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OtherCARDIOVASCULAR PHARMACOLOGY

Structure-Activity Relationships of Spontaneous Nitric Oxide Releasers, FK409 and its Derivatives

Shinichi Fukuyama, Yoshimi Hirasawa, Yasuko Kato, Mie Nishio, Mitsuko Ohno, Shigetaka Nishino, Kazuhiro Maeda, Masayuki Kato and Yasuhiro Kita
Journal of Pharmacology and Experimental Therapeutics July 1997, 282 (1) 236-242;
Shinichi Fukuyama
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Yoshimi Hirasawa
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Yasuko Kato
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Mie Nishio
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Mitsuko Ohno
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Shigetaka Nishino
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Kazuhiro Maeda
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Masayuki Kato
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Yasuhiro Kita
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Abstract

(±)-(E)-4-Ethyl-2-[(E)-hydroxyimino] - 5 - nitro-3-hexenamide (FK409) shows both potent in vitro vasorelaxant and antiplatelet activities via nitric oxide (NO) generated spontaneously from the compound. In this study, we measured spontaneous NO-releasing rates of a series of FK409 derivatives, of which chain lengths or substituents were systematically modified, in sodium-phosphate buffer solution at pH 7.4. Furthermore, we studied their in vitro antiplatelet and vasorelaxant effects to evaluate relationships between spontaneous NO-releasing activities of FK409 analogs and their biological activities. FK409 derivatives were found to possess different spontaneous NO-releasing rates and biological activities according to their structural modification. In addition, these studies revealed a close correlation between NO-releasing rates of FK409 derivatives and their in vitro antiplatelet activities in human platelet-rich plasma, whereas the in vitro vasorelaxant activities of these compounds in isolated rat aorta did not correlate with the rates of NO liberation. The vasorelaxant effects were supposed to be affected by the structural properties of FK409 derivatives as well as their NO-releasing abilities.

Footnotes

  • Send reprint requests to: Dr. Yasuhiro Kita, Exploratory Research Laboratories, Fujisawa Pharmaceutical Co., Ltd., 5-2-3, Tokodai, Tsukuba, Ibaraki 300-26, Japan.

  • Abbreviations:
    FK409
    (±)-(E)-4-ethyl-2-[(E)-hydroxyimino]-5-nitro-3-hexenamide
    NO
    nitric oxide
    PB
    sodium-phosphate buffer
    ADP
    adenosine-5′-diphosphate
    cGMP
    guanosine 3′:5′-cyclic monophosphate
    NMR
    nuclear magnetic resonance
    ESR
    electron spin resonance
    SNP
    sodium nitroprusside
    ISDN
    isosorbide dinitrate
    DMSO
    dimethylsulfoxide
    carboxy-PTIO
    2-(4-carboxyphenyl)-4,4,5,5-tetramethylimidazoline-1-oxyl-3-oxide
    • Received August 26, 1996.
    • Accepted March 12, 1997.
  • The American Society for Pharmacology and Experimental Therapeutics
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Journal of Pharmacology and Experimental Therapeutics
Vol. 282, Issue 1
1 Jul 1997
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OtherCARDIOVASCULAR PHARMACOLOGY

Structure-Activity Relationships of Spontaneous Nitric Oxide Releasers, FK409 and its Derivatives

Shinichi Fukuyama, Yoshimi Hirasawa, Yasuko Kato, Mie Nishio, Mitsuko Ohno, Shigetaka Nishino, Kazuhiro Maeda, Masayuki Kato and Yasuhiro Kita
Journal of Pharmacology and Experimental Therapeutics July 1, 1997, 282 (1) 236-242;

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OtherCARDIOVASCULAR PHARMACOLOGY

Structure-Activity Relationships of Spontaneous Nitric Oxide Releasers, FK409 and its Derivatives

Shinichi Fukuyama, Yoshimi Hirasawa, Yasuko Kato, Mie Nishio, Mitsuko Ohno, Shigetaka Nishino, Kazuhiro Maeda, Masayuki Kato and Yasuhiro Kita
Journal of Pharmacology and Experimental Therapeutics July 1, 1997, 282 (1) 236-242;
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