1-(4-胺乙酰胺基)苄基四氢异喹啉类化合物的合成及其心血管活性

Synthesis and Cardiovascular Activity of 1-(4- Aminoacetylamino)-Benzyl -1,2,3,4-Tetrahydroisoquinolines

研究发现某些异喹啉类化合物具有较好的心血管活性，Ｎ胺乙酰基取代的苄基四氢异喹啉化合物对二氢吡啶（ＤＨＰ）受体有较好的亲和力〔１〕．据报道〔２〕化合物１（２乙胺基乙酰胺基３，４二甲氧基）苄基异喹啉具有较强的抗心律失常作用，毒性远低于利多卡因．...

In an attempt to search for a novel antihypertensive or antiarrhythmic agents acting on calcium or potassium channels,8 novel 1-(4- Aminoacetylamino)-Benzyl -1,2,3,4-Tetrahydroisoquinolines compounds(Ⅶ 1～Ⅶ 8)were designed and prepared.Preliminary pharmacological studies showed that compound(Ⅶ 1) and (Ⅶ 7) were similar to tetrandrine on high KCl(80 mmol·L -1 ) induced contraction of rat aorta at the 10 -6 mol·L -1 concentration,and compound (Ⅶ 1) possessed potent antiarrhythmic action at the dose of 1 mg·kg -1 .