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FAUC-365

Catalog No.
C4494
D3 dopamine receptor agonist
Grouped product items
SizePriceStock Qty
5mg
$182.00
In stock
10mg
$292.00
In stock

Tel: +1-832-696-8203

Email: [email protected]

Worldwide Distributors

Background

FAUC-365 is a D3 dopamine receptor agonist.

The dopamine D3 receptor, first identified in 1990, is preferentially expressed in the nucleus accumbens, where dopamine is released by neurons originating from the ventral tegmental area. Convincing pharmacological studies implicate D3-mediated neurotransmission in the reinforcing effects of cocaine. It is therefore a target for drugs which treat drug addiction, schizophrenia, as well as Parkinson's disease.

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].

In vivo: Up to now, there is no animal in vivo data reported for FAUC-365.

Clinical trial: So far, no clinical study has been conducted.

Reference:
[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.

Chemical Properties

StorageStore at -20°C
M.Wt462.4
Cas No.474432-66-1
FormulaC23H25CI2N3OS
Solubilityinsoluble in EtOH; insoluble in H2O; ≥5.79 mg/mL in DMSO
Chemical NameN-[4-[4-(2,3-dichlorophenyl)-1-piperazinyl]butyl]-benzo[b]thiophene-2-carboxamide
SDFDownload SDF
Canonical SMILESClC1=C(Cl)C(N2CCN(CCCCNC(C3=CC4=C(C=CC=C4)S3)=O)CC2)=CC=C1
Shipping ConditionShip with blue ice, or upon other requests.
General tipsFor obtaining a higher solubility, please warm the tube at 37°C and shake it in the ultrasonic bath for a while. We do not recommend long-term storage for the solution, please use it up soon.

Quality Control

Chemical structure

FAUC-365