PUBLICATION
DARK Classics in Chemical Neuroscience: α-Pyrrolidinovalerophenone ("Flakka")
- Authors
- Kolesnikova, T.O., Khatsko, S.L., Demin, K.A., Shevyrin, V.A., Kalueff, A.V.
- ID
- ZDB-PUB-181127-1
- Date
- 2018
- Source
- ACS Chemical Neuroscience 10(1): 168-174 (Review)
- Registered Authors
- Kalueff, Allan V.
- Keywords
- Zebrafish, anxiety behavior, drugs of abuse, sedation, synthetic cathinone, α-PVP
- MeSH Terms
-
- Animals
- Central Nervous System Stimulants/adverse effects
- Central Nervous System Stimulants/chemistry
- Central Nervous System Stimulants/pharmacology
- Designer Drugs/adverse effects
- Designer Drugs/chemistry*
- Designer Drugs/pharmacology*
- Humans
- Illicit Drugs/adverse effects
- Illicit Drugs/chemistry
- Illicit Drugs/pharmacology
- Psychotropic Drugs/adverse effects
- Psychotropic Drugs/chemistry*
- Psychotropic Drugs/pharmacology*
- Pyrrolidines/adverse effects
- Pyrrolidines/chemistry*
- Pyrrolidines/pharmacology*
- Substance-Related Disorders/diagnosis
- Substance-Related Disorders/psychology
- PubMed
- 30384587 Full text @ ACS Chem. Neurosci.
Citation
Kolesnikova, T.O., Khatsko, S.L., Demin, K.A., Shevyrin, V.A., Kalueff, A.V. (2018) DARK Classics in Chemical Neuroscience: α-Pyrrolidinovalerophenone ("Flakka"). ACS Chemical Neuroscience. 10(1):168-174.
Abstract
Flakka (alpha-pyrrolidinovalerophenone, α-PVP) is a new psychoactive substance, chemically close to cathinone, the primary psychoactive alkaloid of khat ( Catha edulis). Like other synthetic cathinones, α-PVP is a potent inhibitor of the dopamine and norepinephrine transporters. Its robust clinical effects include hallucinations, arousal, aggression/violence, and euphoria. In animal models, α-PVP evokes hyperlocomotion and aberrant/stereotypic behaviors. Here, we discuss the history, synthesis, pharmacological mechanisms, metabolism, abuse potential, and societal impact of α-PVP. Today, α-PVP is a tightly controlled substance, currently banned in the United States and other countries worldwide. However, the growing abuse and complex central nervous system (CNS) effects of α-PVP remain poorly understood, necessitating further pharmacological and pharmacogenetic studies of this drug. Its interesting pharmacological profile (co-inhibition of dopamine and norepinephrine, but not serotonin, transporters) also calls for further studies of α-PVP in animal models, to dissect serotonergic from other monoaminergic mechanisms of action of drugs of abuse. Finally, screening α-PVP and related compounds in vivo may foster discovery of new CNS drugs, including developing novel CNS drugs and identifying their molecular targets.
Genes / Markers
Expression
Phenotype
Mutations / Transgenics
Human Disease / Model
Sequence Targeting Reagents
Fish
Orthology
Engineered Foreign Genes
Mapping