Effect of 5-{3-(((2S)-1,4-Benzodioxan-2-ylmethyl)amino)propoxy}-1,3-benzodioxole HCl (MKC-242), a Novel 5-HT1A-Receptor Agonist, on Aggressive Behavior and Marble Burying Behavior in Mice.
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- Abe Michikazu
- Pharmaceuticals Laboratory I, Yokohama Research Center, Mitsubishi Chemical Corporation
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- Nakai Hiroshi
- Pharmacokinetics and Metabolism Research Laboratory, Yokohama Research Center, Mitsubishi Chemical Corporation
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- Tabata Reiko
- Pharmaceuticals Laboratory I, Yokohama Research Center, Mitsubishi Chemical Corporation
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- Saito Ken-Ichi
- Pharmaceuticals Laboratory I, Yokohama Research Center, Mitsubishi Chemical Corporation
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- Egawa Mitsuo
- Clinical Research Department, Mitsubishi Chemical Corporation
Bibliographic Information
- Other Title
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- Effect of 5 3 2S 1 4 Benzodioxan 2 ylme
- Effect of 5-{3-[((2S)-l,4-Benzodioxan-2-ylmethyl)amino]propoxy}-1,3-benzodioxole HCl (MKC-242), a Novel 5-HT1A-Receptor Agonist, on Aggressive Behavior and Marble Burying Behavior in Mice
- Effect of 5-{3-[((25)-1,4-benzodioxan-2-ylmethyl)amino]propoxy}-1,3-benzodioxole HCl (MKC-242), a novel 5-HT!A-receptor agonist, on aggressive behavior and marble burying behavior in mice
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Abstract
Behavioral effects of 5-{3-[((2S)-1, 4-benzodioxan-2-ylmethyl)amino]propoxy}-1, 3-benzodioxole HCl (MKC-242), a novel 5-HT1A-receptor agonist, were evaluated using animal models of anxiety and obsessive compulsive disorder and compared against reference compounds. MKC-242 suppressed foot shock-induced fighting behavior without loss of motor coordination in mice as the reference compounds did. The ED50 values of MKC-242, buspirone, tandospirone and diazepam were 1.7, 42, 80 and 2.0 mg/kg, p.o., respectively. The duration of the suppression of fighting by MKC-242 was longer than those of buspirone and tandospirone and comparable to that of diazepam. Similar results were also obtained with the water-lick conflict test in rats. The plasma concentration of MKC-242 in rats was much higher than the reported value of buspirone during 0.25 – 6 hr after oral administration. In addition, MKC-242 reduced marble burying behavior without reduction of motor activity. Fluoxetine, tandospirone and diazepam also reduced the behavior at non-sedative doses. These findings indicate that MKC-242 possesses a longer-lasting anxiolytic effect than azapirones. This might be due to the high concentration of the compound in plasma. In addition, it is also suggested that MKC-242 possesses an antiobsessional effect.
Journal
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- The Japanese Journal of Pharmacology
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The Japanese Journal of Pharmacology 76 (3), 297-304, 1998
The Japanese Pharmacological Society
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Details 詳細情報について
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- CRID
- 1390001204284857856
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- NII Article ID
- 10008192063
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- NII Book ID
- AA00691188
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- COI
- 1:CAS:528:DyaK1cXitFCiu7Y%3D
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- ISSN
- 13473506
- 00215198
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- NDL BIB ID
- 4440449
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- PubMed
- 9593223
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- Web Site
- https://ndlsearch.ndl.go.jp/books/R000000004-I4440449
- https://api.elsevier.com/content/article/PII:S0021519819312077?httpAccept=text/xml
- https://api.elsevier.com/content/article/PII:S0021519819312077?httpAccept=text/plain
- https://www.jstage.jst.go.jp/article/jjp/76/3/76_3_297/_pdf
- https://search.jamas.or.jp/link/ui/1998174777
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- Text Lang
- en
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- Data Source
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- JaLC
- NDL
- Crossref
- PubMed
- CiNii Articles
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- Abstract License Flag
- Disallowed