摘要
采用离体和在体标本研究新化合物 TMEP即 ( 1- (萘满酮 - 5 -氧基 ) - 3 - [2 - ( 2 -甲氧基苯氧基 )乙胺基 ]- 2 -丙醇盐酸盐 )对肾上腺素受体的阻断作用。结果发现 ,TMEP可使激动剂的量效曲线平行右移 ,最大反应不降低。阻断α1 受体的 PA2 为 7.4 6± 0 .2 0 ( n=8) ;阻断 β1受体的 PA2 值为 7.11± 0 .2 7( n=8)。可呈剂量依赖性地使异丙肾上腺素诱发家兔心率加快的量效曲线右移 ,同时降低血压。证明 TMEP是一竞争性 α1 和 β1 肾上腺素受体的阻断剂。
In vitro and in vivo samples were used to study the adrenoceptor blocking activity of a novel compound 1 (terealone 5 oxy) 3 [(2 methoxyphenoxy) ethamine] 2 propyld hydrochloride (TMEP) The results indicated that TMEP produced parallel rightward shifts with no significant change in the maximal response The PA2 value for α blocking were 7 46±0 20 ( n =8) in rat anococcygeal muscles and 7 11±0 27 ( n =8) for β blocking in guinea pig atrium The dose response curve of isoprenaline induced tachycardia shifted rightward with a dose dependent manner and the mean arterial blood pressure decreased at the same time It was demonstrated that the TMEP was a competitive antagonist agent against α 1 and β 1 adrenoceptor
出处
《同济医科大学学报》
CAS
CSCD
北大核心
2001年第2期139-141,共3页
Acta Universitatis Medicinae Tongji
关键词
肾上腺素受体阻断剂
TMEP
降压药
丙醇盐酸盐
adrenergic blockade
β 1 adrenergic blockade
PA2
1 (terealone 5 oxy) 3 [(2 methoxyphenoxy) ethamine] 2 propyld hydrochloride