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FAUC 365 

Cat. No. M30133
FAUC 365  Structure
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Biological Activity

FAUC 365 is a highly dopamine D3 receptor-selective antagonist with Ki values of 0.5 nM, 340, 2600, and 3600 nM at D3, D4.4, D2short, and D2Long receptors, respectively. FAUC 365 can be used for the research of schizophrenia, and Parkinson's disease.

Chemical Information
Molecular Weight 462.44
Formula C23H25Cl2N3OS
CAS Number 474432-66-1
Form Solid
Solubility (25°C) DMSO 33.33 mg/mL (ultrasonic)
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Pi-Kai Chang, et al. Neuropharmacology. Dopamine D3 receptor blockade rescues hyper-dopamine activity-induced deficit in novel object recognition memory

[2] Zhiwei Feng, et al. Comb Chem High Throughput Screen. Structure-based drug design for dopamine D3 receptor

[3] Fabrizio Sanna, et al. Behav Brain Res. Dopamine D2-like receptor agonists induce penile erection in male rats: differential role of D2, D3 and D4 receptors in the paraventricular nucleus of the hypothalamus

[4] Ismail Salama, et al. Bioorg Med Chem. CoMFA and CoMSIA investigations of dopamine D3 receptor ligands leading to the prediction, synthesis, and evaluation of rigidized FAUC 365 analogues

[5] Philip Seeman, et al. Synapse. Dopamine D2 and D3 receptors in human putamen, caudate nucleus, and globus pallidus

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