HA-1004 (hydrochloride)

HA-1004 is an inhibitor of protein kinase G (PKG) and PKA (K_is = 1.4 and 2.3 μM, respectively). It also inhibits PKC and blocks intracellular calcium mobilization. HA-1004 induces relaxation of isolated rabbit aortic strips precontracted with histamine, serotonin , A23187 , angiotensin II , or prostaglandin F_2α (; EC₅₀s = 0.32-0.63 μM), as well as phenylephrine (Item Nos. 18619 | 17205) with or without calcium (EC₅₀s = 2.3 and 0.5 μM, respectively). It also inhibits histamine-induced bronchoconstriction in guinea pigs without affecting blood pressure when administered intratracheally at a dose of 0.1 mg per animal.