Danegaptide (GAP-134), has been identified as a potent and selective second generation gapjunction modifier with oral bioavailability.a small modified dipeptide.
Rotigaptide is a novel and specific modulator of Cx43 and is a potent AAP. Rotigaptide prevents the uncoupling of Cx43-mediated gapjunction communication and normalizes cell-to-cell communication during acute metabolic stress.
PQ1, as an enhancer of gapjunction in SW480 human colorectal cancer cells can act by restoring GJIC and increasing connexin expression in breast cancer cell lines while not affecting normal mammary cells.
PQ1 Succinate, a gapjunction enhancer, acts by restoring GJIC and increasing connexin expression in breast cancer cell lines while not affecting normal mammary cells.
Anandamide (AEA), an endogenous cannabinoid, interacts with both central (CB1) and peripheral (CB2) cannabinoid receptors. Its effects are concluded through the cellular uptake and enzymatic breakdown of its amide bond by fatty acid amide hydrolase. Arachidonoyl-N-methyl amide, an analog of anandamide, specifically targets the human CB1 receptor, displaying a binding affinity with a Ki of 60 nM. It completely inhibits rat glial gapjunction intercellular communication at a concentration of 50 µM.