Comparative effects of nicorandil and nitroglycerin on tracheal and vascular smooth muscle in the dog, in vivo and in vitro.

The effects of nicorandil (NCR) on tracheal and vascular smooth muscle in the dog were compared with those of nitroglycerin (NTG) in in vitro and in vivo preparations. In the isolated tracheal strip and coronary artery preparations contracted with KCl (30 mM), the ability of NCR to relax these muscles and arteries by 50% was 1/10-1/15 as potent as NTG. In blood-perfused tracheal preparations, single doses of NCR and NTG injected into the tracheal artery produced dose-related decreases in the intraluminal pressure (ILP) of the trachea (relaxation) and increases in the tracheal blood flow (TBF). When the potency of NCR relative to that of NTG was compared on the basis of doses decreasing the ILP and increasing the TBF by 50%, NCR was 822 times less potent than NTG in producing tracheal relaxation and 572 times less potent in producing tracheal vasodilation. The effects of NCR on the ILP and TBF were not antagonized by propranolol. In non-perfused tracheal preparations, the two drugs administered i.v. elicited the effects in a similar dose-dependent manner; decreases in systemic blood pressure (SBP), left ventricular systolic pressure (LVP), pressure-rate product (PRP), femoral vascular resistance (FVR), and ILP and increases in heart rate (HR) and LVdP/dt max. The results show that NCR has a potent bronchodilating action and that its pharmacological profile is somewhat similar to NTG.

[1]  K. Sakai,et al.  Hypotensive effects and biotransformation of nicorandil, a new antianginal agent, administered to rats by different routes: comparison with nitroglycerin and isosorbide dinitrate , 1984, The Journal of pharmacy and pharmacology.

[2]  K. Sakai,et al.  Pharmacologic potency and selectivity of a new bronchodilator agent, 2,3-dihydro-7-methyl-9-phenyl-1H-pyrazolo [1,2-a] indazolium bromide (FKK) on canine tracheal preparations "in vivo" and "in vitro". , 1983, Archives internationales de pharmacodynamie et de therapie.

[3]  N. Taira,et al.  Effects of nicorandil and its congeners on musculature and vasculature of the dog trachea in situ. , 1982, Archives internationales de pharmacodynamie et de therapie.

[4]  K. Sakai,et al.  The hypotensive mechanisms of the new anti-anginal drug, N-(2-hydroxyethyl)nicotinamide nitrate (SG-75) in beagle dogs. , 1981, Japanese journal of pharmacology.

[5]  N. Taira,et al.  Effects of trapidil on musculature and vasculature of the dog trachea in situ. , 1981, Archives internationales de pharmacodynamie et de therapie.

[6]  T. Itoh,et al.  Vasodilating actions of 2-nicotinamidoethyl nitrate on porcine and guinea-pig coronary arteries. , 1981, The Journal of pharmacology and experimental therapeutics.

[7]  N. Taira,et al.  EFFECTS OF GLYCERYL TRINITRATE AND SIN‐1A ON MUSCULATURE AND VASCULATURE OF THE DOG TRACHEA in situ , 1981, British Journal of Pharmacology.

[8]  K. Sakai,et al.  Cardiovascular Effects of a New Coronary Vasodilator N‐(2‐Hydroxyethyl)nicotinamide Nitrate (SG‐75): Comparison with Nitroglycerin and Diltiazem , 1981, Journal of cardiovascular pharmacology.

[9]  K. Sakai,et al.  Development of tolerance and a new coronary vasodilator, N-(2-hydroxyethyl)nicotinamide nitrate (SG-75): A comparison with nitroglycerin. , 1981 .

[10]  N. Taira,et al.  DIFFERENTIAL EFFECTS OF THE CALCIUM‐ANTAGONISTIC VASODILATORS, NIFEDIPINE AND VERAPAMIL, ON THE TRACHEAL MUSCULATURE AND VASCULATURE OF THE DOG , 1980, British journal of pharmacology.

[11]  柳澤 輝行 Effect of 2-nicotinamidethyl nitrate (SG-75) on the membrane potential of left atrial muscle fibres of the dog : increase in potassium conductance , 1980 .

[12]  H. Kamiyama,et al.  Pharmacodynamic and metabolism studies on a new coronary vasodilator, N-(2-hydroxyethyl) nicotinamide nitrate (SG-75). , 1980, Japanese journal of pharmacology.

[13]  S. Imai,et al.  Effects of 2-nicotinamidoethyl nitrate on the cardiovascular system. , 1979, Japanese heart journal.

[14]  Y. Imai,et al.  PHARMACOLOGICAL PROFILE OF A NEW CORONARY VASODILATOR DRUG, 2‐NICOTINAMIDOETHYL NITRATE (SG‐75) , 1979, Clinical and experimental pharmacology & physiology.

[15]  T. Yanagisawa,et al.  Circumstantial evidence for increased potassium conductance of membrane of cardiac muscle by 2-nicotinamidoethyl nitrate (SG-75). , 1979, Japanese journal of pharmacology.

[16]  YANG WANG,et al.  The Rate-Pressure Product as an Index of Myocardial Oxygen Consumption during Exercise in Patients with Angina Pectoris , 1978, Circulation.

[17]  N. Taira,et al.  A METHOD FOR RECORDING SMOOTH MUSCLE AND VASCULAR RESPONSES OF THE BLOOD‐PERFUSED DOG TRACHEA In situ , 1976, British journal of pharmacology.

[18]  The rate of , 2022 .