Synthesis and Characterizations of Novel Quinoline Derivatives Having Mixed Ligand Activities at the J and I Receptors: Potential Therapeutic Efficacy Against Morphine Dependence
IR@IICB: CSIR-Indian Institute of Chemical Biology, Kolkata
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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
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| Creator |
Deb, Ishani
Paira, Priyankar Hazra, Abhijit Banerjee, Sukdeb Dutta, Pradeep Kumar Mondal, Nirup B Das, Sumantra |
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| Subject |
Chemistry
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| 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
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| Date |
2009
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| Type |
Article
PeerReviewed |
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| Format |
application/pdf
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| 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. |
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| Relation |
http://dx.doi.org/10.1016/j.bmc.2009.07.024
http://www.eprints.iicb.res.in/996/ |
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