Transient receptor potential vanilloid type 1 (TRPV1) is found on sensory neurons, keratinocytes, sebocytes, and dendritic cells. Activated TRPV1 channels are believed to help propagate the itch sensation. Therefore, there has been great interest in targeting TRPV1 to treat pruritus. Since oral formulations aimed at TRPV1 have led to adverse effects such as hyperthermia, there has been emphasis on developing novel topical agents. Several companies are investigating topical TRPV1 anti-pruritic compounds and the initial data has been very promising. These drugs have the potential to be important treatment options for the management of itch. This paper reviews topical products in current development for pruritus that target TRPV1 channels.
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Drug Des Devel Ther
December 2024
Department of Anesthesiology, Faculty of Medicine, University of Yamanashi, Chuo, Yamanashi, Japan.
Purpose: Corneal pain is one of the most common eye symptoms caused by various types of epithelial injuries, including traumatic abrasion, chemical injury, ulcers, ultraviolet exposure, and infection. However, current therapeutic options for corneal pain are limited. In this study, we synthesized a novel quaternary ammonium compound, N-propylamiodarone bromide (NPA), and employed a rodent model of corneal injury to investigate whether NPA offers prolonged corneal analgesia through transient receptor potential vanilloid 1 (TRPV1) channel-mediated selective cellular entry, without hindering corneal epithelial recovery.
View Article and Find Full Text PDFJ Pharm Pharmacol
December 2024
Drugs Testing Laboratory Avam Anusandhan Kendra, Raipur, 492002, C.G., India.
Objectives: A primary objective of this review is to summarize the evidence-based pharmacological applications of capsaicin, particularly its use to manage pain and treat various health conditions. A second goal of the review is to research how recent technological advances are improving the bioavailability and therapeutic index of capsaicin, as well as the development of novel capsaicin-mimetics that are able to enhance therapeutic responses in various human diseases.
Methods: In the review, numerous human clinical trials and preclinical studies are examined to determine how effective, safe, and optimal dosages of capsaicin can be used in pain management and therapeutic applications.
J Nanobiotechnology
November 2024
Department of Anesthesiology, Renji Hospital, Shanghai Jiao Tong University School of Medicine, Shanghai, 200127, China.
Treating psoriasis presents a major clinical challenge because of the limitations associated with traditional topical glucocorticoid therapy. This study introduced a drug delivery system utilizing zinc-doped mesoporous silica nanoparticle (Zn-MSN) and microneedle (MN), designed to enhance drug utilization for prolonged anti-inflammatory and anti-itch effects. The MN system facilitated the transdermal delivery of betamethasone dipropionate (BD), allowing its slow release.
View Article and Find Full Text PDFFundam Clin Pharmacol
December 2024
Department of Veterinary Pharmacology, Faculty of Agriculture, Tottori University, Tottori, Japan.
Background/objectives: Topically applied antifungal agents can induce adverse effects, such as pain and irritation. The transient receptor potential (TRP) channels-TRPA1 and TRPV1-mainly expressed in sensory neurons, act as sensors for detecting irritants. This study aims to evaluate the involvement of nociceptive channels in topical antifungal-induced pain and irritation.
View Article and Find Full Text PDFEur J Med Chem
December 2024
Department of Pharmaceutical Sciences, Università Degli Studi Del Piemonte Orientale, Largo Donegani 2, 28100, Novara, Italy.
A growing body of evidence points to the existence of a crosstalk between the endovanilloid (EV)- and the endocannabinoid (EC) systems, leading to the concept of a single system based on a shared set of endogenous ligands and regulation mechanisms. The EV/EC system encompasses the ion channel TRPV1, the G protein coupled receptors CB1 and CB2, their endogenous ligands and the enzymes for biosynthesis and inactivation. Disorders in which the EV/EC interaction is involved are inflammation, pain, neurodegenerative diseases and disorders of bones and skin.
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