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Comparison of Inodilator Effect of Higenamine, YS49, YS51, Tetrahydroisoquinoline Analogs, and Dobutamine in the Rat

Chong, Won-Seog   (Department of Pharmacology, Cardiovascular Research Institute, College of Medicine, Gyeongsang National UniversityUU0000114  ); Lee, Young-Soo   (Department of Pharmacology, Cardiovascular Research Institute, College of Medicine, Gyeongsang National UniversityUU0000114  ); Kang, Young-Jin   (Department of Pharmacology, Cardiovascular Research Institute, College of Medicine, Gyeongsang National UniversityUU0000114  ); Lee, Duck-Hyung   (Department of Chemistry, Sogang UniversityUU0000674  ); Ryu, Jae-Chun   (Doping Control Center, Korea Institute of Science and TechnologyCC0186926  ); Yun-Choi, Hye-Sook   (Natural Product Research Institute, Seoul National UniversityUU0000691  ); Chang, Ki-Churl   (Department of Pharmacology, Cardiovascular Research Institute, College of Medicine, Gyeongsang National UniversityUU0000114  );
  • 초록

    Tetrahydroisoquinoline (THI) alkaloids can be considered as cyclized derivatives of simple phenylethylamines. Many of them, especially with 6,7-disubstitution, demonstrate a relatively high affinity for catecholamines. Present study examines the pharmacological action of limited series of THI, using rats' isolated atria and aorta. In addition, a $[^3H]$ prazosin displacement binding study with THI compounds was performed, using rat brain homogenates to investigate whether these probes have ? ${\alpha}$ -adrenoceptor affinity. We also compared the vascular relaxation potency of these probes with dobutamine. YS 49, YS 51, higenamine and dobutamine, concentration-dependently, relaxed endothelium-denuded rat thoracic aorta precontracted with phenylephrine (PE, 0.1 ${\mu}M$ ) in which $pEC_{50}$ were $5.56{\pm}0.32$ and $5.55{\pm}0.21$ , $5.99{\pm}1.16$ and $5.57{\pm}0.34$ , respectively. These probes except higenamine also relaxed KCl (65.4 mM)-contracted aorta. In isolated rat atria, all THIs and dobutamine increased heart rate and contractile force. In the presence of propranolol, the concentration response curves of YS 49 and YS 51 shifted to the right and resulted in $pA_2$ values of $8.07{\pm}0.84$ and $7.93{\pm}0.11$ , respectively. The slope of each compound was not deviated from unity, indicating that these chemicals are highly competitive at the cardiac ? ${\beta}-adrenoceptors$ . YS 49, YS 51, and higenamine showed ? ${\alpha)-adrenoceptor$ affinity in rat brain, in which the dissociation constant $(K_i)$ was 2.75, 2.81, and 1.02 ${\mu}M$ , respectively. It is concluded, therefore, that THI alkaloids have weak affinity to ${\alpha)_1-adrenoceptor$ in rat aorta and brain, respectively, while these probes show relatively high affinity for cardiac ${\beta}-adrenoceptors$ . Thus, these chemicals may be useful in the treatment of congestive heart failure.


  • 주제어

    Tetrahydroisoquinoline .   Inotropic action .   Vasodilatation .   Rat .   Adrenoceptor.  

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  • 정원석 (5)

    1. 1991 "GS354, GS389: 새로운 칼슘 길항제" The Korean journal of pharmacology : official journal of the Society of Pharmacology, Republic of Korea 27 (1): 45~52    
    2. 1993 "Nortriptyline 청소율과 Metoprolol 산화대사능과의 상관관계" 臨床藥理學會誌 = The journal of Korean society for Clinical Pharmacology and Therapeutics 1 (2): 148~154    
    3. 1994 "GS 283의 평활근 억제 작용기전" The Korean journal of pharmacology : official journal of the Society of Pharmacology, Republic of Korea 30 (1): 101~109    
    4. 1994 "동맥경화 예방과 치료를 위한 연구시도: Nitric Oxide의 역활 -광 유도 nitric oxide(PIANO)의 혈관이완에 따른 cyclic GMP의 증가" The Korean journal of pharmacology : official journal of the Society of Pharmacology, Republic of Korea 30 (3): 331~336    
    5. 1998 "Pharmacological Characterization of Synthetic Tetrahydroisoquinoline Alkaloids, YS 51 and YS 55, on the Cardiovascular System" The Korean journal of physiology & pharmacology : official journal of the Korean Physiological Society and the Korean Society of Pharmacology 2 (4): 461~469    
  • 이영수 (10)

  • Lee, Duck-Hyung (1)

  • 류재천 (87)

  • Chang, Ki-Churl (26)

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