TRPV1-Targeted Drugs in Development for Human Pain Conditions
Stimulation of TRPV1 evokes a burning sensation, reflecting a central role of the channel in pain. Pharmacological and genetic studies have validated TRPV1 as a therapeutic target in several preclinical models of chronic pain, including cancer, neuropathic, postoperative and musculoskeletal pain.
TRPV1: ON THE ROAD TO PAIN RELIEF - PMC - PubMed Central …
On the basis of so much evidence, it is clear that TRPV1 plays a key role in the physiology of pain, not only integrating several pain-related molecular and physical signals but also mediating a response at several levels of action, from systemic effects through nerve depolarization and signal transmission to the brain, to local effects by ...
Current insights and therapeutic strategies for targeting TRPV1 in ...
2024年10月15日 · The function of TRPV1 in pain perception makes it a promising target for pain management. TRPV1 is a nonselective divalent and monovalent cation (such as Ca 2+, Mg 2+, K +, and Na +) channel that permits cations to pass through, thereby playing an important role in pain regulation, and functioning as a thermos-sensor to regulate body ...
TRPV1: A Potential Drug Target for Treating Various Diseases
Activation of TRPV1 has been linked to chronic inflammatory pain conditions and peripheral neuropathy, as observed in diabetes. Expression of TRPV1 is also observed in non-neuronal sites such as the epithelium of bladder and lungs and in hair cells of the cochlea.
TRP Channels and Pain - Neurobiology of TRP Channels - NCBI Bookshelf
8.4.1.5. TRPV1 in visceral pain. TRPV1 is expressed in DRG neurons that innervate the colon, pancreas, stomach, duodenum, and bladder and is responsible for pain produced by gastrointestinal system inflammation (Beyak and Vanner, 2005). In tissue biopsies of patients with inflammatory bowel disease (IBD), an increase in TRPV1 expression has ...
TRPV1 Antagonists and Chronic Pain: Beyond Thermal Perception
Preclinical localization and expression studies provide a firm foundation for the use of molecules targeting TRPV1 for conditions of bone pain, osteoarthritis and neuropathic pain. Selective TRPV1 antagonists weakly attenuate tactile and mechanical hypersensivity and are partially effective for behavioral and electrophysiological endpoints that ...
TRPV1: on the road to pain relief - PubMed
For these reasons as well as because its continuous activation causes analgesia, TRPV1 has become a viable drug target for clinical use in the management of pain. This review will provide a general picture of the physiological and pathophysiological roles of the TRPV1 channel and of its structural, pharmacological and biophysical properties.
Human TRPV1 structure and inhibition by the analgesic SB-366791
2023年4月28日 · TRPV1 channels are critical neuropathic pain sensors and brain inflammation detectors 8. The revealed mechanism of TRPV1 inhibition by a TRPV1-specific drug in development allows us to...
subfamily 1, TRPV1)通道是一种非选择性阳离子通 道，激活后可使细胞外钙离子内流，导致细胞内钙 离子浓度增高，进而介导一系列生理或病理反应。
TRPV1 in Pain and Itch - PubMed
The fundamental understandings of TRPV1-involved nociception, pruriception, neurogenic inflammation, and cell-specific modulation will help bring out more effective strategies of TRPV1 modulation in treating pain- and itch-related diseases.