Transient receptor potential (TRP) ankyrin 1 (TRPA1) and vanilloid 1 (TRPV1) receptors are implicated in modulation of cough and nociception. In vivo, TRPA1 and TRPV1 are often co-expressed in neurons and TRPA1V1 hetero-tetramer formation is noted in cells co-transfected with the respective expression plasmids. In order to understand the impact of TRP receptor interaction on activity, we created stable cell lines expressing the TRPA1, TRPV1 and co-expressing the TRPA1 and TRPV1 (TRPA1V1) receptors. Among the 600 compounds screened against these receptors, we observed a number of compounds that activated the TRPA1, TRPV1 and TRPA1V1 receptors; compounds that activated TRPA1 and TRPA1V1; compounds that activated TRPV1 and TRPA1V1; compounds in which TRPA1V1 response was modulated by either TRPA1 or TRPV1; and compounds that activated only TRPV1 or TRPA1 or TRPA1V1; and one compound that activated TRPA1 and TRPV1, but not TRPA1V1. These results suggest that co-expression of TRPA1 and TRPV1 receptors imparts unique activation profiles different from that of cells expressing only TRPA1 or TRPV1.

Download full-text PDF

Source
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4092848PMC
http://dx.doi.org/10.3390/cells3020616DOI Listing

Publication Analysis

Top Keywords

trpa1 trpv1
36
trpv1 trpa1v1
16
compounds activated
16
trpa1
12
trpv1
12
activated trpa1
12
transient receptor
8
receptor potential
8
trpv1 co-expressing
8
trpv1 receptors
8

Similar Publications

Optimization and Calibration of 384-well Kinetic Ca Mobilization Assays for the Human Transient Receptor Potential Cation Channels TRPM8, TRPV1, and TRPA1.

SLAS Discov

December 2024

Department of Pharmaceutical Sciences, School of Pharmacy, University of Pittsburgh, Pittsburgh, PA 15261, USA; University of Pittsburgh Hillman Cancer Center, Pittsburgh, PA 15232, USA. Electronic address:

Development, optimization, and calibration of human transient receptor potential (TRP) channel Ca mobilization assays for TRPM8, TRPV1, and TRPA1 are described. Heterologous expression of hTRPM8 in HEK293T cells was required for anti-TRPM8 antibody staining and TRPM8 agonist induced Ca mobilization signals which were both used to optimize transfection efficiency. FLIPR Calcium 6 dye concentration, loading time, and TRPM8 transfected cell seeding density were optimized and a DMSO tolerance of ≤0.

View Article and Find Full Text PDF

Ion Channels as Potential Drug Targets in Dry Eye Disease and Their Clinical Relevance: A Review.

Cells

December 2024

Center for Research on Harmful Effects of Biological and Chemical Hazards, Departments of Genetics, Microbiology and Immunology, Faculty of Medical Sciences, University of Kragujevac, 69 Svetozar Markovic Street, 34000 Kragujevac, Serbia.

Dry eye disease (DED) is a common multifactorial disorder characterized by a deficiency in the quality and/or quantity of tear fluid. Tear hyperosmolarity, the dysfunction of ion channel proteins, and eye inflammation are primarily responsible for the development and progression of DED. Alterations in the structure and/or function of ion channel receptors (transient receptor potential ankyrin 1 (TRPA1), transient receptor potential melastatin 8 (TRPM8), transient receptor potential vanilloid 1 and 4 (TRPV1 and TRPV4)), and consequent hyperosmolarity of the tears represent the initial step in the development and progression of DED.

View Article and Find Full Text PDF

Responses to the activation of different intranasal trigeminal receptors: Evidence from behavioral, peripheral and central levels.

Behav Brain Res

December 2024

Smell and Taste Clinic, Department of Otorhinolaryngology, Faculty of Medicine Carl Gustav Carus, Technische Universität Dresden, Dresden, Germany.

Aim: There are various receptors that mediate intranasal trigeminal sensations. However, few studies compare the response patterns across different receptor activations.

Methods: We recorded negative mucosal potentials (NMPs) in 24 healthy participants and event-related potentials (ERPs) in 17 participants during exposure to five odors that trigger trigeminal sensations and one olfactory stimulus.

View Article and Find Full Text PDF

Xibining inhibition of the PI3K-AKT pathway reduces M1 macrophage polarization to ameliorate KOA synovial inflammation and nociceptive sensitization.

Phytomedicine

November 2024

Department of Orthopaedics and Traumatology, Affiliated Hospital of Nanjing University of Chinese Medicine, Jiangsu Provincial Hospital of Traditional Chinese Medicine, Nanjing 210023, PR China.. Electronic address:

Background: Pain is the most critical symptom of knee osteoarthritis(KOA), which seriously affects the quality of life of patients. Xibining (XBN), a traditional herbal compound, has achieved good results in the clinical treatment of KOA, and its mechanism of action is worth exploring in depth.

Objective: In vivo and in vitro models of KOA were constructed, and the potential drug action mechanism of XBN in improving osteoarthritis pain was explored in combination with transcriptomics.

View Article and Find Full Text PDF

Background: Pruritus ani (PA), a neurofunctional dermatosis, is one of the most common complications of hemorrhoids, which seriously affects the quality of life of patients. Medical hemorrhoid gel (MHG), a product mainly composed of herbal medicine, is widely used for treatment of PA clinically. This study aim to assess the alleviating effect and mechanism of MHG on PA based on rectal epidermis-spinal cord-brain axis using animal models.

View Article and Find Full Text PDF

Want AI Summaries of new PubMed Abstracts delivered to your In-box?

Enter search terms and have AI summaries delivered each week - change queries or unsubscribe any time!