapeutic effects. Opipramol has been used clinically in some countries for the treatment of generalized anxiety disorder. Specific in vivo efficacy data in animal models are available in the primary literature. The compound's pharmacokinetic and pharmacodynamic profiles have been characterized in preclinical and clinical studies. It remains a research tool for studying sigma receptor pharmacology. |
| Enzyme Assay |
For sigma receptor binding assays, membrane preparations from rat brain or cells expressing recombinant sigma receptors are incubated with radiolabeled ligands (e.g., [3H]-DTG or [3H]-haloperidol) and varying concentrations of Opipramol. Non-specific binding is determined using excess unlabeled reference compound. Following incubation at 25°C for 60-120 minutes, bound and free radioligands are separated by rapid filtration through glass fiber filters. Filters are washed, dried, and radioactivity counted. Ki values are calculated from competitive binding curves using the Cheng-Prusoff equation. For receptor profiling, similar assays are performed for other targets (histamine, serotonin, dopamine, adrenergic receptors). Assays are performed in triplicate with appropriate vehicle controls.
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| Cell Assay |
For in vitro cellular assays, cells expressing sigma receptors or other relevant targets are cultured in appropriate media under standard conditions (37°C, 5% CO2). Opipramol is dissolved in DMSO and diluted in culture medium to desired concentrations. Cells are treated with compound for specified durations. Sigma receptor activation can be assessed by measuring downstream signaling pathways or cellular responses. For cell viability assays, standard MTT or CCK-8 assays can be used. For receptor functional assays, cAMP accumulation or calcium flux may be measured. Each concentration is tested in replicate wells with vehicle controls and positive controls.
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| Animal Protocol |
Animal/Disease Models: SD (Sprague-Dawley) rats (male, 150-l 80 g)[2]
Doses: 5-50 mg/kg Route of Administration: intraperitoneal (ip) injections Experimental Results: Increased the levels of DOPAC and HVA in the striatum of the rat, without changing the steady-state levels of DA. Potently increased the metabolism of dopamine in the striatum, olfactory tubercle and pyriform cortex of the rat. Increased plasma prolactin in the rat, only at a dose as large as 50 mg/kg dose. For in vivo animal studies, Opipramol is typically formulated in suitable vehicles and administered via oral gavage, intraperitoneal (i.p.) injection, or subcutaneous (s.c.) injection. Dosing regimens vary by study objective. For anxiety models (e.g., elevated plus maze, open field test, light-dark box), animals are treated with compound and behavioral responses are recorded. For depression models (e.g., forced swim test, tail suspension test), similar protocols are used. For pharmacokinetic studies, blood and brain tissue samples are collected at predetermined time points. All procedures must follow institutional animal care and use committee guidelines. |
| ADME/Pharmacokinetics |
Pharmacokinetic properties of Opipramol are characteristic of a tricyclic antidepressant. The compound has a molecular weight of 363.50, formula C23H29N3O, and CAS number 315-72-0. Purity: 99.91%. Storage: powder at -20°C for 3 years; in solvent at -80°C for 1 year. Solubility: soluble in DMSO and other organic solvents. As a sigma receptor agonist with additional receptor interactions, it is expected to have moderate oral bioavailability and tissue distribution. Specific pharmacokinetic parameters are reported in the primary literature.
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| Toxicity/Toxicokinetics |
Effects During Pregnancy and Lactation
◉ Overview of Use During Lactation Opimidazole is not approved for marketing in the United States, but it is available overseas. There is currently no information regarding the clinical use of opipidazol during lactation. The drug concentration in breast milk appears to be very low, and no adverse effects on breastfed infants are expected. However, the analytical techniques used in this article do not meet modern standards. ◉ Effects on Breastfed Infants No relevant published information was found as of the revision date. ◉ Effects on Lactation and Breast Milk No relevant published information was found as of the revision date. According to available safety information, Opipramol is intended for research use only and is a controlled substance. Standard laboratory safety precautions should be followed when handling this compound, including the use of appropriate personal protective equipment (gloves, lab coat, safety goggles). The compound should be handled in a well-ventilated area. Avoid dust formation and inhalation. In case of skin contact, wash with plenty of soap and water. In case of eye contact, rinse cautiously with water for several minutes. Clinical toxicity data may be available from its use as a pharmaceutical in some countries. |
| References |
[1]. H J Möller, et al. Opipramol for the treatment of generalized anxiety disorder: a placebo-controlled trial including an alprazolam-treated group. J Clin Psychopharmacol. 2001 Feb;21(1):59-65.
[2]. T S Rao, et al. Neurochemical characterization of dopaminergic effects of opipramol, a potent sigma receptor ligand, in vivo. Neuropharmacology. 1990 Dec;29(12):1191-7. |
| Additional Infomation |
2-[4-[3-(11-benzo[b][1]benzo[b][1]benzo[b][1]benzo[b][1]]propyl]-1-piperazinyl]ethanol is a dibenzo[b][1]azinyl[b][1]benz[b][1]benzo[b][1]]propyl]-1-piperazinyl[b][1]]ethanol. Opipramoril has been used in clinical trials for the treatment of dementia, depression, schizophrenia, anxiety disorders, and psychosomatic disorders. It is a tricyclic antidepressant with a mechanism of action similar to amitriptyline.
Opipramol (Ensidon; G-33040) is an atypical tricyclic antidepressant that acts primarily as a sigma (σ) receptor agonist with a Ki of 50 nM. It also interacts with histamine, serotonin, dopamine and alpha-1 adrenergic receptors. The compound can be used for research of generalized anxiety disorder (GAD). It has a molecular weight of 363.50 and formula C23H29N3O. It has been used clinically in some countries as an anxiolytic and antidepressant. It is for research use only. |
| Molecular Formula |
C23H29N3O
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|---|---|
| Molecular Weight |
363.50
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| Exact Mass |
363.231
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| CAS # |
315-72-0
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| Related CAS # |
Opipramol-d4;1215716-70-3
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| PubChem CID |
9417
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| Appearance |
Light yellow to yellow solid powder
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| Density |
1.129 g/cm3
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| Boiling Point |
555.1ºC at 760 mmHg
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| Melting Point |
100-101ºC
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| Flash Point |
290.5ºC
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| Index of Refraction |
1.6500 (estimate)
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| LogP |
3.249
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
27
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| Complexity |
448
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| Defined Atom Stereocenter Count |
0
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| SMILES |
OCCN1CCN(CCCN2C3=CC=CC=C3C=CC3=CC=CC=C23)CC1
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| InChi Key |
YNZFUWZUGRBMHL-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C23H29N3O/c27-19-18-25-16-14-24(15-17-25)12-5-13-26-22-8-3-1-6-20(22)10-11-21-7-2-4-9-23(21)26/h1-4,6-11,27H,5,12-19H2
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| Chemical Name |
2-[4-(3-benzo[b][1]benzazepin-11-ylpropyl)piperazin-1-yl]ethanol
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: 100 mg/mL (275.10 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.88 mM) (saturation unknown) in 10% DMSO + 40% PEG300 +5% Tween-80 + 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 25.0 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. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.7510 mL | 13.7552 mL | 27.5103 mL | |
| 5 mM | 0.5502 mL | 2.7510 mL | 5.5021 mL | |
| 10 mM | 0.2751 mL | 1.3755 mL | 2.7510 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.
Link: https://clinicaltrials.gov/ct2/show/NCT03083405
Conditions:Sleep Bruxism|Hypertension|Thyroid Dysfunction|Mental Status Change|Sleep Apnea|Sleep Disorders|Cardiovascular Risk Factor|Cardiovascular Diseases|Temporomandibular DisorderLink: https://clinicaltrials.gov/ct2/show/NCT02374567
Conditions:Dementia|Depression|Schizophrenia|Psychosomatic Disorders|Anxiety DisordersLink: https://clinicaltrials.gov/ct2/show/NCT03065998
Conditions:Drug AbuseProducts are for research use only; We do not sell to patients
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