Cathinone derivatives are new recreational drugs known to produce psychostimulant effects. However, unlike other psychostimulants, the addictive potential of cathinone derivatives has not been widely studied. Here, we investigated the effects of pentedrone, a type of cathinone derivative, on the dopaminergic system using reverse transcription polymerase chain reaction and Western blot. We also evaluated the addictive potential of pentedrone using conditioned place preference and self-administration. We found that pentedrone increased the mRNA expression of dopamine 1 receptor, dopamine 2 receptor and dopamine transporter, as well as induced phosphorylation of cAMP response element-binding protein in PC-12 cells. Additionally, pentedrone at 3 and 10 mg/kg significantly increased conditioned place preference in mice, while pentedrone at 0.3 mg/kg/infusion significantly increased self-administration in rats. Finally, we found that acute administration of pentedrone enhanced locomotor activity in a dose-dependent manner. Collectively, these data suggest that the addictive properties of pentedrone may be due to its effects on the dopaminergic system.
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http://dx.doi.org/10.1111/adb.12299 | DOI Listing |
Forensic Sci Int
June 2024
Service de Pharmacologie-Toxicologie et Pharmacovigilance, Centre Hospitalo-Universitaire d'Angers, Angers, France.
The use of 3,4-methylenedioxymethamphetamine (MDMA) in drug-facilitated sexual assault (DFSA) is not uncommon. Indeed, the effects associated with the use of this substance may lead to disinhibition. Several synthetic cathinones, such as mephedrone or methylone, also possess marked entactogenic properties.
View Article and Find Full Text PDFPharmaceutics
February 2024
Centro de Informação e Assistência Toxicológica (CIATox) de Campinas, Universidade Estadual de Campinas (UNICAMP), Campinas 13083-859, SP, Brazil.
New Psychoactive Substances (NPSs) are defined as a group of substances produced from molecular modifications of traditional drugs. These molecules represent a public health problem since information about their metabolites and toxicity is poorly understood. N-ethyl pentedrone (NEP) is an NPS that was identified in the illicit market for the first time in the mid-2010s, with four intoxication cases later described in the literature.
View Article and Find Full Text PDFJ Chromatogr B Analyt Technol Biomed Life Sci
July 2023
Laboratório de Química Orgânica e Farmacêutica, Departamento de Ciências Químicas, Faculdade de Farmácia, Universidade do Porto, Rua Jorge Viterbo Ferreira, 228, 4050-313 Porto, Portugal; Centro Interdisciplinar de Investigação Marinha e Ambiental (CIIMAR), Universidade do Porto, Terminal de Cruzeiros do Porto de Leixões, Avenida General Norton de Matos, s/n, 4450-208 Matosinhos, Portugal. Electronic address:
The binding affinity to human serum albumin (HSA) of a series of fourteen synthetic cathinones, new psychoactive substances widely abused, was investigated by high-performance affinity chromatography (HPAC). Zonal elution experiments were conducted to measure the retention times of each synthetic cathinone on an HSA column, which enabled the calculation of the percentage of the drug bound. For some synthetic cathinones, enantioselectivity on HSA was found.
View Article and Find Full Text PDFInt J Mol Sci
May 2023
National Centre on Addiction and Doping, Istituto Superiore di Sanità, 00161 Rome, Italy.
This study presents a validated GC-MS/MS method for the detection and quantification of 4-chloromethcathinone or clephedrone (4-CMC), N-ethyl Pentedrone (NEP), and N-ethyl Hexedrone (NEH, also named HEXEN) in oral fluid and sweat and verifies its feasibility in determining human oral fluid concentrations and pharmacokinetics following the administration of 100 mg of 4-CMC orally and 30 mg of NEP and NEH intranasally. A total of 48 oral fluid and 12 sweat samples were collected from six consumers. After the addition of 5 μL of methylone-d and 200 μL of 0.
View Article and Find Full Text PDFACS Chem Neurosci
February 2023
Department of Medicinal Chemistry, School of Pharmacy, Virginia Commonwealth University, P.O. Box 980540, Richmond, Virginia 23298, United States.
2-(Benzoyl)piperidines (analogues of ), structural hybrids of the clinically employed ADHD medication methylphenidate () and the abused synthetic cathinone pentedrone (), have been previously reported to act as novel and selective reuptake inhibitors of the human dopamine transporter (hDAT). One of the more potent benzoylpiperidines, as is the case with methylphenidate analogues, is its 3,4-dichloroaryl counterpart. Here, we demonstrate using homology models that these compounds (i.
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