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| | FAUC-365 Basic information |
| Product Name: | FAUC-365 | | Synonyms: | FAUC-365;FAUC-365 Benzo[b]thiophene-2-carboxylic acid {4-[4-(2,3-dichloro-
phenyl)-piperazin-1-yl]-butyl}-amide;3-dichloro-;FAUC-365 Benzo[b]thiophene-2-carboxylic acid {4-[4-(2;inhibit,Parkinson's disease,Dopamine Receptor,D3 receptor,FAUC365,Dopamine,Inhibitor,FAUC-365,schizophrenia,SPET,Radioligand,FAUC 365;Benzo[b]thiophene-2-carboxamide, N-[4-[4-(2,3-dichlorophenyl)-1-piperazinyl]butyl]- | | CAS: | 474432-66-1 | | MF: | C23H25Cl2N3OS | | MW: | 462.4351 | | EINECS: | | | Product Categories: | | | Mol File: | 474432-66-1.mol |  |
| | FAUC-365 Chemical Properties |
| Boiling point | 680.3±55.0 °C(Predicted) | | density | 1.300±0.06 g/cm3(Predicted) | | storage temp. | Store at -20°C | | solubility | insoluble in EtOH; insoluble in H2O; ≥5.79 mg/mL in DMSO | | form | A crystalline solid | | pka | 14.55±0.46(Predicted) | | color | Off-white to light yellow |
| | FAUC-365 Usage And Synthesis |
| Description | FAUC-365 is a dopamine D3 receptor antagonist (Ki = 0.5 nM). It is selective for dopamine D3 receptors over dopamine D1, D2L, D2S, and D4 receptors (Kis = 8.8, 3.6, 2.6, and 0.34 μM, respectively) as well as the serotonin (5-HT) receptor subtypes 5-HT1A and 5-HT2 (Kis = 0.36 and 2 μM, respectively). FAUC-365 (1-10 mg/kg) prevents memory impairment in the novel object recognition test in dopamine transporter knockdown (DAT-KD) mice when administered prior to object learning. | | in vitro | fauc-365 was discovered by a rational and interactive sar sequence. as a dichloro derivative, fauc-365 revealed d3 affinities that were comparable to its methoxy-substituted analogues, however, the selectivities of fauc-365 against 5ht-1a, 5-ht2, and r1 were substantially higher, which was demonstrated by that extraordinary selectivity ratios of 17600, 7200, 5200, and 680 over d1, d2long, d2short, and d4, respectively, were determined for fauc-365 with ki of 0.50 nm. in addition, the benzothiophene analog fauc 346 and its oxa analogue showed partial agonist character with ec50 values at 0.36 and 1.5 nm, respectively [1]. | | references | [1] bettinetti l, schlotter k, hübner h, gmeiner p. interactive sar studies: rational discovery of super-potent and highly selective dopamine d3 receptor antagonists and partial agonists. j med chem. 2002 oct 10;45(21):4594-7. |
| | FAUC-365 Preparation Products And Raw materials |
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