[HTML][HTML] A journey from molecule to physiology and in silico tools for drug discovery targeting the transient receptor potential vanilloid type 1 (TRPV1) channel

CA Amaya-Rodriguez, K Carvajal-Zamorano… - Frontiers in …, 2024 - frontiersin.org
The heat and capsaicin receptor TRPV1 channel is widely expressed in nerve terminals of
dorsal root ganglia (DRGs) and trigeminal ganglia innervating the body and face …

A comprehensive review on the regulatory action of TRP channels: a potential therapeutic target for nociceptive pain

S Anand, S Rajagopal - Neuroscience Insights, 2023 - journals.sagepub.com
The transient receptor potential (TRP) superfamily of ion channels in humans comprises
voltage-gated, non-selective cation channels expressed both in excitable as well as non …

Daidzein attenuated paclitaxel-induced neuropathic pain via the down-regulation of TRPV1/P2Y and up-regulation of Nrf2/HO-1 signaling

S Zafar, Y Luo, L Zhang, CH Li, A Khan, MI Khan… - …, 2023 - Springer
Paclitaxel (PTX) is an anti-microtubule agent, used for the treatment of various types of
cancers; however, it produces painful neuropathy which limits its use. Many neuroprotective …

Discovery of N-(1-(2-hydroxyethyl) quinolin-2-one)-N'-(1-phenyl-1H-pyrazol-5-yl) methyl) urea as Mode-Selective TRPV1 antagonist

D Zuo, M Hong, A Jung, S Lee, N Do, S Jung… - Bioorganic & Medicinal …, 2024 - Elsevier
To discover mode-selective TRPV1 antagonists as thermoneutral drug candidates, the
previous potent antagonist benzopyridone 2 was optimized based on the pharmacophore A …

Design, synthesis, and analgesia evaluation of novel Transient Receptor Potential Vanilloid 1 (TRPV1) agonists modified from Cannabidiol (CBD)

F Jin, Y Wen, G Lin, S Yu, C Wang, W Ye… - Bioorganic & Medicinal …, 2023 - Elsevier
Pain-relief is a long-term research hotspot with huge demand in clinical treatment. The
analgesics currently used have several side effects, such as being addictive and causing …

[HTML][HTML] Painful diabetic neuropathy: The role of ion channels

Q Wang, Y Ye, L Yang, L Xiao, J Liu, W Zhang… - Biomedicine & …, 2024 - Elsevier
Painful diabetic neuropathy (PDN) is a common chronic complication of diabetes that
causes neuropathic pain and negatively affects the quality of life. The management of PDN …

[HTML][HTML] Design and experimental validation of a new radiolabeled analog of N-(3-hydroxy-4-methoxy-phenyl-methyl) ferrocene-carboxamide (VFC) targeting the …

T Dallegi, SB Hassen, N Rached, F Menjji… - European Journal of …, 2024 - Elsevier
The TRPV1 receptor has been recognized to play a role in cancer development, being
overexpressed in prostate, breast, lung, and colon cancers. Since TRPV1 activation …

Discovery of N-(1, 4-Benzoxazin-3-one) urea analogs as Mode-Selective TRPV1 antagonists

G Huang, A Jung, LX Li, N Do, S Jung, Y Jeon… - Bioorganic & Medicinal …, 2024 - Elsevier
Abstract A series of 1, 4-benzoxazin-3-one analogs were investigated to discover mode-
selective TRPV1 antagonists, since such antagonists are predicted to minimize target-based …

5‐Alkoxy‐1‐aryl‐3‐polyfluoroalkylpyrazoles with Antinociceptive Activity: Partial Agonists of TRPV1 Ion Channels

OG Khudina, YV Burgart, NA Malkova… - …, 2023 - Wiley Online Library
Chemoselective O‐alkylation of 1‐aryl‐3‐polyfluoroalkylpyrazol‐5‐oles under basic
conditions resulted in a series of 5‐alkoxypyrazoles (26 derivatives). They showed an …

Neuropathy, its Profile and Experimental Nerve Injury Neuropathic Pain Models: A Review

K Kumar Sharma, N Fatima, Z Ali… - Current …, 2023 - ingentaconnect.com
Neuropathy is a terrible disorder that has a wide range of etiologies. Drug-induced
neuropathy, which happens whenever a chemical agent damages the peripheral nerve …