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编 号:F756328
分子式:C21H23ClF2N2O2
分子量:408.87
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生物活性:
D4R antagonist-2 is a potent and selective D4R antagonist with an IC50 of 6.52 μM. D4R antagonist-2 displays very favorable in vitro PK parameters and has good brain penetration. D4R antagonist-2 has the potential for the research of Parkinson’s disease.

体内研究:
D4R antagonist-2 displays very favorable in vitro PK parameters and is brain pentrent (Kp=2.9).b>Pharmacokinetic Parameters of D4R antagonist-2 in rats.rat cassette (0.25 mpk) 11a
CL (ml/min/kg)22.0
T1/2 (h)4.4
C0 (ng/ml)91
Vss (L/kg)5.5
AUC (h*ng/mL)747
Animal Model:rats
Dosage:
Administration:i.v.
Result:Displayed very favorable in vitro PK parameters and was brain pentrent (Kp=2.9).

体外研究:
D4R antagonist-2 (compound 11a) shows good activity with an Ki of 299.4 nM.
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