Ensifentrine

Ensifentrine is a phosphodiesterase 3 (PDE3) inhibitor (IC₅₀ = 0.4 nM).¹ It is selective for PDE3 over PDE4 (IC₅₀ = 1,479 nM). Ensifentrine reduces phytohemagglutinin-induced proliferation of isolated human monocytes in a concentration-dependent manner and inhibits LPS-induced increases of TNF-α protein levels in isolated human monocytes (IC₅₀ = 520 nM). It increases cAMP levels in isolated human neutrophils when used at a concentration of 10 µM. Ensifentrine inhibits electric field stimulation-induced contractile responses in isolated guinea pig trachea in a concentration-dependent manner. Intranasal administration of ensifentrine (25% w/w) inhibits histamine-induced bronchoconstriction and tracheal edema in guinea pigs.

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1. Boswell-Smith, V., Spina, D., Oxford, A.W., et al. The pharmacology of two novel long-acting phosphodiesterase ¾ inhibitors, RPL554 [9,10-dimethoxy-2(2,4,6-trimethylphenylimino)-3-(N-carbamoyl-2-aminoethyl)-3,4,6,7-tetrahydro-2H-pyrimido[6,1-a]isoquinolin-4-one] and RPL565 [6,7-dihydro-2-(2,6-diisopropylphenoxy)-9,10-dimethoxy-4H-pyrimido[6,1-a]isoquinolin-4-one]. J. Pharmacol. Exp. Ther. 318(2), 840-848 (2006).