D4R antagonis-2

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D4R antagonis-2

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D4R antagonist-2 是一种有效的选择性D4R拮抗剂，IC₅₀为 6.87 μM。 D4R antagonist-2 显示非常有利的体外 PK 参数并且具有较好的脑渗透性。 D4R antagonist-2 具有帕金森病研究潜力。

生物活性

D4R antagonist-2 is a potent and selectiveD4Rantagonist with anIC₅₀of 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^[1].

IC₅₀& Target

D₄Receptor

6.87 μM (IC₅₀)

体外研究
(In Vitro)

D4R antagonist-2 (compound 11a) shows good activity with an K_iof 299.4 nM^[1].

体内研究
(In Vivo)

D4R antagonist-2 displays very favorable in vitro PK parameters and is brain pentrent (K_p=2.9)^[1]. b>Pharmacokinetic Parameters of D4R antagonist-2 in rats^[1].

rat cassette (0.25 mpk)	11a
CL (ml/min/kg)	22.0
T_1/2(h)	4.4
C₀(ng/ml)	91
V_ss(L/kg)	5.5
AUC (h*ng/mL)	747

Animal Model:	rats^[1]
Dosage:
Administration:	i.v.
Result:	Displayed very favorable in vitro PK parameters and was brain pentrent (K_p=2.9).

分子量

408.87

Formula

C₂₁H₂₃ClF₂N₂O₂

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.