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ChemicalBook--->CAS DataBase List--->474432-66-1

474432-66-1

474432-66-1 Structure

474432-66-1 Structure
IdentificationBack 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 PropertiesBack 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 InformationBack 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.
Spectrum DetailBack Directory
[Spectrum Detail]

FAUC-365(474432-66-1)1HNMR
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