PMID- 27193726
OWN - NLM
STAT- MEDLINE
DCOM- 20170410
LR  - 20170410
IS  - 1880-3989 (Electronic)
IS  - 0388-1350 (Linking)
VI  - 41
IP  - 3
DP  - 2016
TI  - Novel psychoactive benzofurans strongly increase extracellular serotonin level in 
      mouse corpus striatum.
PG  - 329-37
LID - 10.2131/jts.41.329 [doi]
AB  - 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 x 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 x 10(-4) mol/kg 
      B.W.) produced a 3.41 degrees C +/- 0.28 degrees C rise in rectal temperature after 1 hr, whereas 
      the administration of MDMA (1.6 x 10(-4) mol/kg B.W.) produced an approximate 
      1.85 degrees C +/- 0.26 degrees 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.
FAU - Fuwa, Tatsu
AU  - Fuwa T
AD  - Department of Pharmaceutical and Environmental Sciences, Tokyo Metropolitan 
      Institute of Public Health.
FAU - Suzuki, Jin
AU  - Suzuki J
FAU - Tanaka, Toyohito
AU  - Tanaka T
FAU - Inomata, Akiko
AU  - Inomata A
FAU - Honda, Yoshiko
AU  - Honda Y
FAU - Kodama, Tohru
AU  - Kodama T
LA  - eng
PT  - Comparative Study
PT  - Journal Article
PL  - Japan
TA  - J Toxicol Sci
JT  - The Journal of toxicological sciences
JID - 7805798
RN  - 0 (Benzofurans)
RN  - 0 (Psychotropic Drugs)
RN  - 333DO1RDJY (Serotonin)
RN  - KE1SEN21RM (N-Methyl-3,4-methylenedioxyamphetamine)
RN  - VTD58H1Z2X (Dopamine)
RN  - X4W3ENH1CV (Norepinephrine)
SB  - IM
MH  - Animals
MH  - Benzofurans/chemistry/metabolism/*toxicity
MH  - Biotransformation
MH  - Body Temperature Regulation/drug effects
MH  - Corpus Striatum/*drug effects/metabolism
MH  - Dealkylation
MH  - Dopamine/metabolism
MH  - Dose-Response Relationship, Drug
MH  - Male
MH  - Mice
MH  - Molecular Structure
MH  - N-Methyl-3,4-methylenedioxyamphetamine/toxicity
MH  - Norepinephrine/metabolism
MH  - Psychotropic Drugs/chemistry/metabolism/*toxicity
MH  - Serotonin/*metabolism
MH  - Structure-Activity Relationship
MH  - Time Factors
MH  - Up-Regulation
EDAT- 2016/05/20 06:00
MHDA- 2017/04/11 06:00
CRDT- 2016/05/20 06:00
PHST- 2016/05/20 06:00 [entrez]
PHST- 2016/05/20 06:00 [pubmed]
PHST- 2017/04/11 06:00 [medline]
AID - 10.2131/jts.41.329 [doi]
PST - ppublish
SO  - J Toxicol Sci. 2016;41(3):329-37. doi: 10.2131/jts.41.329.