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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.

journal_name

Bioorg Med Chem

journal_title

Bioorganic & medicinal chemistry

authors

Deb I,Paira P,Hazra A,Banerjee S,Dutta PK,Mondal NB,Das S

doi

10.1016/j.bmc.2009.07.024

subject

Has Abstract

pub_date

2009-08-15 00:00:00

pages

5782-90

issue

16

eissn

0968-0896

issn

1464-3391

pii

S0968-0896(09)00680-4

journal_volume

17

pub_type

杂志文章

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