A5020790730- Psychedelics and Drug Studies
- Neurotransmitter Receptor Influence on Behavior
- Chemical synthesis and alkaloids
- Neuroscience and Neuropharmacology Research
- Treatment of Major Depression
- Plant and fungal interactions
- Nicotinic Acetylcholine Receptors Study
- Biochemical Analysis and Sensing Techniques
- Forensic Toxicology and Drug Analysis
- Analytical Chemistry and Chromatography
- Receptor Mechanisms and Signaling
- Pharmacological Receptor Mechanisms and Effects
- Tryptophan and brain disorders
- Metabolomics and Mass Spectrometry Studies
- Coordination Chemistry and Organometallics
- Vanadium and Halogenation Chemistry
- Fluorine in Organic Chemistry
- Chemical Synthesis and Analysis
- Cholinesterase and Neurodegenerative Diseases
- Crystallization and Solubility Studies
- Pesticide Exposure and Toxicity
- Heme Oxygenase-1 and Carbon Monoxide
- Pain Mechanisms and Treatments
- Cannabis and Cannabinoid Research
- Protein Degradation and Inhibitors
Saint Joseph's University
2023-2024
University of the Sciences
2013-2022
Saarland University
2016
Serotonergic psychedelics possess considerable therapeutic potential. Although 5-HT2A receptor activation mediates psychedelic effects, prototypical activate both 5-HT2A-Gq/11 and β-arrestin2 transducers, making their respective roles unclear. To elucidate this, we develop a series of 5-HT2A-selective ligands with varying Gq efficacies, including β-arrestin-biased ligands. We show that 5-HT2A-Gq but not 5-HT2A-β-arrestin2 recruitment efficacy predicts potential, assessed using head-twitch...
1‐Propionyl‐ d ‐lysergic acid diethylamide hemitartrate (1P‐LSD) has become available as a ‘research chemical’ in the form of blotters and powdered material. This non‐controlled derivative (LSD) previously not been described published literature despite being closely related to 1‐acetyl‐LSD (ALD‐52), which was developed 1950s. study describes characterization 1P‐LSD comparison with LSD using various chromatographic mass spectrometric methods, infrared nuclear magnetic resonance spectroscopy....
The psychedelic properties of lysergic acid diethylamide (LSD) have captured the imagination researchers for many years and its rediscovery as an important research tool is evidenced by clinical use within neuroscientific therapeutic settings. At same time, a number novel LSD analogs recently emerged recreational drugs, which makes it necessary to study their analytical pharmacological properties. One recent addition this series 1-butanoyl-LSD (1B-LSD), constitutional isomer...
1,2-Diarylethylamines including lanicemine, lefetamine, and remacemide have clinical relevance in a range of therapeutic areas pain management, epilepsy, neurodegenerative disease depression. More recently 1,2-diarylethylamines been sold as 'legal highs' number different forms powders tablets. These compounds are to circumvent governmental legislation regulating psychoactive drugs. Examples include the opioid MT-45 dissociative agents diphenidine (DPH) 2-methoxy-diphenidine (2-MXP). A fatal...
Lysergic acid N , ‐diethylamide (LSD) is perhaps one of the most intriguing psychoactive substances known and numerous analogs have been explored to varying extents in previous decades. In 2013, 6 ‐allyl‐6‐norlysergic diethylamide (AL‐LAD) (2’ S ,4’ )‐lysergic 2,4‐dimethylazetidide (LSZ) appeared on ‘research chemicals’/new (NPS) market both powdered blotter form. This study reports analytical characterization AL‐LAD LSZ tartrate samples their semi‐quantitative determination paper. Included...
2-Methoxydiphenidine, i.e. 1-[1-(2-methoxyphenyl)-2-phenylethyl]piperidine, also known as 'MXP' or '2-MeO-diphenidine' (or 2-MXP), has been available a 'research chemical' since 2013 purported alternative to the 'dissociative anesthetics' methoxetamine and ketamine. Three deaths which involved detection of 2-MXP in post-mortem blood urine were encountered forensic casework. The 2-, 3- 4-methoxyphenyl positional isomers synthesized confirm identity concentration 2-MXP. femoral concentrations...
Lysergic acid diethylamide (LSD) is perhaps one of the best-known psychoactive substances and many structural modifications this prototypical lysergamide have been investigated. Several lysergamides were recently encountered as 'research chemicals' or new (NPS). Although lysergic morpholide (LSM-775) appeared on NPS market in 2013, there disagreement literature regarding potency properties LSM-775 humans. The present investigation attempts to address gap information that exists analytical...
The psychoactive properties of lysergic acid diethylamide (LSD) have fascinated scientists across disciplines and the exploration other analogues derivatives has been motivated by deepening understanding ligand‐receptor interactions at molecular level as well search for new therapeutics. Several LSD congeners appeared on substances (NPS) market in form blotters or powders. Examples include 1‐propionyl‐LSD (1P–LSD), AL‐LAD, LSZ. absence analytical data novel compounds is a frequent challenge...
Background: 3-Methoxyphencyclidine (3-MeO-PCP) and 3-methoxyrolicyclidine (3-MeOPCPy) are two new psychoactive substances (NPS). The aims of the present study were elucidation their metabolic fate in rat pooled human liver microsomes (pHLM), identification cytochrome P450 (CYP) isoenzymes involved, detectability using standard urine screening approaches (SUSA) after intake common users' doses gas chromatography-mass spectrometry (GC-MS), liquid chromatography-multi-stage mass (LC-MSn),...
Abstract Lysergic acid diethylamide (LSD) is a prototypical serotonergic psychedelic drug and the subject of many clinical investigations. In recent years, range lysergamides has emerged with production some being inspired by existing scientific literature. Others, for example various 1‐acyl substituted lysergamides, did not exist before their appearance as research chemicals. 1‐Cylopropanoyl‐LSD (1CP‐LSD) recently new addition to group lysergamide‐based designer drugs believed be...
Serotonergic psychedelics possess considerable therapeutic potential. Although 5-HT2A receptor activation mediates psychedelic effects, prototypical activate both 5-HT2A-Gq/11 and β-arrestin2 signaling, making their respective roles unclear. To elucidate this, we developed a series of 5-HT2A-selective ligands with varying Gq efficacies, including β-arrestin-biased ligands. We show that 5-HT2A-Gq but not 5-HT2A-β-arrestin2 efficacy predicts potential, assessed using head-twitch response (HTR)...
The structurally diverse nature of the 1,2-diphenylethylamine template provides access to a range substances for drug discovery work but some have attracted attention as 'research chemicals'. most recent examples include diphenidine, i.e. 1-(1,2-diphenylethyl)piperidine and 2-methoxydiphenidine, 1-[1-(2-methoxyphenyl)-2-phenylethyl]piperidine (MXP, methoxyphenidine, 2-MXP) that been associated with uncompetitive N-methyl-D-aspartate (NMDA) receptor antagonist activity. Analytical challenges...
Abstract: Histone deacetylases (HDACs) are key regulators of gene expression in cells and have been investigated as important therapeutic targets for cancer other diseases. Different subtypes HDACs appear to play disparate roles the associated with specific Therefore, substantial effort has made develop subtype-selective HDAC inhibitors. In an discover existing scaffolds inhibitory activity, we screened a drug library approved by US Food Drug Administration National Institutes Health...
Three psychoactive arylcyclohexylamines, advertised as "research chemicals," were obtained from an online retailer and characterized by gas chromatography ion trap electron chemical ionization mass spectrometry, nuclear magnetic resonance spectroscopy diode array detection. The three phencyclidines identified 2-(ethylamino)-2-(3-methoxyphenyl)cyclohexanone (methoxetamine), N-ethyl-1-(3-methoxyphenyl)cyclohexanamine 1-[1-(3-methoxyphenyl)cyclohexyl]piperidine. A qualitative/quantitative...
To avoid legislation based on chemical structure, research chemicals, frequently used for recreational purposes, are continually being synthesized. N-Ethyl-1,2-diphenylethanamine (ephenidine) is a diarylethylamine that has recently become popular with users searching dissociative hallucinogenic effects. In the present study, pharmacological basis of its neural actions been investigated, initially by assessing profile in central nervous system receptor binding assays and subsequently targeted...
Substances with the diphenylethylamine nucleus represent a recent addition to product catalog of dissociative agents sold as 'research chemicals' on Internet. Diphenidine, i.e. 1-(1,2-diphenylethyl)piperidine (1,2-DEP), is such an example but detailed analytical data are less abundant. The present study describes synthesis diphenidine and its most obvious isomer, 1-(2,2-diphenylethyl)piperidine (2,2-DEP), in order assess ability differentiate between them. Preparation characterization were...
Classic examples of psychoactive arylcycloalkylamines include ketamine and 1‐(1‐phenylcyclohexyl)piperidine (PCP) many others serve as important structural templates for neuropharmacological research. The recent emergence PCP analogues that can be obtained from internet retailers requires the implementation appropriate monitoring strategies harm reduction purposes. Access to analytical data plays a key part when encountering these substances, especially if reference material is not...