| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
|
||
| 10mg |
|
||
| 50mg |
|
||
| Other Sizes |
|
| Targets |
Ki: 50 nM (σ receptor); IC50: 5.5 μM ([3H] DA)[1].
|
|---|---|
| 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].
|
| ln Vivo |
In vivo dopamine release is increased by opiapramol (ip; 5–50 mg/kg)[2].
|
| 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. |
| Toxicity/Toxicokinetics |
Effects During Pregnancy and Lactation
◉ Summary of Use during Lactation Opipramol is not approved for marketing in the United States, but is available overseas. No information is available on the clinical use of opipramol during breastfeeding. Amounts in breastmilk appear to be low and would not be expected to cause any adverse effects in breastfed infants. However, the analytic technique used in the paper would not meet modern standards. ◉ Effects in Breastfed Infants Relevant published information was not found as of the revision date. ◉ Effects on Lactation and Breastmilk Relevant published information was not found as of the revision date. |
| 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]benzazepinyl)propyl]-1-piperazinyl]ethanol is a dibenzoazepine.
Opipramol has been used in trials studying the treatment of Dementia, Depression, Schizophrenia, Anxiety Disorders, and Psychosomatic Disorders. A tricyclic antidepressant with actions similar to AMITRIPTYLINE. |
| Molecular Formula |
C23H29N3O
|
|---|---|
| Molecular Weight |
363.50
|
| Exact Mass |
363.231
|
| CAS # |
315-72-0
|
| Related CAS # |
Opipramol-d4;1215716-70-3
|
| PubChem CID |
9417
|
| Appearance |
Light yellow to yellow solid powder
|
| Density |
1.129 g/cm3
|
| Boiling Point |
555.1ºC at 760 mmHg
|
| Melting Point |
100-101ºC
|
| Flash Point |
290.5ºC
|
| Index of Refraction |
1.6500 (estimate)
|
| LogP |
3.249
|
| Hydrogen Bond Donor Count |
1
|
| Hydrogen Bond Acceptor Count |
4
|
| Rotatable Bond Count |
6
|
| Heavy Atom Count |
27
|
| Complexity |
448
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
OCCN1CCN(CCCN2C3=CC=CC=C3C=CC3=CC=CC=C23)CC1
|
| InChi Key |
YNZFUWZUGRBMHL-UHFFFAOYSA-N
|
| 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
|
| Chemical Name |
2-[4-(3-benzo[b][1]benzazepin-11-ylpropyl)piperazin-1-yl]ethanol
|
| 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 |
| 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: 100 mg/mL (275.10 mM)
|
|---|---|
| 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
