4-P-PDOT 是一种选择性和亲和性的褪黑激素受体拮抗剂，可显著抵消褪黑激素介导的抗氧化作用。它对MT2的选择性是 MT1 的 300 倍以上。

4-P-PDOT is a potent, selective and affinity Melatonin receptor (MT2) antagonist.

In CHO-mt1 cells the amidotetraline 4-P-PDOT (10 mM) has no effect on forskolin-stimulated cyclic AMP levels, either alone, or in the presence of Melatonin. However, 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].

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 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]. 4-P-PDOT treatment significantly reverses the memory function of Melatonin-treated klotho mutant mice.

134865-74-0

C19H21NO

279.38

4-phenyl-2- propionamidotetralin

DMSO:41.67 mg/mL (149.15 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years