PAOPA, an analog of L-proline-l-leucine-glycine amide (PLG) peptide, is an allosteric modulator ofDopamine 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^[1].

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^[1]。
PAOPA (10 μM; 48 h) 促进 D2/eYFP. 细胞中 D2 受体内化^[1]。

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^[1].

254.29

C₁₁H₁₈N₄O₃

114200-31-6

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