Disease-Related Changes in TRPV1 Expression and Its Implications for Drug Development

Premkumar, Louis S.; Bishnoi, Mahendra

doi:10.2174/156802611796904834

Cited by 26 publications

(23 citation statements)

References 258 publications

(327 reference statements)

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“…Furthermore, as mentioned previously, this receptor is not found only in neurons, so blockade could also be problematic. Some of these issues have been reviewed by Premkumar and Bishnoi (2011), but the thermal changes as a potential problem were noted several years ago.…”

Section: Capsaicin As a Therapeutic Pharmacological Agentmentioning

confidence: 99%

Unravelling the Mystery of Capsaicin: A Tool to Understand and Treat Pain

O’Neill

Brock²,

Olesen³

et al. 2012

Pharmacol Rev

293

244

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Section: Capsaicin As a Therapeutic Pharmacological Agentmentioning

confidence: 99%

Unravelling the Mystery of Capsaicin: A Tool to Understand and Treat Pain

O’Neill

Brock²,

Olesen³

et al. 2012

Pharmacol Rev

293

244

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“…Capsaicin can induce its effects by causing Ca 2+ influx through TRPV1 overexpressed in cancerous cells, which can lead to cell death by apoptosis or necrosis. 85 …”

Section: Phytochemicals That Activate Transient Receptor Potential Vamentioning

confidence: 99%

“…Excretion of capsaicin through the kidneys can accumulate in the bladder and exert an effect on the urinary bladder. 85 …”

Section: Phytochemicals That Activate Transient Receptor Potential Vamentioning

confidence: 99%

Transient Receptor Potential Channels as Targets for Phytochemicals

Premkumar

2014

ACS Chem. Neurosci.

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To date, 28 mammalian transient receptor potential (TRP) channels have been cloned and characterized. They are grouped into six subfamilies on the basis of their amino acid sequence homology: TRP Ankyrin (TRPA), TRP Canonical (TRPC), TRP Melastatin (TRPM), TRP Mucolipin (TRPML), TRP Polycystin (TRPP), and TRP Vanilloid (TRPV). Most of the TRP channels are nonselective cation channels expressed on the cell membrane and exhibit variable permeability ratios for Ca2+ versus Na+. They mediate sensory functions (such as vision, nociception, taste transduction, temperature sensation, and pheromone signaling) and homeostatic functions (such as divalent cation flux, hormone release, and osmoregulation). Significant progress has been made in our understanding of the specific roles of these TRP channels and their activation mechanisms. In this Review, the emphasis will be on the activation of TRP channels by phytochemicals that are claimed to exert health benefits. Recent findings complement the anecdotal evidence that some of these phytochemicals have specific receptors and the activation of which is responsible for the physiological effects. Now, the targets for these phytochemicals are being unveiled; a specific hypothesis can be proposed and tested experimentally to infer a scientific validity of the claims of the health benefits. The broader and pressing issues that have to be addressed are related to the quantities of the active ingredients in a given preparation, their bioavailability, metabolism, adverse effects, excretion, and systemic versus local effects.

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“…This is particularly important in the context of the nerve terminal that also becomes refractory to stimulation. Moreover, changes in the expression (down-regulation or up-regulation) of TRPV1 have been associated with neuropathic pain during tissue injury, inflammation and bone cancer (Ueda, 2006;Premkumar and Bishnoi, 2011;Pan et al, 2010).…”

Section: The Role Of Trpv1 In Painmentioning

confidence: 99%