Article
Chemistry, Multidisciplinary
Seong Gi Lim, Sung Eun Seo, Seongjae Jo, Kyung Ho Kim, Lina Kim, Oh Seok Kwon
Summary: In this study, a fast and convenient approach for screening lead vanilloid compounds targeting TRPV1 was proposed. A graphene field-effect transistor with human TRPV1 receptor protein as the bioprobe was fabricated and verified using various analyses. Simulations and experimental analyses confirmed the binding affinity of the ligands with TRPV1.
Article
Biochemistry & Molecular Biology
Joanna K. Bujak, Daria Kosmala, Kinga Majchrzak-Kuligowska, Piotr Bednarczyk
Summary: The study confirmed the expression of the TRPV1 ion channel on both mRNA and protein levels in canine PBMC, and indicated that the ion channel is functional.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2021)
Article
Chemistry, Medicinal
Dmytro Isaev, Keun-Hang Susan Yang, Waheed Shabbir, Frank Christopher Howarth, Murat Oz
Summary: Capsaicin, a natural alkaloid derived from chili pepper, has various pharmacological effects and can affect cardiovascular function by inhibiting ion currents in cardiac myocytes. Therefore, caution should be exercised when administering capsaicin to individuals with cardiac channelopathies or arrhythmia-prone conditions.
Review
Biochemistry & Molecular Biology
Arpad Szallasi
Summary: Resiniferatoxin (RTX) is a potent analgesic with a wide range of pharmacological actions. Targeted RTX therapy shows promise in cancer pain management and treatment of knee pain in patients with osteoarthritis.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2023)
Review
Chemistry, Medicinal
Murat Oz, Dietrich E. Lorke, Frank C. Howarth
Summary: Capsaicin, derived from chili pepper, has various pharmacological actions, including analgesic, anticancer, anti-inflammatory, antiobesity, and antioxidant effects. It acts on not only TRPV1 receptor, but also other ion channels and enzymes. This study categorizes the non-TRPV1 targets of capsaicin and discusses the cellular and molecular mechanisms of its TRPV1-independent effects.
MEDICINAL RESEARCH REVIEWS
(2023)
Article
Multidisciplinary Sciences
Tianci Li, Gaoge Wang, Vivian Chin Chin Hui, Daniel Saad, Joao de Sousa Valente, Paolo La Montanara, Istvan Nagy
Summary: Increased activity and excitability of molecules like TRPV1 in pain-sensing neurons are crucial for pathological pain. Two major mechanisms, post-translational changes in TRPV1 induced by inflammatory mediators and TRPV1 activation-induced feed-forward signalling, contribute to TRPV1 sensitisation in injured tissues. Upregulation in COX2 expression and increased synthesis of COX2 products play a role in TRPV1 activation-induced sensitisation in nociceptive neurons.
SCIENTIFIC REPORTS
(2021)
Article
Neurosciences
Pavel Adamek, Mario Heles, Anirban Bhattacharyya, Monica Pontearso, Jakub Slepicka, Jiri Palecek
Summary: The novel FDA-approved PI3K delta/gamma isoform-specific inhibitor duvelisib shows promising ability in preventing paclitaxel-induced peripheral neuropathy, indicating its potential for use in human medicine.
JOURNAL OF NEUROSCIENCE
(2022)
Article
Multidisciplinary Sciences
Isabel Wank, Lisa Kutsche, Silke Kreitz, Peter Reeh, Andreas Hess
Summary: RTX desensitization of TRPV1-signaling disrupts thermal nociception and affects two distinct brain subnetworks, leading to reduced central nervous system responses to high temperatures in male rats. Resting state and graph-theoretical network analyses provide detailed insight into cerebral processing of noxious temperatures.
Article
Neurosciences
Shi-Yu Deng, Xue-Chun Tang, Yue-Chen Chang, Zhen-Zhen Xu, Qin-Yi Chen, Nan Cao, Liang-Jing-Yuan Kong, Yang Wang, Ke-Tao Ma, Li Li, Jun-Qiang Si
Summary: This study showed that activation of TRPV1 by capsaicin increases the expression and function of NKCC1 protein in DRG, possibly mediated by the PKC/p-ERK signaling pathway. These findings suggest that DRG NKCC1 may participate in the inflammatory pain induced by TRPV1.
FRONTIERS IN CELLULAR NEUROSCIENCE
(2021)
Review
Pharmacology & Pharmacy
Vipin Arora, James N. Campbell, Man-Kyo Chung
Summary: Capsaicin, the pungent ingredient in chili peppers, can cause intense burning pain in humans, but it has also been used as an analgesic for chronic pain conditions. The analgesic effects of capsaicin depend on concentration, with low concentrations inducing short-term defunctionalization and high concentrations leading to long-term defunctionalization.
PHARMACOLOGY & THERAPEUTICS
(2021)
Article
Pharmacology & Pharmacy
He-Ya Qian, Fang Zhou, Rui Wu, Xiao-Jun Cao, Tao Zhu, Hao-Dong Yuan, Ya-Nan Chen, Ping-An Zhang
Summary: The study showed that intrathecal injection of TRPV1 inhibitor or ASICs antagonist significantly increased the paw withdraw threshold of BCP rats. Intraperitoneal injection of Metformin or Vinorelbine markedly elevated the PWT of BCP rats and reduced the expression of TRPV1 and ASIC3 in L4-6 DRGs. This suggests an effective analgesic effect of Metformin on mechanical allodynia of BCP rats, possibly mediated by the downregulation of ASIC3 and TRPV1.
FRONTIERS IN PHARMACOLOGY
(2021)
Article
Cell Biology
Ya-Kai Xie, Hao Luo, Shan-Xin Zhang, Xiao-Ying Chen, Ran Guo, Xiao-Yun Qiu, Shuai Liu, Hui Wu, Wen-Bo Chen, Xing-Hua Zhen, Qiang Ma, Jin-Lan Tian, Shun Li, Xinzhong Chen, Qingjian Han, Shumin Duan, Chengyong Shen, Fan Yang, Zhen-Zhong Xu
Summary: This study reveals the mechanisms underlying the development of DNP in patients with diabetes and identifies a potential therapeutic target. The researchers found that GPR177 in A-fiber neurons mediates the secretion of WNT5a, which in turn activates the TRPV1 ion channel and causes pain. These findings contribute to the search for therapies to relieve neuropathic pain.
SCIENCE TRANSLATIONAL MEDICINE
(2022)
Article
Anesthesiology
Juliana M. M. Navia-Pelaez, Julia Borges Paes Lemes, Leonardo Gonzalez, Lauriane Delay, Luciano dos Santos Aggum Capettini, Jenny W. W. Lu, Gilson Goncalves Dos Santos, Ann M. M. Gregus, Patrick M. M. Dougherty, Tony L. L. Yaksh, Yury I. I. Miller
Summary: Nociceptive signaling in DRG neurons is regulated by the assembly of receptors in lipid rafts. TLR4 and TRPV1 play important roles in this process. AIBP, a protein that targets cholesterol depletion from TLR4-expressing cells, can reverse the effects of CIPN by regulating lipid raft-associated nociceptive processing. This study highlights the significance of lipid rafts and their control by AIBP in nociceptive signaling regulation.
Article
Pharmacology & Pharmacy
Mircea Iftinca, Manon Defaye, Christophe Altier
Summary: TRPV1 is a significant channel in pain perception and its agonists are being studied for chronic pain management. While TRPV1 antagonists have limited clinical use due to side effects, capsaicin offers a potential avenue for long-lasting pain relief by defunctionalising nociceptors. The development of TRPV1-targeted drugs could provide a new generation of analgesics for various pain conditions.
Article
Chemistry, Medicinal
Qianqian Liang, Zhen Qiao, Qiqi Zhou, Dengqi Xue, KeWei Wang, Liming Shao
Summary: This study reports the synthesis of N-indazole-4-aryl piperazine carboxamide analogues as TRPV1 modulators. Compound 28 is identified as a potent and selective TRPV1 agonist, relieving inflammatory and thermal pain by desensitizing the native TRPV1 current in mice. The study also reveals an important hydrogen interaction between Arg557 and the indazole of compound 28.
JOURNAL OF MEDICINAL CHEMISTRY
(2022)