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Mianserin HCl (formerly ORG GB-94; ORG-GB 94; Depnon, Lantanon, Lerivon, Lumin, Norval, Tolvon), the hydrochloride salt of mianserin which is a psychoactive tetracyclic compound, is a novel and potent antagonist (inverse agonist) of H1 histamine receptor and 5-HT serotonin receptors used for the treatment of depression. Hematological issues as well as sleepiness could result from it. Though its exact mode of action is unknown, it appears to block certain types of serotonin, histamine H1, and alpha-adrenergic receptors.
Physicochemical Properties
| Molecular Formula | C18H21CLN2 | |
| Molecular Weight | 300.83 | |
| Exact Mass | 300.139 | |
| Elemental Analysis | C, 71.87; H, 7.04; Cl, 11.78; N, 9.31 | |
| CAS # | 21535-47-7 | |
| Related CAS # | Mianserin; 24219-97-4; Mianserin-d3 hydrochloride; 1219804-97-3; 51152-88-6 ((S)-isomer) | |
| PubChem CID | 68551 | |
| Appearance | White to light yellow solid powder | |
| Density | 1.18 g/cm3 | |
| Boiling Point | 411.3ºC at 760 mmHg | |
| Melting Point | >230ºC (dec.) | |
| Flash Point | 186.1ºC | |
| Vapour Pressure | 5.65E-07mmHg at 25°C | |
| LogP | 3.888 | |
| Hydrogen Bond Donor Count | 1 | |
| Hydrogen Bond Acceptor Count | 2 | |
| Rotatable Bond Count | 0 | |
| Heavy Atom Count | 21 | |
| Complexity | 342 | |
| Defined Atom Stereocenter Count | 0 | |
| SMILES | CN(CC1)CC2N1C3=CC=CC=C3CC4=CC=CC=C24.Cl |
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| InChi Key | YNPFMWCWRVTGKJ-UHFFFAOYSA-N | |
| InChi Code | InChI=1S/C18H20N2.ClH/c1-19-10-11-20-17-9-5-3-7-15(17)12-14-6-2-4-8-16(14)18(20)13-19;/h2-9,18H,10-13H2,1H3;1H | |
| Chemical Name | 5-methyl-2,5-diazatetracyclo[13.4.0.02,7.08,13]nonadeca-1(19),8,10,12,15,17-hexaene;hydrochloride | |
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| 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. |
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| 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 | H1 Receptor | ||
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| References |
[1]. J Pharmacol Exp Ther . 1996 May;277(2):852-60. [2]. Eur J Pharmacol . 1994 Sep 1;262(1-2):125-31. [3]. Neuroreport . 1991 Sep;2(9):525-8. [4]. Psychopharmacology (Berl) . 1995 Jun;119(4):466-73. [5]. Psychopharmacology (Berl) . 1996 Jan;123(2):127-30. |
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| Additional Infomation |
A tetracyclic compound with antidepressant effects. It may cause drowsiness and hematological problems. Its mechanism of therapeutic action is not well understood, although it apparently blocks alpha-adrenergic, histamine H1, and some types of serotonin receptors. See also: Mianserin (annotation moved to). |
Solubility Data
| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (8.31 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 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. Solubility in Formulation 2: ≥ 2.5 mg/mL (8.31 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 25.0 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: ≥ 2.5 mg/mL (8.31 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 25.0 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 | 3.3241 mL | 16.6207 mL | 33.2414 mL | |
| 5 mM | 0.6648 mL | 3.3241 mL | 6.6483 mL | |
| 10 mM | 0.3324 mL | 1.6621 mL | 3.3241 mL |