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

スポンサーリンク

概要

• 論文の詳細を見る

• Effects of MKC-242 (5-｛3-[((2S)-1, 4-benzodioxan-2-ylmethyl)amino]propoxy｝-1, 3-benzodioxole HCl), a novel 5-HT1A-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-HT1A-receptor agonists, MKC-242 and 8-hydroxy-2-(di-n-propylamino)tetralin (8-OH-DPAT). The suppressive effect of MKC-242 on wrap stress-induced defecation was antagonized by prior administration of a 5-HT1A-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-HT1A 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.

• 社団法人 日本薬理学会の論文
• 1998-07-01

著者

• ABE Michikazu

  Pharmacology Department IV, Mitsubishi Tanabe Pharma Co.

• SAITO Ken-ichi

  Pharmaceuticals Laboratory, Research Center, Mitsubishi Kasei Co.

• Abe Michikazu

  Pharmaceutical Laboratory I Yokohama Research Center Mitsubishi Chemical Corporation

• Saito Ken-ichi

  Pharmaceuticals Laboratory I Yokohama Research Center Mitsubishi Chemical Corporation

関連論文

• Inhibitory Effects of Osemozotan, a Serotonin 1A-Receptor Agonist, on Methamphetamine-Induced c-Fos Expression in Prefrontal Cortical Neurons(Pharmacology)
• An Antihyperkinetic Action by the Serotonin 1A-Receptor Agonist Osemozotan Co-administered With Psychostimulants or the Non-stimulant Atomoxetine in Mice
• Interaction of Orally Administered 5-{3-[((2S)-1,4-Benzodioxan-2-ylmethyl)amino]propoxy} - 1,3-benzodioxole (MKC-242)with 5-HT_ Receptors in Rat Brain
• AGONIST ACTIVITY OF A NOVEL COMPOUND, BP-554,AT CENTRAL SEROTONIN-1A RECEPTORS
• Reduction of Wrap Restraint Stress-Induced Defecation by MKC-242, a Novel Benzodioxan Derivative, via 5-HT_-Receptor Agonist Action in Rats
• Effect of 5-{3-[((2S)-1,4-Benzodioxan-2-ylmethyl)amino]propoxy}-1,3-benzodioxole HCl (MKC-242), a Novel 5-HT_-Receptor Agonist, on Aggressive Behavior and Marble Burying Behavior in Mice
• An Antihyperkinetic Action by the Serotonin 1A–Receptor Agonist Osemozotan Co-administered With Psychostimulants or the Non-stimulant Atomoxetine in Mice

スポンサーリンク