TRPA1 antagonists as potential analgesic drugs

Andrade, Edinéia Lemos de; Meotti, Flávia Carla; Calixto, João B.

doi:10.1016/j.pharmthera.2011.10.008

Cited by 136 publications

(128 citation statements)

References 203 publications

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“…TRPA1 as a target for analgesic drugs has been extensively reviewed elsewhere (Garrison and Stucky, 2011;Strassmaier and Bakthavatchalam, 2011;Andrade et al, 2012;Bautista et al, 2013;Brederson et al, 2013;Radresa et al, 2013;Koivisto et al, 2014). The potential role of TRPA1 in chemotherapy-induced neuropathic pain is described below.…”

Section: Transient Receptor Potential Channels: Acquired Diseasesmentioning

confidence: 99%

Transient Receptor Potential Channels as Drug Targets: From the Science of Basic Research to the Art of Medicine

2014

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Section: Transient Receptor Potential Channels: Acquired Diseasesmentioning

confidence: 99%

Transient Receptor Potential Channels as Drug Targets: From the Science of Basic Research to the Art of Medicine

2014

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“…107 The use of TRPA1 channel inhibitors (for example, AP-18, A-967079, HC-030031 and Chembridge-5861528) reduces hyperalgesic and allodynic symptoms after a peripheral lesion produced by either nerve chronic constriction or inflammation. 108 Blocking purinergic P2X receptors with A-740003 antagonists also reduces neuropathic pain induced by a peripheral inflammation. 109 In CCI models, systemic administration of ZD7288 and Eugenol, two inhibitors of hyperpolarization-activated cyclic nucleotide-gated channels channels, produces a significant decrease in allodynic responses after nerve injury.…”

Section: Therapeutic Approaches In Neuropathic Pain Based On the Neurmentioning

confidence: 99%

Neuroplasticity of ascending and descending pathways after somatosensory system injury: reviewing knowledge to identify neuropathic pain therapeutic targets

et al. 2016

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Study design: This is a narrative review of the literature. Objectives: This review aims to be useful in identifying therapeutic targets. It focuses on the molecular and biochemical neuroplasticity changes that occur in the somatosensory system, including ascending and descending pathways, during the development of neuropathic pain. Furthermore, it highlights the latest experimental strategies, based on the changes reported in the damaged nociceptive neurons during neuropathic pain states. Setting: This study was conducted in Girona, Catalonia, Spain. Methods: A MEDLINE search was performed using the following terms: descending pain pathways; ascending pain pathways; central sensitization; molecular pain; and neuropathic pain pharmacological treatment. Results and conclusion: Neuropathic pain triggered by traumatic lesions leads to sensitization and hyperexcitability of nociceptors and projection neurons of the dorsal horn, a strengthening in the descendent excitatory pathway and an inhibition of the descending inhibitory pathway of pain. These functional events are associated with molecular plastic changes such as overexpression of voltagegated ion channels, algogen-sensitive receptors and synthesis of several neurotransmitters. Molecular studies on the plastic changes in the nociceptive somatosensory system enable the development of new pharmacological treatments against neuropathic pain, with higher specificity and effectiveness than classical drug treatments. Although research efforts have already focused on these aspects, additional research may be necessary to further explore the potential therapeutic targets in neuropathic pain involved in the neuroplasticity changes of neuropathological pathways from the injured somatosensory system.

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“…Many reports show that TRPA1 is a potentially interesting target for controlling pain (42). Systemic injection of A967079 decreases spontaneous and mechanically evoked firing of spinal neurons in uninjured, osteoarthritic, and inflamed rats (43).…”

Section: Discussionmentioning

confidence: 99%

Molecular Basis Determining Inhibition/Activation of Nociceptive Receptor TRPA1 Protein

Banzawa

Saito

Imagawa

et al. 2014

Journal of Biological Chemistry

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Background: Nociceptive TRPA1 is an important drug discovery target for identification of analgesics. Results: A967079, one of the most potent mammalian TRPA1 antagonists, showed marked species differences. Conclusion: A single amino acid was responsible for inhibitory/stimulatory actions of A967079. Significance: The present data provide novel insight in the search for analgesics targeting TRPA1.

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TRPA1 antagonists as potential analgesic drugs

Cited by 136 publications

References 203 publications

Transient Receptor Potential Channels as Drug Targets: From the Science of Basic Research to the Art of Medicine

Transient Receptor Potential Channels as Drug Targets: From the Science of Basic Research to the Art of Medicine

Neuroplasticity of ascending and descending pathways after somatosensory system injury: reviewing knowledge to identify neuropathic pain therapeutic targets

Molecular Basis Determining Inhibition/Activation of Nociceptive Receptor TRPA1 Protein

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