[Studies on cardiac ingredients of plants. X. Preparation of nitrates of tetrahydroproscillaridin and their pharmacological activities].
To reduce the vascular contracting effect of the hydrogenated cardiac glycosides, 20-(R)- and 20-(S)-tetrahydroproscillaridins (THPs, 1a, 1b), and to extend the concentration-dependent range, mono- and dinitrates of THPs were prepared. The pharmacological activities of the nitrates of THP were evaluated by use of isolated guinea-pig papillary muscle preparations and Na+,K(+)-adenosine triphosphatase preparations from dog kidney. Furthermore, the effect for smooth muscle was examined using the helical strips isolated from 13-week-old spontaneously hypertensive rat. The positive inotropic effects of mononitrates (11a, 11b, 2a, 2b, 8a, and 8b) were more potent than those of THPs. Nitration of the sugar moiety in THPs resulted in a vascular relaxing effect unobserved in the case of THPs.
Tanase
T
T
Faculty of Pharmaceutical Sciences, Nagoya City University, Japan.
Murakami
N
N
Nagatsu
A
A
Nagai
S
S
Sakakibara
J
J
Ando
H
H
Hotta
Y
Y
Takeya
K
K
Asano
M
M
D000818:Animals; D002301:Cardiac Glycosides / Q000138:chemical synthesis* / Q000494:pharmacology; D004285:Dogs; D004305:Dose-Response Relationship, Drug; D004951:Esterification; D006168:Guinea Pigs; D066298:In Vitro Techniques; D009200:Myocardial Contraction / Q000187:drug effects*; D009566:Nitrates; D011442:Proscillaridin / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000494:pharmacology; D000254:Sodium-Potassium-Exchanging ATPase / Q000037:antagonists & inhibitors*; D013268:Stimulation, Chemical; D013329:Structure-Activity Relationship
D002301:Cardiac Glycosides; D009566:Nitrates; C079220:tetrahydroproscillaridin; D000254:Sodium-Potassium-Exchanging ATPase; D011442:Proscillaridin