新規合成アズレン-1-カルボキサミジン誘導体HNS-32の心血管におよぼす作用 Cardiovascular Effects of Novel Azulene-1-Carboxamidine Derivative, HNS-32
A novel azulene-1-carboxamidine delivative (HNS-32) was synthesized and its cardiovascular effects were assessed using well-established isolated, blood-perfused, canine sinoatrial node, papillary muscle and atrioventricular node preparations. The yields of HNS-32 was about 44 % of the amount expected from the chemical equation. The found, chemical structure, molecular weight and color of HNS-32 were C<SUB>24</SUB>H<SUB>30</SUB>N<SUB>3</SUB>, N<SUP>1</SUP>-dimethyl-N<SUP>2</SUP>-(2-picolino) azulene-l-carboxamidine, 360.242 and dark blue, respectively. HNS-32 suppressed the sinus nodal automaticity and contractile force, while increased the coronary blood flow and AH and HV intervals (n=5). The drug shortened the repolarization phase of monophasic action potentials of right ventricle (n=4). The vasodilator effect was 3-10 times more potent than each cardiac effect. The pharmacological properties resemble those of calcium channel blocking drugs with modest sodium channel inhibition and potassium channel opening. HNS-32 may become a new drug with unique chemical structure that affects cardiovascular system.
日本薬理学雑誌 106, 192-196, 1995-09-01