Description
Zaprinast (M&B 22948) is a potent, cGMP-specific phosphodiesterase inhibitor with IC50 of 0.5-0.76 and 0.15uM for PDE5 and PDE6 respectively, also is an agonist for GPR35 (EC50=16/840nM for rat/human GPR35); weakly inhibits PDE9, PDE10, and PDE11 with IC50 of 10-30uM; enhances the vasodilatory effects of nitric oxide in a range of vascular tissues by prolonging the cGMP-mediated activation of cGMP-dependent protein kinase; also reduces cellular 2HG levels by inhibiting the upstream enzyme glutaminase (GLS), reverses histone hypermethylation and soft-agar growth of IDH1-mutant cells. Asthma Discontinued