Detail of "69441-18-5"

Reference

Inhibition of cyclic AMP phosphodiesterase by 2,6-dimethyl-4-(3-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylic acid 3-[2-(N-benzyl-N-methylamino)] ethyl ester 5-methyl ester hydrochloride (YC-93), a potent vasodilator

Sakamoto, Nobuo; Terai, Michio; Takenaka, Toichi; Maeno, Hiroo (Dep. Pharm. Biochem., Yamanouchi Pharmacol. Co. Ltd., Tokyo, Japan). Biochem. Pharmacol., 27(8), 1269-74 (English) 1978. CODEN: BCPCA6. ISSN: 0006-2952. DOCUMENT TYPE: Journal CA Section: 1 (Pharmacodynamics) Section cross-reference(s): 7 A potent vasodilator, YC-93 (I) [54527-84-3] competitively inhibited cyclic AMP phosphodiesterase (II) [9036-21-9] in the 105,000g supernatant of canine basilar, carotid, coronary, and femoral arteries. At cyclic AMP concns. of approx.In this experiment, several chemicals are used like 69441-18-5 1mM (low Km of II), Ki of I was 2.0-4.3mM, and at cyclic AMP concns. of 50-70mM (high Km) Ki was 4.0-12mM. At either concn. of cyclic AMP, I was more potent than papaverine and 3-isobutyl-1-Me xanthine. The simplest 1,4-dihydropyridine deriv. studied, 3,5-diethoxycarbonyl-1,4-dihydro-2,4,6-collidine-HCl [632-93-9], had an inhibiting potency slightly less than papaverine, but 2 structural modifications greatly increased this potency; these were the addn. of a nitrophenyl group at position 4 of the 1,4-dihydropyridine ring, and the replacement of Et ester at position 3 of this ring by N-benzyl-N-methylaminoethyl ester. Cyclic AMP concn. increased by 64% 1 min after exposure to 1mM I, so II inhibition could be assocd. with the vasodilatory action of the drug. .