FAUC-365 (FAUC365) is a novel, potent and selective dopamine D3 receptor antagonist with the potential to be used for the treatment of schizophrenia, and Parkinson's disease. It has a Ki of 0.5 nM for the dopamine D3 receptor. It is specific to dopamine D3 receptors and not for serotonin (5-HT) receptor subtypes 5-HT1A and 5-HT2 (Kis = 0.36 and 2 µM, respectively), nor for dopamine D1, D2L, D2S, and D4 receptors (Kis = 8.8, 3.6, 2.6, and 0.34 µM, respectively). When given before object learning, FAUC-365 (1–10 mg/kg) protects memory impairment in dopamine transporter knockdown (DAT-KD) mice during the novel object recognition test.
Physicochemical Properties
| Molecular Formula | C23H25CL2N3OS |
| Molecular Weight | 462.43510222435 |
| Exact Mass | 461.109 |
| Elemental Analysis | C, 59.74; H, 5.45; Cl, 15.33; N, 9.09; O, 3.46; S, 6.93 |
| CAS # | 474432-66-1 |
| PubChem CID | 10276451 |
| Appearance | Solid powder |
| Density | 1.3±0.1 g/cm3 |
| Boiling Point | 680.3±55.0 °C at 760 mmHg |
| Flash Point | 365.2±31.5 °C |
| Vapour Pressure | 0.0±2.1 mmHg at 25°C |
| Index of Refraction | 1.638 |
| LogP | 7.14 |
| Hydrogen Bond Donor Count | 1 |
| Hydrogen Bond Acceptor Count | 4 |
| Rotatable Bond Count | 7 |
| Heavy Atom Count | 30 |
| Complexity | 561 |
| Defined Atom Stereocenter Count | 0 |
| SMILES | ClC1C(=CC=CC=1N1CCN(CCCCNC(C2=CC3C=CC=CC=3S2)=O)CC1)Cl |
| InChi Key | CPTSTFKVXWZGEV-UHFFFAOYSA-N |
| InChi Code | InChI=1S/C23H25Cl2N3OS/c24-18-7-5-8-19(22(18)25)28-14-12-27(13-15-28)11-4-3-10-26-23(29)21-16-17-6-1-2-9-20(17)30-21/h1-2,5-9,16H,3-4,10-15H2,(H,26,29) |
| Chemical Name | N-[4-[4-(2,3-dichlorophenyl)piperazin-1-yl]butyl]-1-benzothiophene-2-carboxamide |
| Synonyms | FAUC365; FAUC 365; FAUC-365 |
| HS Tariff Code | 2934.99.03.00 |
| 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
| References |
[1]. Dopamine D2 and D3 receptors in human putamen, caudate nucleus, and globus pallidus. Synapse. 2006 Sep 1;60(3):205-11. [2]. Synthesis and radioiodination of selective ligands for the dopamine D3 receptor subtype. Bioorg Med Chem Lett. 2004 Aug 2;14(15):3963-6. |
Solubility Data
| Solubility (In Vitro) | DMSO: ~33.3 mg/mL (~72.1 mM) |
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.41 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 (5.41 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 | 2.1624 mL | 10.8122 mL | 21.6244 mL | |
| 5 mM | 0.4325 mL | 2.1624 mL | 4.3249 mL | |
| 10 mM | 0.2162 mL | 1.0812 mL | 2.1624 mL |