Quercetin, a bioflavonoid, reverses development of tolerance and dependence to morphine

Singh, Amanpreet; Naidu, Pattipati S.; Kulkarni, Shrinivas K.

doi:10.1002/ddr.10119

Cited by 10 publications

(13 citation statements)

References 26 publications

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“…Activation of Ras proteins requires posttranslational farnesylation, a process of covalently attaching a 15-carbon farnesyl moiety to conserved cysteine residues [32]. As result, there has been considerable interest recently in searching for inhibitors of farnesyltransferase (FTase) for use in the treatment of cancer [33,34].…”

Section: Inhibitors Of Protein Farnesyltrans-ferasementioning

confidence: 99%

“…Hasvold and coworkers developed a series of pyridone farnesyltransferase inhibitors (44), obtained through deletion of the B-ring of tipifarnib (R115777) (34) (Fig. 20) [43].…”

Section: Imidazole Containing Inhibitors Of Protein Farnesyltransferasementioning

confidence: 99%

“…22). To solve the selectivity issue with A315493(51), Wang and coworkers [44] compared A315493(51) closely with R115777 (34). To solve the selectivity issue with A315493(51), Wang and coworkers [44] compared A315493(51) closely with R115777 (34).…”

Section: Imidazole Containing Inhibitors Of Protein Farnesyltransferasementioning

confidence: 99%

“…However, A315493 (51) is also a potent GGTase-I inhibitor (IC 50 = 24nM). Both A315493 (51) and R115777 (34) have an N-methylimidazole ring that presumably interacts with the zinc ion in the catalytic site of FTase. Both A315493 (51) and R115777 (34) have an N-methylimidazole ring that presumably interacts with the zinc ion in the catalytic site of FTase.…”

Section: Imidazole Containing Inhibitors Of Protein Farnesyltransferasementioning

confidence: 99%

“…To solve the selectivity issue with A315493(51), Wang and coworkers [44] compared A315493(51) closely with R115777 (34). From a 3-D model, it appears that the 5-cyano-2pyridyl group of A315493 (51) occupies the same site as the N-methylquinolin-2-one of R115777 (34) . From a 3-D model, it appears that the 5-cyano-2pyridyl group of A315493 (51) occupies the same site as the N-methylquinolin-2-one of R115777 (34) .…”

Section: Imidazole Containing Inhibitors Of Protein Farnesyltransferasementioning

confidence: 99%

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Author Index to Volume 12

2006

curr med chem

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Imidazoles are an important class of heterocycles and include many substances of both biological and chemical interest. They are part of a large number of highly significant biomolecules such as the essential amino acid histidine and related compounds, biotin, and the imidazole alkaloids. Insertion of the imidazole nucleus is an important synthetic strategy in drug discovery. Imidazole drugs have broad applications in many areas of clinical medicine. The imidazoles are a class of antifungal azole derivatives and have a broad spectrum of activities both in vitro and in vivo. The imidazole moiety is also contained in many histaminergic ligands for histamine H1, H2, and H3 receptors. These are currently used as tools in pharmacological studies. The important therapeutic properties of imidazole related drugs have encouraged the medicinal chemists to synthesize and test a large number of novel molecules. Some of these have chemotherapeutic properties, such as for example several FTase inhibitors with an imidazole moiety. Imidazole derivatives have also been shown to have antibacterial activity and recently several P38 MAP Kinase inhibitors and 5-Lipoxygenase inhibitors containing the imidazole moiety have been synthesized. This review reports current progress in the area of new biologically active imidazoles and recently discovered naturally occurring imidazole.

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Section: Inhibitors Of Protein Farnesyltrans-ferasementioning

confidence: 99%

“…Hasvold and coworkers developed a series of pyridone farnesyltransferase inhibitors (44), obtained through deletion of the B-ring of tipifarnib (R115777) (34) (Fig. 20) [43].…”

Section: Imidazole Containing Inhibitors Of Protein Farnesyltransferasementioning

confidence: 99%

Section: Imidazole Containing Inhibitors Of Protein Farnesyltransferasementioning

confidence: 99%

Section: Imidazole Containing Inhibitors Of Protein Farnesyltransferasementioning

confidence: 99%

Section: Imidazole Containing Inhibitors Of Protein Farnesyltransferasementioning

confidence: 99%

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Author Index to Volume 12

2006

curr med chem

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Possible mechanisms of action in quercetin reversal of morphine tolerance and dependence

Naidu¹,

Singh²,

Joshi³

et al. 2003

Addiction Biology

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In an earlier study, we reported the ability of quercetin to reverse the development of morphine tolerance and dependence in mice. In the present study we have attempted to explore the possible involvement of nitric oxide (NO) system in quercetin reversal of morphine tolerance and dependence in mice. Co-administration of L-N(G)-nitro arginine methyl ester (L-NAME) or quercetin with morphine during the induction phase (days 1-9) delayed the development of tolerance to the antinociceptive action of morphine and also reversed naloxone precipitated withdrawal jumps. L-Arginine administration during the induction phase enhanced the development of tolerance to the antinociceptive effect of morphine but had no effect on the naloxone-precipitated withdrawal jumps. During the expression phase (day 10) acute administration of quercetin or L-NAME reversed, whereas L-arginine facilitated naloxone- precipitated withdrawal jumps in morphine-tolerant mice, but none of these drugs affected the nociceptive threshold in morphine-tolerant mice. Further, co-administration of quercetin or L-NAME with L-arginine during the induction phase antagonized the latter effects on the development of morphine tolerance. Also, prior administration of quercetin or L-NAME reversed the L-arginine potentiation of nalaxone-precipitated withdrawal jumps in morphine-tolerant mice. The results of the present study suggest that quercetin reversal of morphine tolerance and dependence may involve its ability to suppress nitric oxide synthase (NOS) activity.

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