73274-27-8Relevant academic research and scientific papers
MELANIN CONCENTRATING HORMONE RECEPTOR LIGANDS: SUBSTITUTED TETRAHYDROISOQUINOLINE ANALOGUES
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Page/Page column 28, (2010/02/13)
Melanin concentrating hormone receptor ligands (especially substituted tetrahydroisoquinoline analogues), capable of modulating MCH receptor activity, are provided. Such ligands may be used to modulate MCH binding to MCH receptors in vivo or in vitro, and are particularly useful in the treatment of a variety of metabolic, feeding and sexual disorders in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for treating such disorders are provided, as are methods for using such ligands for detecting MCH receptors (e.g., receptor localization studies).
Synthesis of novel substituted isoquinolones
Briet, Nicolas,Brookes, Michael H,Davenport, Richard J,Galvin, Frances C.A,Gilbert, Philip J,Mack, Stephen R,Sabin, Verity
, p. 5761 - 5766 (2007/10/03)
A series of novel substituted isoquinolones have been synthesised. This has been achieved by two routes, either Curtius rearrangment of cinnamic acids or via an isoquinoline N-oxide.
Inhibitors of phenylethanolamine N-methyltransferase and epinephrine biosynthesis: I. Chloro-substituted 1,2,3,4-tetrahydroisoquinolines
Bondinell,Chapin,Girard,Kaiser,Krog,Pavloff,Schwartz,Silvestri,Vaidya,Lam,Wellman,Pendleton
, p. 506 - 511 (2007/10/02)
In a search for inhibitors of epinephrine biosynthesis as potential therapeutic agents, a series of 13 ring-chlorinated 1,2,3,4-tetrahydroisoquinolines was prepared. These compounds were tested initially for their ability to inhibit rabbit adrenal phenylethanolamine N-methyltransferase (PNMT) in vitro. Enzyme-inhibitor dissociation constants, determined for the six most potent members of the series, indicated the following order of decreasing potency: 7,8-Cl2>6,7,8-Cl3>7-Cl~8-Cl>5,6,7,8-Cl4>5,7,8-Cl3. These compounds were subsequently examined for PNMT-inhibiting activity in intact rats and mice. 7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline (SK&F 64139) was the most potent member of the series both in vitro and in vivo and is currently undergoing clinical investigation.
