PMID- 37600151
OWN - NLM
STAT- PubMed-not-MEDLINE
LR  - 20230823
IS  - 2772-7246 (Electronic)
IS  - 2772-7246 (Linking)
VI  - 8
DP  - 2023 Sep
TI  - Locomotor and discriminative stimulus effects of three benzofuran compounds in 
      comparison to abused psychostimulants.
PG  - 100182
LID - 10.1016/j.dadr.2023.100182 [doi]
LID - 100182
AB  - AIMS: Benzofurans are used recreationally, due their ability to cause 
      psychostimulant and/or entactogenic effects, but unfortunately produce 
      substantial adverse effects, including death. Three benzofurans 
      5-(2-aminopropyl)-2,3-dihydrobenzofuran (5-APDB), 
      5-(2-aminopropyl)-2,3-dihydrobenzofuran (5-MAPB) and 6-(2-aminopropyl) benzofuran 
      (6-APB) were tested to determine their behavioral effects in comparison with 
      2,3-methylenedioxymethamphetamine (MDMA), cocaine, and methamphetamine. METHODS: 
      Locomotor activity was tested in groups of 8 male Swiss-Webster mice in an 
      open-field task to screen for locomotor stimulant or depressant effects and to 
      identify behaviorally active doses and times of peak effect. Discriminative 
      stimulus effects were tested in groups of 6 male Sprague-Dawley rats trained to 
      discriminate MDMA (1.5 mg/kg), cocaine (10 mg/kg), or methamphetamine (1 mg/kg) 
      from saline using a FR 10 for food in a two-lever operant task. RESULTS: In the 
      locomotor activity test, MDMA (ED(50) = 8.34 mg/kg) produced peak stimulant 
      effects 60 to 80 min following injection. 5-MAPB (ED(50) = 0.92 mg/kg) produced 
      modest stimulant effects 50 to 80 min after injection, whereas 6-APB 
      (ED(50) = 1.96 mg/kg) produced a robust stimulant effect 20 to 50 min after 
      injection. 5-APDB produced an early depressant phase (ED(50) = 3.38 mg/kg) 
      followed by a modest stimulant phase (ED(50) = 2.57 mg/kg) 20 to 50 min after 
      injection. In the drug discrimination tests, 5-APDB (ED(50) = 1.02 mg/kg), 5-MAPB 
      (ED(50) = 1.00 mg/kg) and 6-APB (ED(50) = 0.32 mg/kg) fully substituted in 
      MDMA-trained rats, whereas only 5-MAPB fully substituted for cocaine, and no 
      compounds fully substituted for methamphetamine. CONCLUSIONS: The synthetic 
      benzofuran compound 5-APDB and 5-MAPB produced weak locomotor effects, whereas 
      6-APB produced robust locomotor stimulant effects. All compounds were more potent 
      than MDMA. All three compounds fully substituted in MDMA-trained rats suggesting 
      similar subjective effects. Taken together, these results suggest that these 
      benzofuran compounds may have abuse liability as substitutes for MDMA.
CI  - (c) 2023 The Author(s).
FAU - Hill, Rebecca D
AU  - Hill RD
AD  - University of North Texas Health Science Center, Department of Pharmacology and 
      Neuroscience, 3500 Camp Bowie Blvd, Fort Worth, TX 76109, United States.
FAU - Shetty, Ritu A
AU  - Shetty RA
AD  - University of North Texas Health Science Center, Department of Pharmacology and 
      Neuroscience, 3500 Camp Bowie Blvd, Fort Worth, TX 76109, United States.
FAU - Sumien, Nathalie
AU  - Sumien N
AD  - University of North Texas Health Science Center, Department of Pharmacology and 
      Neuroscience, 3500 Camp Bowie Blvd, Fort Worth, TX 76109, United States.
FAU - Forster, Michael J
AU  - Forster MJ
AD  - University of North Texas Health Science Center, Department of Pharmacology and 
      Neuroscience, 3500 Camp Bowie Blvd, Fort Worth, TX 76109, United States.
FAU - Gatch, Michael B
AU  - Gatch MB
AD  - University of North Texas Health Science Center, Department of Pharmacology and 
      Neuroscience, 3500 Camp Bowie Blvd, Fort Worth, TX 76109, United States.
LA  - eng
PT  - Journal Article
DEP - 20230805
PL  - Netherlands
TA  - Drug Alcohol Depend Rep
JT  - Drug and alcohol dependence reports
JID - 9918350383506676
PMC - PMC10432784
OTO - NOTNLM
OT  - Cocaine
OT  - Drug discrimination
OT  - MDMA
OT  - Methamphetamine
OT  - Rats
COIS- The authors declare the following financial interests/personal relationships 
      which may be considered as potential competing interests: Michael J. Forster 
      reports financial support was provided by National Institute on Drug Abuse 
      Division of Therapeutics and Medical Consequences.
EDAT- 2023/08/21 06:42
MHDA- 2023/08/21 06:43
PMCR- 2023/08/05
CRDT- 2023/08/21 04:41
PHST- 2022/12/29 00:00 [received]
PHST- 2023/07/15 00:00 [revised]
PHST- 2023/08/03 00:00 [accepted]
PHST- 2023/08/21 06:43 [medline]
PHST- 2023/08/21 06:42 [pubmed]
PHST- 2023/08/21 04:41 [entrez]
PHST- 2023/08/05 00:00 [pmc-release]
AID - S2772-7246(23)00052-5 [pii]
AID - 100182 [pii]
AID - 10.1016/j.dadr.2023.100182 [doi]
PST - epublish
SO  - Drug Alcohol Depend Rep. 2023 Aug 5;8:100182. doi: 10.1016/j.dadr.2023.100182. 
      eCollection 2023 Sep.