PMID- 37489044
OWN - NLM
STAT- MEDLINE
DCOM- 20240404
LR  - 20240404
IS  - 1942-7611 (Electronic)
IS  - 1942-7603 (Linking)
VI  - 16
IP  - 4
DP  - 2024 Apr
TI  - Characterization of neurotransmitter inhibition for seven cathinones by a 
      proprietary fluorescent dye method.
PG  - 339-347
LID - 10.1002/dta.3547 [doi]
AB  - Many new psychoactive substances (NPS) are stimulants, and information about 
      their potency and abuse potential is often lacking. To start addressing this 
      need, a method measuring the inhibition of the dopamine, serotonin, and 
      norepinephrine transporters (DAT, SERT, and NET) by stimulant drugs was 
      developed. The use of a proprietary fluorescent dye mixture and three cell lines 
      (CHO-K1, HEK 293, and MDCK), each expressing a single transporter, allowed for a 
      semiautomated, one-pot determination of inhibition in a 384-well format. The 
      method was validated using well characterized stimulants, including cocaine, 
      amphetamine, 3,4-methylenedioxymethamphetamine (MDMA), alpha-PVP, and fluoxetine and 
      performed similarly to other methods. Seven synthetic cathinones all showed 
      highest potency for DAT inhibition, followed by NET and SERT. The rank potency 
      for DAT inhibition IC(50) (nM) was MPHP (4.53) > 4Cl-alpha-PVP (8.05) > 3F-alpha-PVP 
      (12.7) > alpha-PiHP (13.4) > N-ethylpentylone (16.9) > N-ethylhexedrone 
      (44.5) > 4-methylpentedrone (261). All but 4-methylpentedrone were more potent 
      than amphetamine (257) and cocaine (111). The DAT/SERT inhibition ratio for the 
      cathinones was in the range from 5.02 for 4-methylpentedrone to >3730 for alpha-PiHP, 
      compared to 1.64 for cocaine and >4030 for alpha-PVP. All seven substances had 
      inhibition profiles similar to those of potent stimulants with high abuse 
      potential.
CI  - (c) 2023 The Authors. Drug Testing and Analysis published by John Wiley & Sons Ltd.
FAU - Persson, Mattias
AU  - Persson M
AUID- ORCID: 0000-0002-4383-2902
AD  - Department of Forensic Genetics and Forensic Toxicology, National Board of 
      Forensic Medicine, Linkoping, Sweden.
FAU - Vikingsson, Svante
AU  - Vikingsson S
AUID- ORCID: 0000-0001-5977-3049
AD  - Department of Forensic Genetics and Forensic Toxicology, National Board of 
      Forensic Medicine, Linkoping, Sweden.
AD  - Division of Clinical Chemistry and Pharmacology, Department of Biomedical and 
      Clinical Sciences, Faculty of Medicine and Health Sciences, Linkoping University, 
      Linkoping, Sweden.
AD  - Center for Forensic Science Advancement and Application, RTI International, 
      Research Triangle Park, North Carolina, USA.
FAU - Kronstrand, Robert
AU  - Kronstrand R
AUID- ORCID: 0000-0002-4222-9597
AD  - Department of Forensic Genetics and Forensic Toxicology, National Board of 
      Forensic Medicine, Linkoping, Sweden.
AD  - Division of Clinical Chemistry and Pharmacology, Department of Biomedical and 
      Clinical Sciences, Faculty of Medicine and Health Sciences, Linkoping University, 
      Linkoping, Sweden.
FAU - Green, Henrik
AU  - Green H
AUID- ORCID: 0000-0002-8015-5728
AD  - Department of Forensic Genetics and Forensic Toxicology, National Board of 
      Forensic Medicine, Linkoping, Sweden.
AD  - Division of Clinical Chemistry and Pharmacology, Department of Biomedical and 
      Clinical Sciences, Faculty of Medicine and Health Sciences, Linkoping University, 
      Linkoping, Sweden.
LA  - eng
GR  - Public Health Agency of Sweden/
GR  - National Board of Forensic Medicine/
PT  - Journal Article
DEP - 20230724
PL  - England
TA  - Drug Test Anal
JT  - Drug testing and analysis
JID - 101483449
RN  - 0 (4-methylpentedrone)
RN  - 540EI4406J (cathinone)
RN  - 767K3AWA4R (1-phenyl-2-(1-pyrrolidinyl)-1-pentanone)
RN  - 0 (Fluorescent Dyes)
RN  - 0 (Central Nervous System Stimulants)
RN  - CK833KGX7E (Amphetamine)
RN  - I5Y540LHVR (Cocaine)
RN  - 0 (Neurotransmitter Agents)
RN  - 0 (Dopamine Plasma Membrane Transport Proteins)
RN  - 0 (Alkaloids)
RN  - 0 (Methylamines)
RN  - 0 (Pentanones)
RN  - 0 (Pyrrolidines)
SB  - IM
MH  - Humans
MH  - Fluorescent Dyes
MH  - HEK293 Cells
MH  - *Central Nervous System Stimulants/pharmacology
MH  - Amphetamine
MH  - *Cocaine/pharmacology
MH  - Neurotransmitter Agents
MH  - Dopamine Plasma Membrane Transport Proteins
MH  - *Alkaloids
MH  - *Methylamines
MH  - *Pentanones
MH  - *Pyrrolidines
OTO - NOTNLM
OT  - cathinones
OT  - inhibition ratio
OT  - monoamine transporter
OT  - neurotransmitter inhibition
OT  - new psychoactive substances
EDAT- 2023/07/25 06:43
MHDA- 2024/04/04 06:45
CRDT- 2023/07/25 02:53
PHST- 2023/06/28 00:00 [revised]
PHST- 2023/01/11 00:00 [received]
PHST- 2023/07/04 00:00 [accepted]
PHST- 2024/04/04 06:45 [medline]
PHST- 2023/07/25 06:43 [pubmed]
PHST- 2023/07/25 02:53 [entrez]
AID - 10.1002/dta.3547 [doi]
PST - ppublish
SO  - Drug Test Anal. 2024 Apr;16(4):339-347. doi: 10.1002/dta.3547. Epub 2023 Jul 24.