1. GPCR/G Protein
    Neuronal Signaling
  2. Melatonin Receptor
  3. 4-P-PDOT

4-P-PDOT 

Cat. No.: HY-100609 Purity: >99.0%
Handling Instructions

4-P-PDOT is a potent, selective and affinity Melatonin receptor (MT2) antagonist. 4-P-PDOT is >300-fold more selective for MT2 than MT1. 4-P-PDOT significantly counteracts Melatonin-mediated antioxidant effects (GSH/GSSG ratio, phospho-ERK, Nrf2 nuclear translocation, Nrf2 DNA-binding activity).

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4-P-PDOT Chemical Structure

4-P-PDOT Chemical Structure

CAS No. : 134865-74-0

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10 mM * 1 mL in DMSO USD 154 Get quote
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Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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Description

4-P-PDOT is a potent, selective and affinity Melatonin receptor (MT2) antagonist. 4-P-PDOT is >300-fold more selective for MT2 than MT1. 4-P-PDOT significantly counteracts Melatonin-mediated antioxidant effects (GSH/GSSG ratio, phospho-ERK, Nrf2 nuclear translocation, Nrf2 DNA-binding activity)[1][2][3][4].

IC50 & Target

MT2 receptor[1]

In Vitro

In CHO-mt1 cells the amidotetraline 4-P-PDOT (10 mM) has no e€ect on forskolin-stimulated cyclic AMP levels, either alone, or in the presence of Melatonin. In contrast, in CHO-MT2 cells, 4-P-PDOT is an agonist, producing a concentration-dependent inhibition of forskolin stimulated cyclic AMP, with a pEC50 value of 8.72 and intrinsic activity of 0.86[1].

In Vivo

4-P-PDOT (0.5-1.0 mg/kg; intravenous injection; klotho mutant mice) treatment significantly reverses antioxidant effects mediated by Melatonin. And significantly reverses the changes in the levels of these GSH-related parameters. 4-P-PDOT treatment significantly reverses the memory function of Melatonin-treated klotho mutant mice. 4-P-PDOT also counteracts Melatonin-mediated attenuation in response to the decreases in phospho-ERK expression, Nrf2 nuclear translocation, Nrf2 DNA-binding activity, and GCL mRNA expression in the hippocampi of klotho mutant mice[2].

Animal Model: Klotho mutant mice treatment with Melatonin[2]
Dosage: 0.5 mg/kg or 1.0 mg/kg
Administration: Intravenous injection
Result: Significantly reversed antioxidant effects mediated by Melatonin. Significantly reversed the changes in the levels of these GSH-related parameters. Significantly reversed the memory function of Melatonin-treated klotho mutant mice.
Molecular Weight

279.38

Formula

C₁₉H₂₁NO

CAS No.

134865-74-0

SMILES

CCC(NC1CC2=C(C=CC=C2)C(C3=CC=CC=C3)C1)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
In solvent -80°C 6 months
  -20°C 1 month
References

Purity: >99.0%

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Keywords:

4-P-PDOTMelatonin ReceptorNrf2 ERKoxidativedamageGSHGSSGMT2memoryMelatoninInhibitorinhibitorinhibit

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