Identification | Back Directory | [Name]
FAUC-365 | [CAS]
474432-66-1 | [Synonyms]
FAUC-365 3-dichloro- FAUC-365 Benzo[b]thiophene-2-carboxylic acid {4-[4-(2 FAUC-365 Benzo[b]thiophene-2-carboxylic acid {4-[4-(2,3-dichloro-
phenyl)-piperazin-1-yl]-butyl}-amide | [Molecular Formula]
C23H25Cl2N3OS | [MDL Number]
MFCD28160534 | [MOL File]
474432-66-1.mol | [Molecular Weight]
462.435 |
Chemical Properties | Back Directory | [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 |
Hazard Information | Back Directory | [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]. | [storage]
Store at -20°C | [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. |
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