Novel psychoactive benzofurans strongly increase extracellular serotonin level in mouse corpus striatum
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- Fuwa Tatsu
- Department of Pharmaceutical and Environmental Sciences, Tokyo Metropolitan Institute of Public Health
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- Suzuki Jin
- Department of Pharmaceutical and Environmental Sciences, Tokyo Metropolitan Institute of Public Health
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- Tanaka Toyohito
- Department of Pharmaceutical and Environmental Sciences, Tokyo Metropolitan Institute of Public Health
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- Inomata Akiko
- Department of Pharmaceutical and Environmental Sciences, Tokyo Metropolitan Institute of Public Health
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- Honda Yoshiko
- Laboratory of Physiological Psychology, Tokyo Metropolitan Institute of Medical Science
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- Kodama Tohru
- Laboratory of Physiological Psychology, Tokyo Metropolitan Institute of Medical Science
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説明
We examined the effects of three benzofurans [1-(Benzofuran-5-yl)-N-methylpropan-2-amine (5-MAPB), 1-(Benzofuran-2-yl)-N-methylpropan-2-amine (2-MAPB), and 1-(Benzofuran-5-yl)-N-ethylpropan-2-amine (5-EAPB)] on the extracellular monoamine level in mouse corpus striatum by the microdialysis method and compared them with the effects of psychoactive 3,4-Methylenedioxymethamphetamine (MDMA). The effects of benzofurans on the extracellular monoamine level were qualitatively analogous to that of MDMA, with an increase in serotonin (5-HT) level exceeding dopamine (DA) level. The effects of 2-MAPB and 5-EAPB were almost the same as the effect of MDMA. However, 5-MAPB strongly increased extracellular monoamine level than MDMA. These differences in the potency appear to have a structure-activity relationship. The administration of 5-MAPB (1.6 × 10-4 mol/kg B.W.) resulted in the death of two-thirds of the mice. The same dose of MDMA did not cause any deaths. The administration of 5-MAPB (1.6 × 10-4 mol/kg B.W.) produced a 3.41°C ± 0.28°C rise in rectal temperature after 1 hr, whereas the administration of MDMA (1.6 × 10-4 mol/kg B.W.) produced an approximate 1.85°C ± 0.26°C rise. These results suggest that benzofurans have 5-HT toxicity similar to MDMA, and 5-MAPB has a higher risk of lethal intoxication than MDMA. Furthermore, 5-APB, the metabolic product of 5-MAPB demethylation, may be involved in the acute 5-HT toxicity and may cause lethal intoxication in mice.
収録刊行物
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- The Journal of Toxicological Sciences
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The Journal of Toxicological Sciences 41 (3), 329-337, 2016
一般社団法人 日本毒性学会
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詳細情報 詳細情報について
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- CRID
- 1390001204906760064
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- NII論文ID
- 130005152351
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- NII書誌ID
- AN00002808
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- ISSN
- 18803989
- 03881350
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- NDL書誌ID
- 027467058
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- PubMed
- 27193726
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- 本文言語コード
- en
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- データソース種別
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- JaLC
- NDL
- Crossref
- PubMed
- CiNii Articles
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- 使用不可