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FAUC-365 is a selective dopamine D3 receptor antagonist with a high affinity (Ki = 0.5 nM) for dopamine D3 receptors, showing significant selectivity over other dopamine receptors (D1, D2L, D2S, and D4) and serotonin receptor subtypes (5-HT1A and 5-HT2). It has been demonstrated to prevent memory impairment in dopamine transporter knockdown (DAT-KD) mice when administered before object learning, making it a potential candidate for therapeutic applications related to memory and cognitive functions.

474432-66-1

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474432-66-1 Usage

Uses

Used in Pharmaceutical Industry:
FAUC-365 is used as a therapeutic agent for targeting dopamine D3 receptors, particularly in the treatment of conditions related to memory impairment and cognitive dysfunction. Its high selectivity for dopamine D3 receptors over other receptors makes it a promising candidate for developing targeted treatments with minimal side effects.
Used in Research and Development:
FAUC-365 serves as a valuable research tool for studying the role of dopamine D3 receptors in various neurological and psychiatric disorders. Its use in preclinical studies can help researchers understand the underlying mechanisms of these conditions and develop more effective treatments.
Used in Drug Design and Optimization:
The selective antagonistic properties of FAUC-365 can be leveraged in the design and optimization of new drugs targeting dopamine D3 receptors. Understanding its binding characteristics and selectivity profile can guide the development of more potent and selective compounds with improved therapeutic potential.
Used in Drug Delivery Systems:
To enhance the bioavailability, delivery, and therapeutic outcomes of FAUC-365, novel drug delivery systems can be developed. These systems may include various organic and metallic nanoparticles or other advanced delivery methods to improve the compound's pharmacokinetics and target engagement, ultimately leading to more effective treatments for related conditions.

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.

Check Digit Verification of cas no

The CAS Registry Mumber 474432-66-1 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 4,7,4,4,3 and 2 respectively; the second part has 2 digits, 6 and 6 respectively.
Calculate Digit Verification of CAS Registry Number 474432-66:
(8*4)+(7*7)+(6*4)+(5*4)+(4*3)+(3*2)+(2*6)+(1*6)=161
161 % 10 = 1
So 474432-66-1 is a valid CAS Registry Number.

474432-66-1Downstream Products

474432-66-1Relevant academic research and scientific papers

Structure-affinity relationship study on N-[4-(4-arylpiperazin-1-yl)butyl]arylcarboxamides as potent and selective dopamine D3 receptor ligands

Leopoldo, Marcello,Berardi, Francesco,Colabufo, Nicola A.,De Giorgio, Paola,Lacivita, Enza,Perrone, Roberto,Tortorella, Vincenzo

, p. 5727 - 5735 (2007/10/03)

The benzamide PB12 (N- [2-[4-(4-chlorophenyl)piperazin-1-yl] ethyl]-3-methoxybenzamide) (1), already reported as potent and selective dopamine D4 receptor ligand, has been modified searching for structural features that could lead to D3/s

Interactive SAR studies: Rational discovery of super-potent and highly selective dopamine D3 receptor antagonists and partial agonists

Bettinetti, Laura,Schlotter, Karin,Hübner, Harald,Gmeiner, Peter

, p. 4594 - 4597 (2007/10/03)

Starting from dopamine receptor ligand BP897, an interactive drug discovery process leading to heterocyclic bioisosteres is demonstrated. The four step strategy involved a careful optimization of geometric and electronic properties by systematic modificat

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