PMID- 28537942
OWN - NLM
STAT- MEDLINE
DCOM- 20180126
LR  - 20231213
IS  - 1473-5849 (Electronic)
IS  - 0955-8810 (Print)
IS  - 0955-8810 (Linking)
VI  - 28
IP  - 5
DP  - 2017 Aug
TI  - Locomotor and discriminative stimulus effects of four novel hallucinogens in 
      rodents.
PG  - 375-385
LID - 10.1097/FBP.0000000000000309 [doi]
AB  - There has been increasing use of novel synthetic hallucinogenic compounds, 
      2-(4-bromo-2,5-dimethoxyphenyl)-N-(2-methoxybenzyl)ethanamine hydrochloride 
      (25B-NBOMe), 2-(4-chloro-2,5-dimethoxyphenyl)-N-(2-methoxybenzyl)ethanamine 
      hydrochloride (25C-NBOMe), 
      2-(4-iodo-2,5-dimethoxyphenyl)-N-(2-methoxybenzyl)ethanamine hydrochloride 
      (25I-NBOMe), and N,N-diallyl-5-methoxy tryptamine (5-MeO-DALT), which have been 
      associated with severe toxicities. These four compounds were tested for 
      discriminative stimulus effects similar to a prototypical hallucinogen 
      (-)-2,5-dimethoxy-4-methylamphetamine (DOM) and the entactogen 
      (+/-)-3,4-methylenedioxymethamphetamine (MDMA). Locomotor activity in mice was 
      tested to obtain dose range and time-course information. 25B-NBOMe, 25C-NBOMe, 
      and 25I-NBOMe decreased locomotor activity. 5-MeO-DALT dose dependently increased 
      locomotor activity, with a peak at 10 mg/kg. A higher dose (25 mg/kg) suppressed 
      activity. 25B-NBOMe fully substituted (>/=80%) in both DOM-trained and MDMA-trained 
      rats at 0.5 mg/kg. However, higher doses produced much lower levels of 
      drug-appropriate responding in both DOM-trained and MDMA-trained rats. 25C-NBOMe 
      fully substituted in DOM-trained rats, but produced only 67% drug-appropriate 
      responding in MDMA-trained rats at doses that suppressed responding. 25I-NBOMe 
      produced 74-78% drug-appropriate responding in DOM-trained and MDMA-trained rats 
      at doses that suppressed responding. 5-MeO-DALT fully substituted for DOM, but 
      produced few or no MDMA-like effects. All of the compounds, except 25I-NBOMe, 
      fully substituted for DOM, whereas only 25B-NBOMe fully substituted for MDMA. 
      However, the failure of 25I-NBOMe to fully substitute for either MDMA or DOM was 
      more likely because of its substantial rate-depressant effects than weak 
      discriminative stimulus effects. All of the compounds are likely to attract 
      recreational users for their hallucinogenic properties, but probably of much less 
      interest as substitutes for MDMA. Although no acute adverse effects were observed 
      at the doses tested, the substantial toxicities reported in humans, coupled with 
      the high likelihood for illicit use, suggests that these compounds have the same 
      potential for abuse as other, currently scheduled compounds.
FAU - Gatch, Michael B
AU  - Gatch MB
AD  - Department of Pharmacology and Neuroscience, University of North Texas Health 
      Science Center, Fort Worth, Texas, USA.
FAU - Dolan, Sean B
AU  - Dolan SB
FAU - Forster, Michael J
AU  - Forster MJ
LA  - eng
GR  - HHSN271201300001C/DA/NIDA NIH HHS/United States
GR  - T32 AG020494/AG/NIA NIH HHS/United States
PT  - Journal Article
PL  - England
TA  - Behav Pharmacol
JT  - Behavioural pharmacology
JID - 9013016
RN  - 0 (Anisoles)
RN  - 0 (Benzylamines)
RN  - 0 (Dimethoxyphenylethylamine)
RN  - 0 (Hallucinogens)
RN  - 0 (Phenethylamines)
RN  - 15588-95-1 (DOM 2,5-Dimethoxy-4-Methylamphetamine)
RN  - 547KGL06IP (2-(4-iodo-2,5-dimethoxyphenyl)-N-(2-methoxybenzyl)ethanamine)
RN  - 9FGW3C260N 
      (2-(4-chloro-2,5-dimethoxyphenyl)-N-((2-methoxyphenyl)methyl)ethanamine)
RN  - KE1SEN21RM (N-Methyl-3,4-methylenedioxyamphetamine)
RN  - S6NAA81PHK 
      (2-(4-bromo-2,5-dimethoxyphenyl)-N-((2-methoxyphenyl)methyl)ethanamine)
SB  - IM
MH  - DOM 2,5-Dimethoxy-4-Methylamphetamine/pharmacology
MH  - Animals
MH  - Anisoles/metabolism/*pharmacology
MH  - Benzylamines/metabolism/*pharmacology
MH  - Dimethoxyphenylethylamine/*analogs & derivatives/metabolism/pharmacology
MH  - Hallucinogens/metabolism/pharmacology
MH  - Locomotion/drug effects
MH  - Male
MH  - Mice
MH  - N-Methyl-3,4-methylenedioxyamphetamine/pharmacology
MH  - Phenethylamines/metabolism/*pharmacology
MH  - Rats
MH  - Rats, Sprague-Dawley
PMC - PMC5498282
MID - NIHMS867776
EDAT- 2017/05/26 06:00
MHDA- 2018/01/27 06:00
PMCR- 2018/08/01
CRDT- 2017/05/25 06:00
PHST- 2017/05/26 06:00 [pubmed]
PHST- 2018/01/27 06:00 [medline]
PHST- 2017/05/25 06:00 [entrez]
PHST- 2018/08/01 00:00 [pmc-release]
AID - 10.1097/FBP.0000000000000309 [doi]
PST - ppublish
SO  - Behav Pharmacol. 2017 Aug;28(5):375-385. doi: 10.1097/FBP.0000000000000309.