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编 号:F044528
分子式:C11H18N4O3
分子量:254.29
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生物活性:
PAOPA, an analog of L-proline-l-leucine-glycine amide (PLG) peptide, is an allosteric modulator of Dopamine D2 Receptor. PAOPA can effectively reduce behavioral abnormalities in rodent models of schizophrenia. PAOPA increases the high affinity dopamine D2 receptor and promotes its binding to agonists.

体内研究:
PAOPA (1 mg/kg; i.p.; once daily for 45 d) in chronic administration induces increased expression of D2 receptor regulation and downstream molecules (including GRK2, arrestin-3, and extracellular receptor kinase ERK 1/2) in mice.

体外研究:
PAOPA (10 μM; 1.5 h) 增加 D2/eYFP. 细胞中 GRK2 的纹状体、arrestin-3、磷酸化 ERK1 和 ERK2 的表达。PAOPA (10 μM; 48 h) 促进 D2/eYFP. 细胞中 D2 受体内化。
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