Folia Pharmacologica Japonica
Online ISSN : 1347-8397
Print ISSN : 0015-5691
ISSN-L : 0015-5691
Volume 97, Issue 3
Displaying 1-5 of 5 articles from this issue
  • Yasuo TAKAHASHI
    1991 Volume 97 Issue 3 Pages 135-144
    Published: 1991
    Released on J-STAGE: February 13, 2007
    JOURNAL FREE ACCESS
    There are some functionally important proteins in the central nervous system. We have studied some of these proteins and analyzed the structure and function of their genes and mRNAs. In this review, we briefly described the present state of the studies on 14-3-3 protein, GABA receptor and dopamine receptor from the standpoint of cDNA and genomic DNA analyses. Particularly, we have emphasized the function, heterogeneity, primary structures, nucleotide sequences, gene structures and the distribution of these proteins and mRNAs in the central nervous system.
    Download PDF (8937K)
  • Kiyoshi WATANABE, Yutaka HAYASHI, Kenro IKEDA, Haruo OHNISHI
    1991 Volume 97 Issue 3 Pages 145-151
    Published: 1991
    Released on J-STAGE: February 13, 2007
    JOURNAL FREE ACCESS
    Effect of moxisylyte on the lower urinary tracts was studied in comparison with those of prazosin and bunazosin in the isolated rabbit bladder and urethra. Moxisylyte dose-dependently inhibited the urethral contraction induced by phenylephrine. The IC50 value of moxisylyte was 1.01 ×: 10-6 M. Prazosin and bunazosin inhibited the urethral contraction as well as moxisylyte. The IC50 values of prazosin and bunazosin were 2.88 ×: 10-7 M and 1.44 ×: 10-7 M, respectively. Moreover, moxisylyte and bunazosin inhibited the urethral contraction induced by KCI. The IC50 values of moxisylyte and bunazosin were 1.17 ×: 10-5 M and 1. 35 ×: 10-4M, respectively. The KCl/phenylephrine ratios of moxisylyte, bunazosin and prazosin were as follows: 17, 938 and 9201, respectively. Moxisylyte has a relaxant action on the urethra that is probably ascribable to its al-adrenoceptor antagonist and Ca++ antagonist actions. In the isolated bladder, moxisylyte inhibited the bladder contraction induced by KCl, with an IC50 value of 4.46 ×: 10-5 M. However, moxisylyte did not affect the contractile response to acetylcholine. These results suggest that the relaxant effect of moxisylyte on the urethra is due to α1-adrenoceptor antagonist and Ca++ antagonist actions. Therefore, moxisylyte is useful for the therapeutic treatment of micturitional disorder.
    Download PDF (4674K)
  • Kiyoshi WATANABE, Yutaka HAYASHI, Kenro IKEDA, Haruo OHNISHI
    1991 Volume 97 Issue 3 Pages 153-165
    Published: 1991
    Released on J-STAGE: February 13, 2007
    JOURNAL FREE ACCESS
    Effect of moxisylyte on the lower urinary tracts was studied with the urethral pressure profile (UPP) and balloon method in anesthetized female dogs. In the UPP, moxisylyte produced relaxation in both the proximal and distal urethras. The relaxation effects of prazosin and bunazosin on the distal urethra was weaker than on the proximal urethra. In the balloon method, moxisylyte, prazosin, bunazosin and phentolamine caused a decrease in urethral pressure dose-dependently. The ID25 values of moxisylyte, prazosin, bunazosin and phentolamine were 23.4, 0.43, 0.76 and 33.1 μg/kg, respectively. In the balloon method, moxisylyte noncompetitively antagonized phenylephrine induced contraction of the urethra at high doses, whereas prazosin, bunazosin, phentolamine and yohimbine competitively antagonized phenylephrine induced contraction of the urethra. These results suggest that moxisylyte relaxes both the proximal and distal urethras due to α1-adrenoceptor antagonistic and direct urethral smooth muscle relaxant actions. Therefore, moxisylyte is useful for the therapeutic treatment of micturitional disorder.
    Download PDF (7929K)
  • Kyozo YAMANAKA, Makoto SUZUKI, Shiro MUNEHASU, Jun-ichi ISHIKO
    1991 Volume 97 Issue 3 Pages 167-178
    Published: 1991
    Released on J-STAGE: February 13, 2007
    JOURNAL FREE ACCESS
    Amlodipine (AML), a new 1, 4-dihydropyridine derivative, similar to nifedipine (NIF), dosedependently relaxed or inhibited the KCl-contraction (cont.) of dog coronary artery (DCA) and rat aorta (RA) and the spontaneous motility of rat portal vein (RPV). However, in contrast to the case of NIF, the maximum effect was obtained at 1-2 hr following an addition of AML, and the recovery of KCl-cont. after removal of AML was very slow. Similar effects of AML on KCl-cont. were observed in dog femoral artery (DFA), dog basilar artery (DBA) and rabbit aorta (RBA). The IC50 values of AML for producing the half-maximal effect were 6.5 × 10-9 M, 6.5 ×: 10-9 M, 1.1 ×: 10-8 M, 1.7 ×: 10-8 M and 4.8 ×: 10-8 M in DCA, DFA, RPV, DBA and RBA, respectively. In these vessels, the potency of AML was slightly less than the potency of NIF. On the other hand, AML (10-7, 10-6 M) only slightly attenuated norepinephrine (NE) -induced cont. in DFA and RA. Based on the ratio of IC50 values in DFA, AML exhibited 846-fold higher selectivity toward KCl-cont. than NE-cont., and it was much higher than the selectivity of NIF. In calcium-free medium, AML failed to inhibit the NE-cont. in RA, but it markedly inhibited CaCl2-induced cont. These results indicate that AML significantly inhibits KCl-cont. in blood vessels at lower doses with slightly less potency than NIF, but with a higher selectivity than NIF in comparison with the potency against NE-cont., and they also confirmed that the effect of AML is of slow onset and long-lasting.
    Download PDF (7384K)
  • [in Japanese]
    1991 Volume 97 Issue 3 Pages 179-182
    Published: 1991
    Released on J-STAGE: February 13, 2007
    JOURNAL FREE ACCESS
    Download PDF (2280K)
feedback
Top