Synthesis and characterizations of novel quinoline derivatives having mixed ligand activities at the kappa and mu receptors: Potential therapeutic efficacy against morphine dependence.

Abstract	Based on an established 3D pharmacophore, a series of quinoline derivatives were synthesized. The opioidergic properties of these compounds were determined by a competitive binding assay using (125)I-Dynorphine, (3)H-DAMGO and (125)I-DADLE for kappa, mu, and delta receptors, respectively. Results showed varying degree of activities of the compounds to kappa and mu opioid receptors with negligible interactions at the delta receptor. The compound, S4 was the most successful in inhibiting the two most prominent quantitative features of naloxone precipitated withdrawal symptoms - stereotyped jumping and body weight loss. Determination of IC(50) of S4 revealed a greater affinity towards mu compared to kappa receptor. In conclusion, quinoline derivatives of S4 like structure offer potential tool for treatment of narcotic addictions.
Authors	Ishani Deb, Priyankar Paira, Abhijit Hazra, Sukdeb Banerjee, Pradip Kumar Dutta, Nirup Bikash Mondal, Sumantra Das
Journal	Bioorganic & medicinal chemistry (Bioorg Med Chem) Vol. 17 Issue 16 Pg. 5782-90 (Aug 15 2009) ISSN: 1464-3391 [Electronic] England
PMID	19640720 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
Chemical References	2-(2-methylquinolin-4-ylamino)-N-phenylacetamide Acetanilides Aminoquinolines Ligands Narcotic Antagonists Quinolines Receptors, Opioid, kappa Receptors, Opioid, mu
Topics	Acetanilides (chemical synthesis, chemistry, pharmacology) Aminoquinolines (chemical synthesis, chemistry, pharmacology) Animals Cell Line, Tumor Competitive Bidding Humans Ligands Mice Mice, Inbred BALB C Morphine Dependence (drug therapy) Narcotic Antagonists (chemical synthesis, chemistry, pharmacology) Quinolines (chemical synthesis, chemistry, pharmacology) Rats Receptors, Opioid, kappa (antagonists & inhibitors, metabolism) Receptors, Opioid, mu (antagonists & inhibitors, metabolism)

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