DARK Classics in Chemical Neuroscience

α-Pyrrolidinovalerophenone ("Flakka")

Tatiana O. Kolesnikova, Sergey L. Khatsko, Konstantin A. Demin, Vadim A. Shevyrin, Allan V. Kalueff

Research output: Contribution to journalReview articleResearchpeer-review

2 Citations (Scopus)

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.

Original languageEnglish
Pages (from-to)168-174
Number of pages7
JournalACS Chemical Neuroscience
Volume10
Issue number1
DOIs
StatePublished - 16 Jan 2019

Keywords

  • anxiety behavior
  • drugs of abuse
  • sedation
  • synthetic cathinone
  • Zebrafish
  • α-PVP

Scopus subject areas

  • Biochemistry
  • Physiology
  • Cognitive Neuroscience
  • Cell Biology

Cite this

Kolesnikova, Tatiana O. ; Khatsko, Sergey L. ; Demin, Konstantin A. ; Shevyrin, Vadim A. ; Kalueff, Allan V. / DARK Classics in Chemical Neuroscience : α-Pyrrolidinovalerophenone ("Flakka"). In: ACS Chemical Neuroscience. 2019 ; Vol. 10, No. 1. pp. 168-174.
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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.",
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DARK Classics in Chemical Neuroscience : α-Pyrrolidinovalerophenone ("Flakka"). / Kolesnikova, Tatiana O.; Khatsko, Sergey L.; Demin, Konstantin A.; Shevyrin, Vadim A.; Kalueff, Allan V.

In: ACS Chemical Neuroscience, Vol. 10, No. 1, 16.01.2019, p. 168-174.

Research output: Contribution to journalReview articleResearchpeer-review

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T1 - DARK Classics in Chemical Neuroscience

T2 - α-Pyrrolidinovalerophenone ("Flakka")

AU - Kolesnikova, Tatiana O.

AU - Khatsko, Sergey L.

AU - Demin, Konstantin A.

AU - Shevyrin, Vadim A.

AU - Kalueff, Allan V.

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