Reduction of Wrap Restraint Stress-Induced Defecation by MKC-242, a Novel Benzodioxan Derivative, via 5-HT_<1A>-Receptor Agonist Action in Rats

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Effects of MKC-242 (5-{3-[((2<I>S</I>)-1, 4-benzodioxan-2-ylmethyl)amino]propoxy}-1, 3-benzodioxole HCl), a novel 5-HT<SUB>1A</SUB>-receptor agonist, and reference compounds on wrap restraint stress-induced defecation were evaluated in rats. Wrapping restraint stress increased defecation in rats. The increase was attenuated by putative 5-HT<SUB>1A</SUB>-receptor agonists, MKC-242 and 8-hydroxy-2-(di-<I>n</I>-propylamino)tetralin (8-OH-DPAT). The suppressive effect of MKC-242 on wrap stress-induced defecation was antagonized by prior administration of a 5-HT<SUB>1A</SUB>-receptor antagonist, WAY100135. MKC-242 did not affect spontaneous defecation and 5-HT-induced defecation. Diazepam and amitriptyline also significantly reduced the stress-induced defecation. However, amitriptyline showed a potent anti-cholinergic effect in the oxotremorine-induced tremor test and reduced spontaneous defecation. In contrast to MKC-242 and 8-OH-DPAT, buspirone and tandospirone tended to suppress the increase at high doses. A major metabolite of buspirone and tandospirone, 1-(2-pyrimidinyl)piperazine, antagonized the suppressive effect of MKC-242. These findings suggest that stimulation of 5-HT<SUB>1A</SUB> receptors reduces stress-induced defecation but not spontaneous and 5-HT-induced defecation and that MKC-242 may be useful for the treatment of irritable bowel syndrome.

収録刊行物

  • The Japanese journal of pharmacology

    The Japanese journal of pharmacology 77(3), 211-217, 1998-07-01

    The Japanese Pharmacological Society

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各種コード

  • NII論文ID(NAID)
    10008193202
  • NII書誌ID(NCID)
    AA00691188
  • 本文言語コード
    ENG
  • 資料種別
    ART
  • ISSN
    00215198
  • NDL 記事登録ID
    4525737
  • NDL 雑誌分類
    ZS51(科学技術--薬学)
  • NDL 請求記号
    Z53-D199
  • データ提供元
    CJP書誌  NDL  J-STAGE 
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