KMUP-1

KMUP-1 is a synthetic xanthine derivative with broad phosphodiesterase (PDE) inhibitory activity (notably on PDE3, PDE4, and PDE5), leading to increased levels of cyclic AMP and cyclic GMP. It acts through molecular pathways involving protein kinase A (PKA), protein kinase G (PKG), and modulation of potassium channels. KMUP-1 also activates soluble guanylate cyclase (sGC), enhances the nitric oxide (NO)/cGMP pathway, and exhibits anti-inflammatory and anti-oxidant activities in multiple preclinical models. It is being investigated primarily for pulmonary arterial hypertension (PAH), osteoarthritis, inflammatory diseases, periodontitis, and retinopathy. Studies have shown effects such as tracheal relaxation, attenuation of pulmonary vasoconstriction, inhibition of osteoclastogenesis, anti-inflammatory activity, and retinoprotective effects in animal disease models.[1][2][3][4][5][6][10]

Other names

7-[2-[4-(2-chlorophenyl)piperazinyl]ethyl]-1,3-dimethylxanthine