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FAUC-365
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
FAUC-365图片
CAS NO:474432-66-1
包装与价格:
包装价格(元)
1mg电议
5mg电议
10mg电议

产品介绍
Cas No.474432-66-1
化学名N-[4-[4-(2,3-dichlorophenyl)-1-piperazinyl]butyl]-benzo[b]thiophene-2-carboxamide
Canonical SMILESClC1=C(Cl)C(N2CCN(CCCCNC(C3=CC4=C(C=CC=C4)S3)=O)CC2)=CC=C1
分子式C23H25CI2N3OS
分子量462.4
溶解度DMF: 30 mg/ml,DMSO: 30 mg/ml,DMSO:PBS (pH 7.2) (1:2): 0.25 mg/ml,Ethanol: 2 mg/ml
储存条件Store at -20℃
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

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.