Short transient receptor potential channel 4 (TRPC4) (TRPC4)

Short transient receptor potential channel 4 (TRPC4) is a non-selective cation channel that belongs to the canonical subfamily of transient receptor potential (TRP) channels (UniProt, 2024). It is widely expressed in the brain, particularly in the amygdala and hippocampus, as well as in peripheral tissues like the vascular endothelium and smooth muscle (NCBI Gene, 2024). TRPC4 plays a critical role in regulating intracellular calcium homeostasis, which is essential for processes such as neurotransmitter release, smooth muscle contraction, and vascular permeability (PubMed, 2023). In the central nervous system, TRPC4 is heavily involved in the mediation of fear and anxiety-related behaviors, making it a significant target for neuropsychiatric drug development (PubMed, 2018). In the periphery, it contributes to the regulation of vascular tone and has been implicated in conditions like pulmonary arterial hypertension (PubMed, 2021). Pharmacological modulation of TRPC4, primarily through small-molecule inhibitors like ML204 and HC-070, is being investigated for the treatment of generalized anxiety disorder and various gastrointestinal and cardiovascular conditions (PubChem, 2024). Activators like Englerin A have also shown potential in oncology by inducing calcium-mediated cytotoxicity in specific cancer cell lines (PubMed, 2015).

Other names

TRP4CCE1Transient receptor potential cation channel subfamily C member 4hTrp-4hTrp4

TRPC4 inhibitors block the non-selective cation current, reducing intracellular calcium levels and modulating downstream signaling pathways involved in smooth muscle contraction or neuronal excitability (PubMed, 2018).