742075-06-5

Upstream product

• 103-67-3 benzyl-methyl-amine 
• 742075-03-2 tert-butyl (4R,4aS,7aR,12bS)-4a-hydroxy-9-methoxy-7-oxo-1,2,4,4a,5,6,7,7a-octahydro-3H-4,12-methanobenzofuro[3,2-e]isoquinoline-3-carboxylate 
• 52446-07-8 (4′R,4a′S,7a′R,12b′S)-9′-methoxy-1′,2′,3′,4′,5′,6′-hexahydro-4a′H,7a′H-spiro[[1,3]dioxolane-2,7′-[4,12]methanobenzofuro[3,2-e]isoquinolin]-4a′-ol 
• 197242-23-2 17-(cyclopropylmethyl)-4,5α-epoxy-14-hydroxy-3-methoxy-6-(1,3-dioxolan-2-yl)morphinan 
• 16617-07-5 naltrexone methyl ether 
• 16676-29-2 naltrexone Hydrochloride 
• 52446-25-0 noroxyoxycodone hydrochloride 

Relevant academic research and scientific papers

Syntheses of potential metabolites of a potent κ-opioid receptor agonist, TRK-820

Chemical syntheses of three kinds of potential metabolites of TRK-820, a potent κ-opioid receptor agonist, were described. One of the potential metabolites 2, 17-N-dealkylated TRK-820, was synthesized starting from noroxycodone through 8 steps in 21% tota

Design and Synthesis of Potent and Highly Selective Orexin 1 Receptor Antagonists with a Morphinan Skeleton and Their Pharmacologies

Nalfurafine, a κ-selective opioid receptor agonist, unexpectedly showed a selective antagonist activity toward the orexin 1 receptor (OX1R) (Ki = 250 nM). Modification of the 17-amino side chain of the opioid ligand to an arylsulfonyl group and the 6-furan acrylamide chain to 2-pyridyl acrylamide led to compound 71 with improvement of the antagonist activity (OX1R, Ki = 1.36 nM; OX2R, not active) without any detectable affinity for the opioid receptor. The dihydrosulfate salt of 71, freely soluble in water, attenuated the physical dependence of morphine. Furthermore, all of the active nalfurafine derivatives in this study had almost no activity for OX2R, which led to high OX1R selectivity. These results suggest that nalfurafine derivatives could be a useful series of lead compounds to develop highly selective OX1R antagonists.