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Dalibor Sames

15 papers in the library · 323 citations · publishing 2016-2026

Papers

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Development and validation of a UPLC-MS/MS method for real-time neuropharmacokinetic monitoring of iboga alkaloids in rat brain.

Journal of Pharmaceutical and Biomedical Analysis June 24, 2026 Scot Mcintosh, Isabella Maldonado, Nickalus C Smith et al.

Iboga alkaloids, including ibogaine, its primary metabolite noribogaine, and the naturally occurring congener ibogamine, have shown promise for the treatment of substance use and other neuropsychiatric disorders but are limited by cardiotoxic effects. Safer synthetic analogs, such as oxa-noribogaine, are under active development; however, validated analytical methods for quantifying these...

Oxa-noribogaine reduces alcohol drinking through aversion learning and by altering glutamatergic activity in the mPFC

Research Square March 31, 2026 Marcus W. Meinhardt, Ivan Skorodumov, Florian Walter et al.

Abstract Alcohol use disorder is a major global health problem, and current treatments often fail to produce lasting reductions in harmful drinking1,2. Psychedelic-assisted therapies may promote durable behavioural change by enhancing brain plasticity during emotionally meaningful experiences, but progress has been limited by a lack of experimental models that capture these context-dependent...

Deciphering Ibogaine’s Matrix Pharmacology: Multiple Transporter Modulation at Serotonin Synapses

Journal of the American Chemical Society December 26, 2025 Christopher Hwu, Václav Havel, Xavier Westergaard et al. 2 citations

) that has a unique therapeutic potential across multiple indications, including opioid dependence, substance use disorders, depression, anxiety, posttraumatic stress disorder (PTSD), and traumatic brain injury (TBI). We systematically examined the effects of ibogaine, its main metabolite noribogaine, and a series of iboga analogs at monoamine neurotransmitter transporters, some of which have...

Oxa-Iboga alkaloids lack cardiac risk and disrupt opioid use in animal models.

Nature Communications September 20, 2024 Václav Havel, Andrew C Kruegel, Benjamin Bechand et al. 18 citations

Ibogaine and its main metabolite noribogaine provide important molecular prototypes for markedly different treatment of substance use disorders and co-morbid mental health illnesses. However, these compounds present a cardiac safety risk and a highly complex molecular mechanism. We introduce a class of iboga alkaloids - termed oxa-iboga - defined as benzofuran-containing iboga analogs and...

Structural pharmacology and therapeutic potential of 5-methoxytryptamines.

Nature June 1, 2024 Audrey L Warren, David Lankri, Michael J. Cunningham et al. 74 citations

Psychedelic substances such as lysergic acid diethylamide (LSD) and psilocybin show potential for the treatment of various neuropsychiatric disorders1-3. These compounds are thought to mediate their hallucinogenic and therapeutic effects through the serotonin (5-hydroxytryptamine (5-HT)) receptor 5-HT2A (ref. 4). However, 5-HT1A also plays a part in the behavioural effects of tryptamine...

Molecular Design of SERTlight: A Fluorescent Serotonin Probe for Neuronal Labeling in the Brain.

Journal of the American Chemical Society April 10, 2024 Wei-Li Lee, Xavier Westergaard, Christopher Hwu et al. 18 citations

The serotonergic transmitter system plays fundamental roles in the nervous system in neurotransmission, synaptic plasticity, pathological processes, and therapeutic effects of antidepressants and psychedelics, as well as in the gastrointestinal and circulatory systems. We introduce a novel small molecule fluorescent agent, termed SERTlight, that specifically labels serotonergic neuronal cell...

Robust Methods For Quantifying Neuronal Morphology And Molecular Signaling Reveal That Psychedelics Do Not Induce Neuroplasticity

bioRxiv Preprint Server March 4, 2024 Umed Boltaev, Hyun W. Park, Keaon R. Brown et al. 4 citations preprint

Induction of neuroplasticity has become the dominant explanatory framework for the rapid and sustained therapeutic effects of classic psychedelics. Within this broad concept, examination of morphological neuronal plasticity, such as dendritic arbor growth, is widely used to assess the neuroplasticity effects of classic and novel psychedelics. At the molecular level, it has been reported that...

Pharmacological Mechanism of the Non-hallucinogenic 5-HT2A Agonist Ariadne and Analogs

ACS Chemical Neuroscience December 15, 2022 Michael J. Cunningham, Hailey A. Bock, Inis C. Serrano et al. 65 citations

Ariadne is a non-hallucinogenic analog in the phenylalkylamine chemical class of psychedelics that is closely related to an established synthetic hallucinogen, 2,5-dimethoxy-4-methyl-amphetamine (DOM), differing only by one methylene group in the α-position to the amine. Ariadne has been tested in humans including clinical trials at Bristol-Myers Company that indicate a lack of hallucinogenic...

Novel Class of Psychedelic Iboga Alkaloids Disrupts Opioid Use

bioRxiv (Cold Spring Harbor Laboratory) July 23, 2021 Václav Havel, Andrew C Kruegel, Benjamin Bechand et al. 3 citations preprint

Abstract Substance use and related mental health epidemics are causing increasing suffering and death in diverse communities. 1,2 Despite extensive efforts focused on developing pharmacotherapies for treating substance use disorders, there is an urgent need for radically different therapeutic approaches. 3,4 Ibogaine provides an important drug prototype in this direction, as a psychoactive...

A Single Administration of the Atypical Psychedelic Ibogaine or Its Metabolite Noribogaine Induces an Antidepressant-Like Effect in Rats.

ACS Chemical Neuroscience June 3, 2020 Paola Rodrı Guez, Jessika Urbanavicius, José Pedro Prieto et al. 44 citations

Anecdotal reports and open-label case studies in humans indicated that the psychedelic alkaloid ibogaine exerts profound antiaddictive effects. Ample preclinical evidence demonstrated the efficacy of ibogaine, and its main metabolite, noribogaine, in substance-use-disorder rodent models. In contrast to addiction research, depression-relevant effects of ibogaine or noribogaine in rodents have...

A Single Administration of the Atypical Psychedelic Ibogaine or its Metabolite Noribogaine Induces an Antidepressant-like Effect in Rats

ChemRxiv March 19, 2020 Paola Rodrı́guez, Jessika Urbanavicius, José Pedro Prieto et al. 1 citation

Anecdotal reports and open label case studies in humans indicated that the psychedelic alkaloid ibogaine exert profound anti-addictive effects. Ample preclinical evidence demonstrated the efficacy of ibogaine, and its main metabolite noribogaine, in substance use disorder rodent models. In contrast to addiction research, depression-relevant effects of ibogaine or noribogaine in rodents have not...

Ibogaine Administration Modifies GDNF and BDNF Expression in Brain Regions Involved in Mesocorticolimbic and Nigral Dopaminergic Circuits.

Frontiers in Pharmacology 2019 Soledad Marton, Bruno González, Sebastián Rodríguez-bottero et al. 71 citations

Ibogaine is an atypical psychedelic alkaloid, which has been subject of research due to its reported ability to attenuate drug-seeking behavior. Recent work has suggested that ibogaine effects on alcohol self-administration in rats are related to the release of Glial cell Derived Neurotrophic Factor (GDNF) in the Ventral Tegmental Area (VTA), a mesencephalic region which hosts the soma of...

Ibogaine Modifies GDNF, BDNF and NGF Expression in Brain Regions Involved in Mesocorticolimbic and Nigral Dopaminergic Circuits

ChemRxiv October 29, 2018 Soledad Marton, Bruno González, Sebastián Rodríguez et al.

Ibogaine is a psychedelic alkaloid which has been subject of intense scientific research due to its reported ability to attenuate drug-seeking behavior. Recent work suggested that ibogaine effects on alcohol self-administration in rats was related to the release of Glial Cell Derived Neurotrophic Factor (GDNF) in the Ventral Tegmental Area (VTA), a mesencephalic region which hosts soma of...

Deconstructing the Iboga Alkaloid Skeleton: Potentiation of FGF2-induced Glial Cell Line-Derived Neurotrophic Factor Release by a Novel Compound.

ACS Chemical Biology January 15, 2016 Madalee M Gassaway, Teresa L Jacques, Andrew C Kruegel et al. 23 citations

Modulation of growth factor signaling pathways in the brain represents a new experimental approach to treating neuropsychiatric disorders such as depression, anxiety, and addiction. Neurotrophins and growth factors exert synaptic, neuronal, and circuit level effects on a wide temporal range, which suggests a possibility of rapid and lasting therapeutic effects. Consequently, identification of...