134865-74-0

134865-74-0 structure

Name: 4-P-PDOT
Chemical Name: N-[(2S,4R)-4-phenyl-1,2,3,4-tetrahydronaphthalen-2-yl]propanamide
CAS Number: 134865-74-0
Molecular Formula: C₁₉H₂₁NO
Molecular Weight: 279.37600
Catalog: Signaling Pathways GPCR/G Protein Melatonin Receptor
Create Date: 2019-06-08 17:36:20
Modify Date: 2024-01-02 17:56:06
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].

Name	N-[(2S,4R)-4-phenyl-1,2,3,4-tetrahydronaphthalen-2-yl]propanamide
Synonyms	Tocris-1034 4-P-PDOT 4P-PDOT

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].
Related Catalog	Signaling Pathways >> Neuronal Signaling >> Melatonin Receptor Signaling Pathways >> GPCR/G Protein >> Melatonin Receptor Research Areas >> Neurological Disease
Target	MT2 receptor[1]
In Vitro	In CHO-mt1 cells the amidotetraline 4-P-PDOT (10 mM) has no eect 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.
References	[1]. Dubocovich ML. Melatonin receptors: are there multiple subtypes? Trends Pharmacol Sci. 1995 Feb;16(2):50-6. [2]. hin EJ, et al. Melatonin attenuates memory impairment induced by Klotho gene deficiency via interactive signaling between MT2 receptor, ERK, and Nrf2-related antioxidant potential. Int J Neuropsychopharmacol. 2014 Dec 30;18(6). pii: pyu105. [3]. Christopher Browning, et al. Pharmacological characterization of human recombinant melatonin mt1 and MT2 receptors. British Journal of Pharmacology (2000) 129, 877-886. [4]. Dubocovich ML, et al. Melatonin receptor antagonists that differentiate between the human Mel1a and Mel1b recombinant subtypes are used to assess the pharmacological profile of the rabbit retina ML1 presynaptic heteroreceptor. Naunyn Schmiedebergs Arch Pharmacol. 1997 Mar;355(3):365-75.

Density	1.11g/cm3
Boiling Point	480.1ºC at 760 mmHg
Molecular Formula	C₁₉H₂₁NO
Molecular Weight	279.37600
Flash Point	292ºC
Exact Mass	279.16200
PSA	29.10000
LogP	4.05040
Vapour Pressure	2.22E-09mmHg at 25°C
Index of Refraction	1.595

Symbol	GHS07
Signal Word	Warning
Hazard Statements	H302
RIDADR	NONH for all modes of transport
RTECS	TX1498350

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