Targeting TRP channels for pain relief

Brederson, Jill-Desiree; Kym, Philip R.; Szállaśi, A

doi:10.1016/j.ejphar.2013.03.003

Cited by 257 publications

(233 citation statements)

References 157 publications

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“…TRPV1 channel ligation can be beneficial in one organ and induce unacceptable adverse side effects in another 56. For example, in clinical trials, small molecule TRPV1 (TRPV3 and TRPA1) antagonists were used to treat inflammatory, neuropathic, and visceral pain, but studies were terminated because of adverse effects induced by TRPV1 antagonists 100. Hyperthermia and impaired noxious heat sensation placed patients at risk for scalding injury.…”

Section: Summary: Promise and Challenges For Cannabinoid Therapeuticsmentioning

confidence: 99%

“…Hyperthermia and impaired noxious heat sensation placed patients at risk for scalding injury. Second generation TRP antagonists that do not induce an increase in core body temperature has been reported, nevertheless the therapeutic utility is not yet known 100. Administration of CB1 agonists in vivo causes complex hemodynamic changes, including changes of heart rate as well as increased and decreased blood pressure 101…”

Section: Summary: Promise and Challenges For Cannabinoid Therapeuticsmentioning

confidence: 99%

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Cannabinoids, the Heart of the Matter

Alfulaij

Meiners

Michalek

et al. 2018

JAHA

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Section: Summary: Promise and Challenges For Cannabinoid Therapeuticsmentioning

confidence: 99%

Section: Summary: Promise and Challenges For Cannabinoid Therapeuticsmentioning

confidence: 99%

Cannabinoids, the Heart of the Matter

Alfulaij

Meiners

Michalek

et al. 2018

JAHA

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“…A number of target sites have been proposed for the treatment of PDN [Vincent et al 2011]. Manipulation of the temperature-sensitive transient receptor potential (TRP) channel on nociceptive neurons has been proposed as an attractive strategy in targeting the pain pathway, especially since TRPV1 desensitization by topical agonists such as capsaicin has been in use for PDN [Brederson et al 2013].…”

Section: Future Directionsmentioning

confidence: 99%

Treatment of painful diabetic neuropathy

Javed

Petropoulos²,

Alam

et al. 2014

Therapeutic Advances in Chronic Disease

179

129

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Painful diabetic neuropathy (PDN) is a debilitating consequence of diabetes that may be present in as many as one in five patients with diabetes. The objective assessment of PDN is difficult, making it challenging to diagnose and assess in both clinical practice and clinical trials. No single treatment exists to prevent or reverse neuropathic changes or to provide total pain relief. Treatment of PDN is based on three major approaches: intensive glycaemic control and risk factor management, treatments based on pathogenetic mechanisms, and symptomatic pain management. Clinical guidelines recommend pain relief in PDN through the use of antidepressants such as amitriptyline and duloxetine, the γ-aminobutyric acid analogues gabapentin and pregabalin, opioids and topical agents such as capsaicin. Of these medications, duloxetine and pregabalin were approved by the US Food and Drug Administration (FDA) in 2004 and tapentadol extended release was approved in 2012 for the treatment of PDN. Proposed pathogenetic treatments include α-lipoic acid (stems reactive oxygen species formation), benfotiamine (prevents vascular damage in diabetes) and aldosereductase inhibitors (reduces flux through the polyol pathway). There is a growing need for studies to evaluate the most potent drugs or combinations for the management of PDN to maximize pain relief and improve quality of life. A number of agents are potential candidates for future use in PDN therapy, including Nav 1.7 antagonists, N-type calcium channel blockers, NGF antibodies and angiotensin II type 2 receptor antagonists.

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“…Julius and co-workers discovered that TRPV 1 was activated by vanilloid compounds and noxious thermal stimuli and desensitized when sufficiently provoked in calcium-dependent fashion, a discovery that may underlie the paradoxical analgesic effect of capsaicin. TRP channels have been targeted for pain relief [40]. Qutenza is the brand name of a capsaicin containing patch, which has an anaesthetic effect and is used for management of peripheral neuropathic pain.…”

Section: Pro Nociceptive Componentsmentioning

confidence: 99%

“…Correlations between the lipids in plasma and in microdialysate were analysed at each time point (20,40,60,80, and 120 minutes after catheter insertion) to reveal the fluctuation between systemic and locally sampled levels. The blood samples were collected at one time point (200 min after MD catheter insertion).…”

Section: Papers Ii-iii: a Comparison Of The Lipid Levels In Microdialmentioning

confidence: 99%

Endocannabinoids and Related Lipids in Chronic Pain: Analytical and Clinical Aspects

Stensson¹

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Targeting TRP channels for pain relief

Cited by 257 publications

References 157 publications

Cannabinoids, the Heart of the Matter

Cannabinoids, the Heart of the Matter

Treatment of painful diabetic neuropathy

Endocannabinoids and Related Lipids in Chronic Pain: Analytical and Clinical Aspects

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