4-(3,4-Dihydroxyphenyl)-1,2,3,4-tetrahydroisoquinoline derivatives. II. Their renal vasodilation activity and structure-activity relationship.
A series of 4-(3,4-dihydroxyphenyl)-1,2,3,4-tetrahydroisoquinoline derivatives showed potent DA1 agonistic activities. We investigated the structure-activity relationship of the racemic compounds of this series. 4-(3,4-Dihydroxyphenyl)-7-methanesulfonamido-1,2,3,4-tetrahydroiso quinoline (43) was identified as a potent renal vasodilator with activity almost equal to that of YM435 (1).
Anan
H
H
Institute for Drug Discovery Research, Yamanouchi Pharmaceutical Co., Ltd., Ibaraki, Japan.
Tanaka
A
A
Tsuzuki
R
R
Yokota
M
M
Yatsu
T
T
Fujikura
T
T
D000818:Animals; D004285:Dogs; D018491:Dopamine Agonists / Q000737:chemistry / Q000494:pharmacology; D004305:Dose-Response Relationship, Drug; D005260:Female; D007546:Isoquinolines / Q000737:chemistry / Q000494:pharmacology*; D008297:Male; D017447:Receptors, Dopamine D1 / Q000819:agonists; D012079:Renal Circulation / Q000187:drug effects*; D013329:Structure-Activity Relationship; D044005:Tetrahydroisoquinolines; D014665:Vasodilator Agents / Q000138:chemical synthesis* / Q000494:pharmacology
D018491:Dopamine Agonists; D007546:Isoquinolines; D017447:Receptors, Dopamine D1; D044005:Tetrahydroisoquinolines; D014665:Vasodilator Agents; C073504:zelandopam