1. GPCR/G Protein Neuronal Signaling
  2. Dopamine Receptor
  3. PAOPA

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.

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PAOPA Chemical Structure

PAOPA Chemical Structure

CAS No. : 114200-31-6

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Description

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[1].

IC50 & Target[1]

D2 Receptor

 

In Vitro

PAOPA (10 μM; 1.5 h) increases the expression of GRK2 striatum, arrestin-3, phosphorylated ERK1 and ERK2 in D2/eYFP. Cells[1].
PAOPA (10 μM; 48 h) promotes the internalization of D2 receptors in D2/eYFP. Cells[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

PAOPA (1 mg/kg; 腹腔注射; 每天 1 次, 共 45 天) 慢性给药,引起小鼠体内 D2 受体调节和下游分子 (包括 GRK2、arrestin-3 和细胞外受体激酶 ERK 1/2) 的表达增加[1]

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

254.29

Formula

C11H18N4O3

CAS No.
SMILES

O=C([C@@H]1CCCN1)N[C@H]2C(N(CC2)CC(N)=O)=O

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    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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PAOPA
Cat. No.:
HY-103423
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