The antinociceptive effect and mechanism of action of SY0916

Zhang, Haijing; Wu, Li‐Wei; Liu, Yang; Peng, Shan-Ying; Wang, Wenjie

doi:10.1016/j.intimp.2016.01.004

Cited by 4 publications

(3 citation statements)

References 37 publications

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“…Antinociceptive activity of TA was further assessed using the tail-flick test [17]. Mice were treated with TA (100, 200 and 400 mg/kg, i.g.)…”

Section: Tail-flick Testmentioning

confidence: 99%

“…Classical types of analgesic medication for treating pain include non-steroidal anti-inflammatory drugs (NSAIDs) and opioids [3]. However, long-term use of NSAIDs can induce some adverse effects, such as gastric mucosal injury and hemorrhage, and the repeated use of opioids can induce severe drug dependence [4,5]. Thus, the clinical efficacy and application of conventional analgesics were limited by their unwanted adverse effects.…”

Section: Introductionmentioning

confidence: 99%

See 1 more Smart Citation

Anti-nociceptive effect of total alkaloids isolated from the seeds of Areca catechu L (Arecaceae) in mice

Zhao¹,

Yu²,

Yang³

et al. 2017

Trop. J. Pharm Res

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“…Antinociceptive activity of TA was further assessed using the tail-flick test [17]. Mice were treated with TA (100, 200 and 400 mg/kg, i.g.)…”

Section: Tail-flick Testmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Anti-nociceptive effect of total alkaloids isolated from the seeds of Areca catechu L (Arecaceae) in mice

Zhao¹,

Yu²,

Yang³

et al. 2017

Trop. J. Pharm Res

View full text Add to dashboard Cite

“…Platelet-activation factor (PAF) is considered a significant inflammatory mediator of different pathologies, including various types of inflammation [1, 2], allergy [3], and immune diseases [4, 5]. SY0916 ((E)-ethyl1-(5-(4-chlorophenyl)-3-oxopent-4-enyl)piperidine-4-carboxylate, Figure 1), a first-in-class PAF receptor antagonist, has been proven to be highly effective for rheumatoid arthritis therapy in preclinical studies and has been shown to be safe in phase I clinical trials [6–11]. Unlike commercially available antiarthritis drugs, which have the side effect of causing gastrointestinal injury, SY0916 possesses the notable advantage of protecting gastric mucosa [6].…”

Section: Introductionmentioning

confidence: 99%

Degradation Characteristics of a Novel PAF Receptor Antagonist, SY0916, in Aqueous Solution

Jin

Wang

Zhang

et al. 2019

Journal of Analytical Methods in Chemistry

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SY0916 has been proven to be a potent treatment agent against rheumatoid arthritis in preclinical studies and has been shown to be safe in phase I clinical trials. However, SY0916 is unstable in water, which is frequently used in pharmaceutical development processes. The degradation behaviour and stability of SY0916 in aqueous solutions were investigated at different pH levels, periods of time, and temperatures. Two degradation products (DPs) were successfully separated and characterized by liquid chromatography coupled to high-resolution tandem mass spectrometry (LC-HRMS/MS), liquid chromatography coupled to nuclear magnetic resonance with solid phase extraction (LC-SPE-NMR), and nuclear magnetic resonance (NMR). SY0916 decomposed to its α,β-unsaturated ketone in protonic solvents, and the α,β-unsaturated ketone further transformed into its alcohol form through a conjugate addition reaction in aqueous media. The results of this study indicate that the pH of the buffer solutions should be maintained between 3.0 and 3.6 for maximum SY0916 stability. Factors that affect degradation should be carefully controlled to mitigate or avoid drug decay.

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Pharmacological and toxicological evaluations of the new pyrazole compound (LQFM-021) as potential analgesic and anti-inflammatory agents

et al. 2016

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Chronic inflammation is a world health problem. There is a need to develop new anti-inflammatory and analgesic drugs with improved activity and reduced side effects. In this context, the aim of this study was to evaluate the antinociceptive and anti-inflammatory effects of the pyrazole compound LQFM-021 after acute and sub-chronic administration in rats submitted to a CFA-induced chronic arthritis model, as well as compare the toxicity of this compound to that of dipyrone, given throughout 7 days. Firstly, we observed that acute oral administration of the higher dose (130 µmol/kg) of LQFM-021 reduced paw lifting time (PET) and edema formation. These effects disappeared on the following day, requiring another dose to maintain the effects. This dose also promoted reduction of the polymorphonuclear recruitment in the synovial fluid. In another experiment, both treatments with LQFM-021, 65 µmol/kg twice a day and 130 µmol/kg once a day, produced a progressive and permanent reduction of the PET and edema, also reducing polymorphonuclear recruitment. However, the single treatment with 130 µmol/kg was more effective than the double treatment with 65 µmol/kg. LQFM-021 did not produce toxicity signs. However, dipyrone (130 µmol/kg once a day) promoted erosion of the epithelial cells and decreased mucus in the gastric mucosa. These data indicate that LQFM-021 produced antinociceptive and anti-inflammatory effects in CFA-induced arthritis in rats. These effects occurred in the absence of apparent toxic effects, indicating that the pyrazole compound LQFM-021 may be considered a good prototype for development of new analgesic/anti-inflammatory drug.

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The antinociceptive effect and mechanism of action of SY0916

Cited by 4 publications

References 37 publications

Anti-nociceptive effect of total alkaloids isolated from the seeds of Areca catechu L (Arecaceae) in mice

Anti-nociceptive effect of total alkaloids isolated from the seeds of Areca catechu L (Arecaceae) in mice

Degradation Characteristics of a Novel PAF Receptor Antagonist, SY0916, in Aqueous Solution

Pharmacological and toxicological evaluations of the new pyrazole compound (LQFM-021) as potential analgesic and anti-inflammatory agents

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