127255-69-0

Upstream product

• 3470-53-9 6-amino-1-tetralone 
• 1679-18-1 4-Chlorophenylboronic acid 
• 66361-67-9 6-bromo-3,4-dihydro-2H-naphthalen-1-one 

Relevant academic research and scientific papers

Discovery of Potent and Selective Agonists of δ Opioid Receptor by Revisiting the "message-Address" Concept

The classic "message-address" concept was proposed to address the binding of endogenous peptides to the opioid receptors and was later successfully applied in the discovery of the first nonpeptide δ opioid receptor (DOR) antagonist naltrindole. By revisiting this concept, and based on the structure of tramadol, we designed a series of novel compounds that act as highly potent and selective agonists of DOR among which (-)-6j showed the highest affinity (Ki = 2.7 nM), best agonistic activity (EC50 = 2.6 nM), and DOR selectivity (more than 1000-fold over the other two subtype opioid receptors). Molecular docking studies suggest that the "message" part of (-)-6j interacts with residue Asp1283.32 and a neighboring water molecule, and the "address" part of (-)-6j packs with hydrophobic residues Leu3007.35, Val2816.55, and Trp2846.58, rendering DOR selectivity. The discovery of novel compound (-)-6j, and the obtained insights into DOR-agonist binding will help us design more potent and selective DOR agonists.

6 - Substituted aryl amino methyl tetralin derivatives or salts thereof, and its preparation and use

The invention provides a 6-substituted aryl amino methyl tetrahydronaphthalene derivative or salt thereof and a preparation method and application of the 6-substituted aryl amino methyl tetrahydronaphthalene derivative, belongs to the pharmaceutical field

5-Aryl-indan-1-one and analogs useful as progesterone receptor modulators

Compounds of formula I or II are provided, wherein R1—R8 are defined herein, and pharmaceutical compositions and kits containing these compounds. Also provides are methods of inducing contraception, providing hormone replacement ther