TRPC4/5 inhibitors: Phase I results and proof of concept studies
Sign Up to like & getrecommendations! Published in 2024 at "European Archives of Psychiatry and Clinical Neuroscience"
DOI: 10.1007/s00406-024-01890-0
Abstract: Transient receptor potential canonical (TRPC) ion channels are expressed in areas of the brain responsible for processing emotion and mood and have been implicated in the pathophysiology of internalizing disorders such as major depressive disorder… read more here.
Keywords: ion channels; inhibitors phase; trpc4 inhibitors; phase results ... See more keywords
Elevated Expression of TRPC4 in Cortical Lesions of Focal Cortical Dysplasia II and Tuberous Sclerosis Complex
Sign Up to like & getrecommendations! Published in 2017 at "Journal of Molecular Neuroscience"
DOI: 10.1007/s12031-017-0923-z
Abstract: Focal cortical dysplasia type II (FCD II) and tuberous sclerosis complex (TSC) are well-known causes of chronic refractory epilepsy in children. Canonical transient receptor potential channels (TRPCs) are non-selective cation channels that are commonly activated… read more here.
Keywords: focal cortical; tuberous sclerosis; sclerosis complex; cortical dysplasia ... See more keywords
Property-Based Design of Xanthine Derivatives as Potent and Orally Available TRPC4/5 Inhibitors for Depression and Anxiety.
Sign Up to like & getrecommendations! Published in 2025 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.4c02870
Abstract: Transient receptor potential canonical channels 4 and 5 (TRPC4/5) are nonselective cation channels involved in emotional regulation, positioning them to be promising targets for treating mental disorders such as anxiety and depression. HC-070, a potent… read more here.
Keywords: property based; trpc4 inhibitors; trpc4; based design ... See more keywords
The Molecular Heterogeneity of Store-Operated Ca2+ Entry in Vascular Endothelial Cells: The Different roles of Orai1 and TRPC1/TRPC4 Channels in the Transition from Ca2+-Selective to Non-Selective Cation Currents
Sign Up to like & getrecommendations! Published in 2023 at "International Journal of Molecular Sciences"
DOI: 10.3390/ijms24043259
Abstract: Store-operated Ca2+ entry (SOCE) is activated in response to the inositol-1,4,5-trisphosphate (InsP3)-dependent depletion of the endoplasmic reticulum (ER) Ca2+ store and represents a ubiquitous mode of Ca2+ influx. In vascular endothelial cells, SOCE regulates a… read more here.
Keywords: trpc4; endothelial cells; trpc1 trpc4; store operated ... See more keywords
Molecular evolution of TRPC4 regulatory sequences supports a role in mammalian thermoregulatory adaptation
Sign Up to like & getrecommendations! Published in 2025 at "PeerJ"
DOI: 10.7717/peerj.19697
Abstract: Background Proteins encoded by the canonical transient receptor potential (Trpc) gene family form transmembrane channels involved in diverse signal-transduction pathways. Trpc4 has been shown necessary for the induction of nonshivering thermogenesis (NST) in mice, a… read more here.
Keywords: mammalian thermoregulatory; evolutionary rate; regulatory sequences; selection ... See more keywords