title: Synthesis, resolution, and renal vasodilation activity of novel DA1 agonists: 4-(3,4-dihydroxyphenyl)-1,2,3,4-tetrahydroisoquinoline derivatives.
abstract: 7,8-Dihydroxy-4-(3,4-dihydroxyphenyl)-1,2,3,4-tetrahydroisoquinoline (1) and 4-(3,4-dihydroxyphenyl)-7-hydroxy-8-methyl-1,2,3, 4-tetrahydroisoquinoline (2) are potent renal vasodilators which selectively stimulate DA1 (peripheral dopamine receptor-1) receptors. Especially, (S)-(-)-1 is the most potent. Its DA1 agonist activity is about 10 times stronger than dopamine for increasing renal blood flow in anesthetized dogs. The renal and cardiovascular effects of (S)-(-)-1 may be suitable for the treatment of patients with renal insufficiency, heart failure and hypertension.
authors.affiliation: Central Research Laboratories, Yamanouchi Pharmaceutical Co., Ltd., Ibaraki, Japan.
authors.forename: H
authors.initials: H
authors.lastname: Anan
authors.forename: A
authors.initials: A
authors.lastname: Tanaka
authors.forename: R
authors.initials: R
authors.lastname: Tsuzuki
authors.forename: M
authors.initials: M
authors.lastname: Yokota
authors.forename: T
authors.initials: T
authors.lastname: Yatsu
authors.forename: K
authors.initials: K
authors.lastname: Honda
authors.forename: M
authors.initials: M
authors.lastname: Asano
authors.forename: S
authors.initials: S
authors.lastname: Fujita
authors.forename: T
authors.initials: T
authors.lastname: Furuya
authors.forename: T
authors.initials: T
authors.lastname: Fujikura
mesh_terms: D000818:Animals; D004285:Dogs; D018492:Dopamine Antagonists; D006439:Hemodynamics / Q000187:drug effects; D007546:Isoquinolines / Q000138:chemical synthesis* / Q000494:pharmacology; D017447:Receptors, Dopamine D1; D012079:Renal Circulation / Q000187:drug effects*; D044005:Tetrahydroisoquinolines; D014665:Vasodilator Agents / Q000494:pharmacology*
chemical_list: D018492:Dopamine Antagonists; D007546:Isoquinolines; D017447:Receptors, Dopamine D1; D044005:Tetrahydroisoquinolines; D014665:Vasodilator Agents; C073506:4-(3,4-dihydroxyphenyl)-7-hydroxy-8-methyl-1,2,3,4-tetrahydroisoquinoline; C073504:zelandopam