Nomifensine Maleate, the maleate salt of nomifensine, is a novel, potent and selective dopamine uptake inhibitor interacting with the dopamine transporter at a site different from that of cocaine; antidepressan.
Physicochemical Properties
| Molecular Formula | C20H22N2O4 |
| Molecular Weight | 354.39968 |
| Exact Mass | 354.158 |
| Elemental Analysis | C, 67.78; H, 6.26; N, 7.90; O, 18.06 |
| CAS # | 32795-47-4 |
| Related CAS # | Nomifensine; 24526-64-5 |
| PubChem CID | 5358907 |
| Appearance | Solid powder |
| Density | 1.114g/cm3 |
| Boiling Point | 378.4ºC at 760mmHg |
| Melting Point | 179-181ºC |
| Flash Point | 164ºC |
| Index of Refraction | 1.581 |
| LogP | 3.077 |
| Hydrogen Bond Donor Count | 3 |
| Hydrogen Bond Acceptor Count | 6 |
| Rotatable Bond Count | 3 |
| Heavy Atom Count | 26 |
| Complexity | 391 |
| Defined Atom Stereocenter Count | 0 |
| SMILES | NC1=CC=CC2=C1CN(C)CC2C3=CC=CC=C3.O=C(O)/C=C\C(O)=O |
| InChi Key | GEOCVSMCLVIOEV-BTJKTKAUSA-N |
| InChi Code | InChI=1S/C16H18N2.C4H4O4/c1-18-10-14(12-6-3-2-4-7-12)13-8-5-9-16(17)15(13)11-18;5-3(6)1-2-4(7)8/h2-9,14H,10-11,17H2,1H3;1-2H,(H,5,6)(H,7,8)/b;2-1- |
| Chemical Name | (Z)-but-2-enedioic acid;2-methyl-4-phenyl-3,4-dihydro-1H-isoquinolin-8-amine |
| Synonyms | Nomifensine Maleate |
| 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) |
Biological Activity
| References |
[1]. Exp Anim . 2018 May 10;67(2):147-153. |
| Additional Infomation |
An isoquinoline derivative that prevents dopamine reuptake into synaptosomes. The maleate was formerly used in the treatment of depression. It was withdrawn worldwide in 1986 due to the risk of acute hemolytic anemia with intravascular hemolysis resulting from its use. In some cases, renal failure also developed. (From Martindale, The Extra Pharmacopoeia, 30th ed, p266) See also: Nomifensine (annotation moved to). |
Solubility Data
| Solubility (In Vitro) |
DMSO: ≥ 80 mg/mL (~225.7 mM) H2O: ~2.2 mg/mL (~6.2 mM) |
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.75 mg/mL (7.76 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 27.5 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: ≥ 2.75 mg/mL (7.76 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 27.5 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: ≥ 2.75 mg/mL (7.76 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 27.5 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 | 2.8217 mL | 14.1084 mL | 28.2167 mL | |
| 5 mM | 0.5643 mL | 2.8217 mL | 5.6433 mL | |
| 10 mM | 0.2822 mL | 1.4108 mL | 2.8217 mL |