Article
Biochemistry & Molecular Biology
Nuria Nadal-Gratacos, Esther Lleixa, Monica Gibert-Serramia, Roger Estrada-Tejedor, Xavier Berzosa, Xavier Batllori, David Pubill, Jordi Camarasa, Elena Escubedo, Raul Lopez-Arnau
Summary: Changes in the molecular structure of synthetic cathinones have led to an increase in the number of novel emerging drugs in the illicit drug market. This study investigates the effects of para- and meta-halogen substitutions on the in vivo, in vitro, and in silico effects of alpha-PVP derivatives. The study provides evidence of the rewarding and anxiety-like properties of halogenated alpha-PVP derivatives.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2022)
Article
Biochemistry & Molecular Biology
Rachel A. Davies, Vy T. Nguyen, Jose M. Eltit, Richard A. Glennon
Summary: a-Pyrrolidinohexiophenone (a-PHP) is a synthetic cathinone central stimulant that is structurally similar to a-PVP. It is a potent dopamine transporter (DAT) reuptake inhibitor. In this study, a series of 4-substituted a-PHP analogues were examined, and most showed selective DAT reuptake inhibition with a narrow range of potency. The 4-CF3 analogue was an outlier with reduced potency and selectivity. QSAR study was not possible due to limited empirical results.
ACS CHEMICAL NEUROSCIENCE
(2023)
Article
Ornithology
Yu-Chia Ku, Yu-Chi Chen, Chih-Ming Hung, Chen Siang Ng
Summary: This study investigated the genetic factors associated with the expansion of African Sacred Ibises in Taiwan and found that genetic variation in behavior-related genes may not have played a significant role in the successful invasion of these birds. Despite inbreeding effects, the behavior-related genes showed high levels of genetic variation.
Article
Neurosciences
L. Duart-Castells, N. Nadal-Gratacos, M. Muralter, B. Puster, X. Berzosa, R. Estrada-Tejedor, M. Niello, S. Bhat, D. Pubill, J. Camarasa, H. H. Sitte, E. Escubedo, R. Lopez-Arnau
Summary: The study highlights the role of amino terminal substitution in the pharmacological profile of novel synthetic cathinones, including their potency in inhibiting dopamine uptake and inducing psychostimulant and rewarding effects in mice. The results demonstrate a significant correlation between predicted binding affinities by molecular docking and affinity constants for human dopamine transporter, indicating the importance of amino substitutions in determining the biological activity of these compounds.
Article
Biochemistry & Molecular Biology
Daria S. Kalinina, Vsevolod A. Lyakhovetskii, Oleg V. Gorskii, Polina Yu. Shkorbatova, Natalia V. Pavlova, Elena Yu. Bazhenova, Yurii I. Sysoev, Raul R. Gainetdinov, Pavel E. Musienko
Summary: Dopamine is a critical neurotransmitter involved in controlling muscle tone and body posture. In this study, we investigated the effects of dopamine deficiency on motor capacities and muscle responses to postural disturbance. The results showed that dopamine deficiency led to bradykinesia, rigidity, and postural instability, and affected the initiation pattern of corrective responses. These findings provide insights into the role of dopamine in postural reactions and can be used to study dopamine-related diseases.
Article
Multidisciplinary Sciences
Marco Niello, Spyridon Sideromenos, Ralph Gradisch, Ronan O'Shea, Jakob Schwazer, Julian Maier, Nina Kastner, Walter Sandtner, Kathrin Jantsch, Carl R. Lupica, Alexander F. Hoffman, Gert Lubec, Claus J. Loland, Thomas Stockner, Daniela D. Pollak, Michael H. Baumann, Harald H. Sitte
Summary: By using various in vitro, computational, and in vivo approaches, we found that the drug-binding kinetics of S-enantiomers of pyrovalerone analogs at DAT correlate with the time-course of in vivo psychostimulant action in mice. In particular, the slow dissociation (i.e., slow koff) of S-enantiomers of pyrovalerone analogs from DAT can predict their more persistent in vivo effects compared to cocaine and methylphenidate. Overall, our findings highlight the critical importance of drug-binding kinetics at DAT in determining the in vivo profile of effects produced by psychostimulant drugs.
PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA
(2023)
Article
Pharmacology & Pharmacy
Adithya Gopinath, Tabish Riaz, Emily Miller, Leah Phan, Aidan Smith, Ohee Syed, Stephen Franks, Luis R. Martinez, Habibeh Khoshbouei
Summary: Methamphetamine, a commonly abused psychostimulant, targets the dopamine transporter (DAT) and inhibits dopamine uptake while increasing dopamine release in the brain. It also affects peripheral immune cells expressing DAT, leading to impaired wound healing and increased susceptibility to infection. The study showed that methamphetamine treatment down-regulated DAT expression in innate and adaptive immune cells, without affecting their total numbers. Additionally, serum cytokine distributions were altered in methamphetamine-treated mice. These findings suggest that methamphetamine modulates peripheral immune responses by regulating DAT expression.
BASIC & CLINICAL PHARMACOLOGY & TOXICOLOGY
(2023)
Article
Neurosciences
Sarah Threlfell, Amir Saeid Mohammadi, Brent J. Ryan, Natalie Connor-Robson, Nicola J. Platt, Rishi Anand, Florence Serres, Trevor Sharp, Nora Bengoa-Vergniory, Richard Wade-Martins, Andrew Ewing, Stephanie J. Cragg, Katherine R. Brimblecombe
Summary: This study investigated the impact of human alpha-synuclein on DAT function in a transgenic mouse model of early PD. The results show that alpha-synuclein can promote striatal DAT function, which is regulated by extracellular cholesterol.
FRONTIERS IN CELLULAR NEUROSCIENCE
(2021)
Article
Biology
John Sebastiani, Allyson Sabatelli, M. Danielle McDonald
Summary: Mild hypoxia in toadfish results in increased 5-HT uptake and degradation in peripheral tissues, leading to reduced plasma 5-HT levels. The gill appears to play a major role in the clearance of 5-HT.
JOURNAL OF EXPERIMENTAL BIOLOGY
(2022)
Article
Biochemistry & Molecular Biology
Maria Ptukha, Zoia Fesenko, Anastasia Belskaya, Arina Gromova, Arseniy Pelevin, Natalia Kurzina, Raul R. Gainetdinov, Anna Volnova
Summary: This study evaluated the effect of atomoxetine on the behavior and brain activity of dopamine transporter knockout (DAT-KO) rats, which exhibit ADHD-like behavior. Atomoxetine improved PPI and reduced repetitive behaviors in DAT-KO rats and also influenced the behavior of wild-type rats. Furthermore, it led to significant changes in power spectra and coherence of both DAT-KO and wild type rats.
Article
Biochemistry & Molecular Biology
Monia Lenzi, Veronica Cocchi, Sofia Gasperini, Raffaella Arfe, Matteo Marti, Patrizia Hrelia
Summary: The study evaluated the mutagenicity of Mexedrone, alpha-PVP and alpha-PHP on DNA, indicating Mexedrone's mutagenic potential while the other two compounds did not show mutagenicity; even with extrinsic metabolic activation, the mutagenic capacity of alpha-PVP and alpha-PHP could not be excluded, and their metabolites were found to be mutagenic. The induction of reactive oxygen species (ROS) was evaluated as a possible mechanism for the effects but did not show a statistically significant increase in ROS levels for any of the tested substances.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2021)
Article
Biochemistry & Molecular Biology
Lucia Caffino, Francesca Mottarlini, Sabrine Bilel, Giorgia Targa, Micaela Tirri, Coralie Maggi, Matteo Marti, Fabio Fumagalli
Summary: The study reveals that the expression of neuroplastic markers in the brain can be altered by low doses of MDPV or alpha-PVP, suggesting the widespread impact of these cathinones on brain plasticity.
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
(2021)
Article
Biology
Sepand Riyahi, Jose G. Carrillo-Ortiz, Francesc Uribe, Francesc Calafell, Juan Carlos Senar
Summary: The SNP290 polymorphism of the SERT gene is strongly associated with risk-taking behaviors in great tits. Birds with the CT genotype exhibit faster response to the flag, higher distress calling rate, and fewer hissing calls compared to birds with the CC genotype. Hissing behavior should be considered as fear-induced shy behavior.
JOURNAL OF EXPERIMENTAL BIOLOGY
(2022)
Article
Clinical Neurology
Vadim Yuferov, Eduardo R. Butelman, Matthew Randesi, Wim van den Brink, Peter Blanken, Jan M. van Ree, Mary Jeanne Kreek
Summary: The functional SERT promoter tandem repeat genotype may be associated with heavy cocaine exposure and more rapid escalation of cocaine use, in persons with and without opioid dependence diagnosis.
NEUROPSYCHIATRIC DISEASE AND TREATMENT
(2021)
Article
Neurosciences
Gael Villanueva-Charbonneau, Stephane Potvin, Serge Marchand, Alexander McIntyre, Diane McIntosh, Alain Bissonnette, Alain Gendron, Charles-edouard Giguere, Marie-eve Koue, Edouard Kouassi
Summary: This study found that mRNA expression of serotonin transporter (SERT) on the surface of peripheral blood mononuclear cells (PBMCs) was significantly reduced in subjects with major depression disorder (MDD), but not in those with fibromyalgia (FM) or FM + MDD. Although drug treatment improved symptoms, it had no significant effect on SERT mRNA expression.
Article
Biochemical Research Methods
Jose Luiz Costa, Kelly Francisco Cunha, Rafael Lanaro, Ricardo Leal Cunha, Donna Walther, Michael H. Baumann
DRUG TESTING AND ANALYSIS
(2019)
Article
Neurosciences
Brenda M. Gannon, Michael H. Baumann, Donna Walther, Cristian Jimenez-Morigosa, Agnieszka Sulima, Kenner C. Rice, Gregory T. Collins
NEUROPSYCHOPHARMACOLOGY
(2018)
Article
Biochemistry & Molecular Biology
Donna Walther, Abdelrahman R. Shalabi, Michael H. Baumann, Richard A. Glennon
ACS CHEMICAL NEUROSCIENCE
(2019)
Article
Neurosciences
Kusumika Saha, Yang Li, Marion Holy, Kurt R. Lehner, Mohammad O. Bukhari, John S. Partilla, Walter Sandtner, Harald H. Sitte, Michael H. Baumann
PSYCHOPHARMACOLOGY
(2019)
Article
Neurosciences
Bruce E. Blough, Ann M. Decker, Antonio Landavazo, Ojas A. Namjoshi, John S. Partilla, Michael H. Baumann, Richard B. Rothman
PSYCHOPHARMACOLOGY
(2019)
Article
Pharmacology & Pharmacy
Charles W. Schindler, Eric B. Thorndike, Kenner C. Rice, John S. Partilla, Michael H. Baumann
JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS
(2019)
Article
Neurosciences
Adam L. Halberstadt, Simon D. Brandt, Donna Walther, Michael H. Baumann
PSYCHOPHARMACOLOGY
(2019)
Article
Clinical Neurology
Dino Luethi, Karolina E. Kolaczynska, Melanie Walter, Masaki Suzuki, Kenner C. Rice, Bruce E. Blough, Marius C. Hoener, Michael H. Baumann, Matthias E. Liechti
JOURNAL OF PSYCHOPHARMACOLOGY
(2019)
Article
Neurosciences
Marianne Skov-Skov Bergh, Inger Lise Bogen, Nancy Garibay, Michael H. Baumann
Article
Pharmacology & Pharmacy
Chloe J. Jordan, Bree A. Humburg, Eric B. Thorndike, Anver Basha Shaik, Zheng-Xiong Xi, Michael H. Baumann, Amy Hauck Newman, Charles W. Schindler
JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS
(2019)
Article
Biochemical Research Methods
Simon D. Brandt, Laura Carlino, Pierce Kavanagh, Folker Westphal, Wolfgang Dreiseitel, Geraldine Dowling, Michael H. Baumann, Harald H. Sitte, Adam L. Halberstadt
DRUG TESTING AND ANALYSIS
(2020)
Article
Neurosciences
Simon D. Brandt, Hailey M. Walters, John S. Partilla, Bruce E. Blough, Pierce V. Kavanagh, Michael H. Baumann
PSYCHOPHARMACOLOGY
(2020)
Article
Chemistry, Multidisciplinary
Grant C. Glatfelter, Duyen N. K. Pham, Donna Walther, James A. Golen, Andrew R. Chadeayne, Michael H. Baumann, David R. Manke
Summary: This study reported the synthesis, structural characterization, and pharmacological activity of several quaternary tryptammonium analogues. The results showed that these analogues do not target 5-HT2A sites but may have affinity for the serotonin transporter (SERT), providing potential templates for exploring selective actions at SERT.
Article
Chemistry, Medicinal
Grant C. Glatfelter, Marilyn Naeem, Duyen N. K. Pham, James A. Golen, Andrew R. Chadeayne, David R. Manke, Michael H. Baumann
Summary: Analogues of psilocybin are being sold and developed as potential medications for psychedelic-assisted therapies. These analogues produce psychedelic-like effects primarily by agonist activity at serotonin 2A receptors. The present study examines the targeted receptors and the effects of a specific psilocybin analogue, 4-propionoxy-N,N-dimethyltryptamine, in mice.
ACS PHARMACOLOGY & TRANSLATIONAL SCIENCE
(2023)
Editorial Material
Neurosciences
Michael H. Baumann, Gavril W. Pasternak, Sidney S. Negus