RELAXING EFFECT OF VESNARINONE (OPC-8212) ON THE TRACHEAL MUSCLE STRIPS ISOLATED FROM GUINEA-PIGS

被引:0
|
作者
TAKEYA, K
ANDO, H
ANDO, S
YAJIMA, M
NOMURA, H
机构
[1] Department of Pharmacology, Aichi Medical University, Aichi 480-11
来源
JAPANESE JOURNAL OF PHARMACOLOGY | 1993年 / 62卷 / 02期
关键词
VESNARINONE; TRACHEAL MUSCLE; CYCLIC AMP;
D O I
10.1254/jjp.62.191
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
The effect of vesnarinone (OPC-8212), an orally active positive inotropic agent was studied in tracheal muscle isolated from guinea pigs, and the mechanism of its action was analyzed. Vesnarinone (10(-6) - 10(-4) M) caused a concentration-dependent relaxation of tracheal muscle pre-contracted by 10(-)4 M histamine. The potency of the relaxing effect of vesnarinone was greater than that of theophylline; the pD2 values for vesnarinone and theophylline were 4.9 and 4.5, respectively. Vesnarinone reduced the high-K+-induced contracture of depolarized tracheal muscle non-competitively (pD'2 = 3.7). Vesnarinone at the low concentration of 3 x 10(-6) M shifted the concentration-response curve for isoproterenol in a parallel fashion to the left. Vesnarinone additively acted on the relaxing effect of isobutyl methyl xanthine. Propranolol (10(-5) M) and reserpine pre-treatment (5 mg/kg, i.p., 24 hr) had no effect on the relaxing effect of vesnarinone. These results suggested that vesnarinone elevated the intracellular cyclic AMP level via phosphodiesterase inhibition, resulting in the tracheal muscle relaxation.
引用
收藏
页码:191 / 197
页数:7
相关论文
共 50 条
  • [21] Effects of rhubarb on isolated gastric muscle strips of guinea pigs
    Yu, Mei
    Luo, Ya-Li
    Zheng, Jun-Wei
    Ding, Yong-Hui
    Li, Wei
    Zheng, Tian-Zhen
    Qu, Song-Yi
    WORLD JOURNAL OF GASTROENTEROLOGY, 2005, 11 (17) : 2670 - 2673
  • [22] INCREASED INVITRO RESPONSES OF TRACHEAL SMOOTH-MUSCLE FROM HYPERRESPONSIVE GUINEA-PIGS
    ISHIDA, K
    PARE, PD
    THOMSON, RJ
    SCHELLENBERG, RR
    JOURNAL OF APPLIED PHYSIOLOGY, 1990, 68 (04) : 1316 - 1320
  • [23] MEDIATION OF PROSTAGLANDIN-E2 IN BIPHASIC RESPONSE TO ATP OF ISOLATED TRACHEAL MUSCLE OF GUINEA-PIGS
    KAMIKAWA, Y
    SHIMO, Y
    JOURNAL OF PHARMACY AND PHARMACOLOGY, 1976, 28 (04) : 294 - 297
  • [24] AFFERENT NERVE-ENDINGS IN THE TRACHEAL MUSCLE OF GUINEA-PIGS AND RATS
    BALUK, P
    GABELLA, G
    ANATOMY AND EMBRYOLOGY, 1991, 183 (01): : 81 - 87
  • [25] Effect of cholecystokinin and secretin on contractile activity of isolated gastric muscle strips in guinea pigs
    Li, W
    Zheng, TZ
    Qu, SY
    WORLD JOURNAL OF GASTROENTEROLOGY, 2000, 6 (01) : 93 - 95
  • [26] Effect of cholecystokinin and secretin on contractile activity of isolated gastric muscle strips in guinea pigs
    Li W
    Zheng TZ
    Qu SY
    World Journal of Gastroenterology, 2000, 6 (01) : 93 - 95
  • [27] Effect of cyclosporin-A on histamine release from tracheal strips of sensitized guinea pigs
    Bovingdon, M
    Assem, ESK
    Wan, BYC
    INFLAMMATION RESEARCH, 1996, 45 : S7 - S8
  • [28] EFFECT OF MODE OF ACTIVATION OF HUMAN EOSINOPHILS ON TRACHEAL SMOOTH-MUSCLE CONTRACTION IN GUINEA-PIGS
    STREK, ME
    WHITE, SR
    HSIEU, TR
    KULP, GVP
    WILLIAMS, FS
    LEFF, AR
    AMERICAN JOURNAL OF PHYSIOLOGY, 1993, 264 (05): : L475 - L481
  • [29] EFFECTS OF VESNARINONE (OPC-8212) ON CA2+-ACTIVATED K-CHANNELS AND CYTOSOLIC CA2+ IN CULTURED SMOOTH-MUSCLE CELLS FROM PORCINE CORONARY-ARTERY
    SAITO, K
    NAKAYA, Y
    MIYOSHI, Y
    WAKATSUKI, T
    NOMURA, M
    SHONO, M
    JAPANESE HEART JOURNAL, 1994, 35 (01): : 61 - 71
  • [30] IMMUNOPHARMACOLOGICAL INVESTIGATIONS ON TRACHEAL SEGMENTS FROM RATS AND GUINEA-PIGS
    MULLER, RKM
    DIETRICH, FM
    EXPERIENTIA, 1975, 31 (06): : 731 - 731