473248-87-2

Upstream product

• 270574-03-3 3-[1,4']Bipiperidinyl-1'-ylmethyl-2-phenyl-quinoline-4-Carboxylic Acid Methyl Ester 
• 43071-45-0 3-methyl-2-phenylquinoline-4-carboxylic acid 
• 174636-71-6 3-methyl-2-phenylquinoline-4-carbonyl chloride 
• 74960-43-3 3-methyl-2-phenyl-quinoline-4-carboxylic acid methyl ester 
• 272104-64-0 methyl 3-bromomethyl-2-phenylquinoline-4-carboxylate 
• 91-56-5 indole-2,3-dione 
• 93-55-0 1-phenyl-propan-1-one 

Downstream Products

• 1336960-15-6 3-(1,4'-bipiperidin-1'-ylmethyl)-2-phenyl-N-(1-phenylcyclopropyl)-4-quinolinecarboxamide 

Relevant academic research and scientific papers

Discovery of GSK2193874: An Orally Active, Potent, and Selective Blocker of Transient Receptor Potential Vanilloid 4

Transient Receptor Potential Vanilloid 4 (TRPV4) is a member of the Transient Receptor Potential (TRP) superfamily of cation channels. TRPV4 is expressed in the vascular endothelium in the lung and regulates the integrity of the alveolar septal barrier. Increased pulmonary vascular pressure evokes TRPV4-dependent pulmonary edema, and therefore, inhibition of TRPV4 represents a novel approach for the treatment of pulmonary edema associated with conditions such as congestive heart failure. Herein we report the discovery of an orally active, potent, and selective TRPV4 blocker, 3-(1,4′-bipiperidin-1′-ylmethyl)-7-bromo-N-(1-phenylcyclopropyl)-2-[3-(trifluoromethyl)phenyl]-4-quinolinecarboxamide (GSK2193874, 28) after addressing an unexpected off-target cardiovascular liability observed from in vivo studies. GSK2193874 is a selective tool for elucidating TRPV4 biology both in vitro and in vivo.

TRPV4 ANTAGONISTS

The present invention relates to quinoline analogs, pharmaceutical compositions containing them and their use as TRPV4 antagonists.

Stepwise modulation of neurokinin-3 and neurokinin-2 receptor affinity and selectivity in quinoline tachykinin receptor antagonists

A stepwise chemical modification from human neurokinin-3 receptor (hNK-3R)-selective antagonists to potent and combined hNK-3R and hNK-2R antagonists using the same 2-phenylquinoline template is described. Docking studies with 3-D models of the hNK-3 and