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Synthesis and Characterizations of Novel Quinoline Derivatives Having Mixed Ligand Activities at the J and I Receptors: Potential Therapeutic Efficacy Against Morphine Dependence

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Title Synthesis and Characterizations of Novel Quinoline Derivatives Having Mixed Ligand Activities at the J and I Receptors: Potential Therapeutic Efficacy Against Morphine Dependence
 
Creator Deb, Ishani
Paira, Priyankar
Hazra, Abhijit
Banerjee, Sukdeb
Dutta, Pradeep Kumar
Mondal, Nirup B
Das, Sumantra
 
Subject Chemistry
 
Description 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 125I-Dynorphine,
3H-DAMGO and 125I-DADLE for j, l, and d receptors, respectively. Results showed varying degree
of activities of the compounds to j and l opioid receptors with negligible interactions at the d 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 IC50 of S4 revealed a greater affinity towards l compared to j receptor. In conclusion, quinoline derivatives
of S4 like structure offer potential tool for treatment of narcotic addictio
 
Date 2009
 
Type Article
PeerReviewed
 
Format application/pdf
 
Identifier http://www.eprints.iicb.res.in/996/1/22_BMC_2009.pdf
Deb, Ishani and Paira, Priyankar and Hazra, Abhijit and Banerjee, Sukdeb and Dutta, Pradeep Kumar and Mondal, Nirup B and Das, Sumantra (2009) Synthesis and Characterizations of Novel Quinoline Derivatives Having Mixed Ligand Activities at the J and I Receptors: Potential Therapeutic Efficacy Against Morphine Dependence. Bioorganic & Medicinal Chemistry, 17 (16). pp. 5782-5790.
 
Relation http://dx.doi.org/10.1016/j.bmc.2009.07.024
http://www.eprints.iicb.res.in/996/