Mirtazapine D3 (6-Azamianserin D3; Org-3770 D3) is the tri-deuterated form of Mirtazapine (Remeron), which is is an orally bioactive atypical antidepressant acting as a 5-HT2/3 receptor inhibitor as well as an noradrenergic and specific serotonergic antidepressant (NaSSA) agent.
Physicochemical Properties
| Molecular Formula | C₁₇H₁₆D₃N₃ |
| Molecular Weight | 268.37 |
| Exact Mass | 268.177 |
| CAS # | 1216678-68-0 |
| Related CAS # | Mirtazapine;85650-52-8;(S)-Mirtazapine;61337-87-9;(S)-Mirtazapine-d3;(R)-Mirtazapine;61364-37-2;(R)-Mirtazapine-d3 |
| PubChem CID | 45039945 |
| Appearance | White to off-white solid powder |
| LogP | 2.481 |
| Hydrogen Bond Donor Count | 0 |
| Hydrogen Bond Acceptor Count | 3 |
| Rotatable Bond Count | 0 |
| Heavy Atom Count | 20 |
| Complexity | 345 |
| Defined Atom Stereocenter Count | 0 |
| SMILES | [2H]C([2H])([2H])N1CCN2C(C1)C3=CC=CC=C3CC4=C2N=CC=C4 |
| InChi Key | RONZAEMNMFQXRA-FIBGUPNXSA-N |
| InChi Code | InChI=1S/C17H19N3/c1-19-9-10-20-16(12-19)15-7-3-2-5-13(15)11-14-6-4-8-18-17(14)20/h2-8,16H,9-12H2,1H3/i1D3 |
| Chemical Name | 5-(trideuteriomethyl)-2,5,19-triazatetracyclo[13.4.0.02,7.08,13]nonadeca-1(15),8,10,12,16,18-hexaene |
| Synonyms | Org 3770 D3 Org3770 D3 Mirtazapine D3 6-Azamianserin D3Org-3770 D3 |
| 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) |
Biological Activity
| ln Vivo | The phenotypic scores of MeCP2-null mice were improved by mirtazapine (ip; 10–50 mg/Kg; 14 days) treatment, which also normalized heart rate, respiratory rate, anxiety levels, and eliminated the jumping behavior [ 2]. |
| Animal Protocol |
Animal/Disease Models: MeCP2-deficient mice [2] Doses: 10-50 mg/Kg Route of Administration: intraperitoneal (ip) injection; 10-50 mg/kg; 14 days Experimental Results: The thickness of the somatosensory cortex of MeCP2-deficient mice was restored, especially II -Layer III and VI. |
| References |
[1]. Anttila, S.A. and E.V. Leinonen, A review of the pharmacological and clinical profile of mirtazapine. CNS Drug Rev, 2001. 7(3): p. 249-64. [2]. Interaction between enantiomers of mianserin and ORG3770 at 5-HT3 receptors in cultured mouse neuroblastoma cells.Neuropharmacology. 1994 Mar-Apr;33(3-4):501-7. |
Solubility Data
| Solubility (In Vitro) | DMSO : ~100 mg/mL (~372.62 mM) |
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (9.32 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 (9.32 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 (9.32 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 | 3.7262 mL | 18.6310 mL | 37.2620 mL | |
| 5 mM | 0.7452 mL | 3.7262 mL | 7.4524 mL | |
| 10 mM | 0.3726 mL | 1.8631 mL | 3.7262 mL |