Mexiletine 10mg/5ml oral solution

Pore-forming subunit of Nav1.5, a voltage-gated sodium (Nav) channel that directly mediates the depolarizing phase of action potentials in excitable membranes. Navs, also called VGSCs (voltage-gated sodium channels) or VDSCs (voltage-dependent sodium channels), operate by switching between closed and open conformations depending on the voltage difference across the membrane. In the open conformation they allow Na(+) ions to selectively pass through the pore, along their electrochemical gradient.

The influx of Na(+) ions provokes membrane depolarization, initiating the propagation of electrical signals throughout cells and tissues .
PMID:1309946 PMID:21447824 PMID:23085483 PMID:23420830 PMID:25370050 PMID:26279430 PMID:26392562 PMID:26776555

Nav1.5 is the predominant sodium channel expressed in myocardial cells and it is responsible for the initial upstroke of the action potential in cardiac myocytes, thereby initiating the heartbeat .
PMID:11234013 PMID:11804990 PMID:12569159 PMID:1309946

Required for normal electrical conduction including formation of the infranodal ventricular conduction system and normal action potential configuration, as a result of its interaction with XIRP2 (By similarity)

Ligand-activated transcription factor that enables cells to adapt to changing conditions by sensing compounds from the environment, diet, microbiome and cellular metabolism, and which plays important roles in development, immunity and cancer .
PMID:23275542 PMID:30373764 PMID:32818467 PMID:7961644

Upon ligand binding, translocates into the nucleus, where it heterodimerizes with ARNT and induces transcription by binding to xenobiotic response elements (XRE) .
PMID:23275542 PMID:30373764 PMID:7961644

Regulates a variety of biological processes, including angiogenesis, hematopoiesis, drug and lipid metabolism, cell motility and immune modulation .
PMID:12213388
Xenobiotics can act as ligands: upon xenobiotic-binding, activates the expression of multiple phase I and II xenobiotic chemical metabolizing enzyme genes (such as the CYP1A1 gene) .
PMID:7961644 PMID:33193710
Mediates biochemical and toxic effects of halogenated aromatic hydrocarbons .
PMID:34521881 PMID:7961644
Next to xenobiotics, natural ligands derived from plants, microbiota, and endogenous metabolism are potent AHR agonists .
PMID:18076143
Tryptophan (Trp) derivatives constitute an important class of endogenous AHR ligands .
PMID:32818467 PMID:32866000
Acts as a negative regulator of anti-tumor immunity: indoles and kynurenic acid generated by Trp catabolism act as ligand and activate AHR, thereby promoting AHR-driven cancer cell motility and suppressing adaptive immunity .
PMID:32818467
Regulates the circadian clock by inhibiting the basal and circadian expression of the core circadian component PER1 .
PMID:28602820
Inhibits PER1 by repressing the CLOCK-BMAL1 heterodimer mediated transcriptional activation of PER1 .
PMID:28602820
The heterodimer ARNT:AHR binds to core DNA sequence 5'-TGCGTG-3' within the dioxin response element (DRE) of target gene promoters and activates their transcription PMID:28602820