Novel Amphetamine

A novel analytical method was developed for the simultaneous quantification of the R/S-enantiomers of amphetamine, methamphetamine, MDA and MDMA in hair samples using liquid chromatography-tandem mass spectrometry (LC-MS-MS). This method involved a straightforward derivatization step with dansyl chloride and the use of a chiral column, enabling the separation and quantification of all eight enantiomers in a single analysis. The method exhibited excellent linearity across a concentration range of 0.03-3.00 ng/mg for each enantiomer...

Obsessive Compulsive Disorder (OCD) is a debilitating psychiatric disorder characterized by intrusive obsessive thoughts and compulsive behaviors. Multiple studies have shown association of polymorphisms in the SLC1A1 gene with OCD. The most common of these OCD-associated polymorphisms increases expression of the encoded protein, Excitatory Amino Acid Transporter 3 (EAAT3), a neuronal glutamate transporter. Previous work has shown that increased EAAT3 expression results in OCD-relevant behavioral phenotypes in rodent models...

Novel psychoactive substances (NPS) in the form of impregnated papers delivered to prisoners are of particular concern in prison settings, where they are commonly used by vaping. The purpose of this study was to create a qualitative method for identifying the various emerging NPS impregnated onto paper samples sent to prisoners. It helps to demonstrate that these findings can be used to predict drug prevalence and trends in prisons. Between 2018 and 2020, 1250 non-judicial paper samples seized from 12 English prisons were analysed to determine the NPSs being circulated...

Biogenic monoamines, vital transmitters orchestrating neurological, endocrinal, and immunological functions1-5 , are stored in secretory vesicles by vesicular monoamine transporters (VMATs) for controlled quantal release6,7 . Harnessing proton antiport, VMATs enrich monoamines ~10,000-fold and sequester neurotoxicants to protect neurons8-10 . VMATs are targeted by an arsenal of therapeutic drugs and imaging agents to treat and monitor neurodegenerative disorders, hypertension, and drug addiction1,8,11-16 . However, the structural mechanisms underlying these actions remain elusive...

Methamphetamine (METH) is the most commonly misused amphetamine-type stimulant throughout the globe. METH is very rewarding, and its misuse can lead to a diagnosis of METH use disorder (MUD). Although METH use is observed in both sexes, there are, however, reported differences in the clinical manifestations of METH use and its consequences. These observations indicate the need for more research on the long-term sex-dependent consequences of METH taking in both preclinical and clinical settings. In effect, sex is a biological variable that can impact conclusions drawn from various basic and clinical studies...

Due to the increase in the use of novel psychoactive substances (NPS) and their overall prevalence, it is important to have effective and reliable screening technologies to detect NPS in biological matrices. Enzyme-linked immunosorbent assays (ELISA) are among the most popular screening methods. To evaluate the effectiveness of ELISA for NPS detection, five subclasses of NPS (novel synthetic opioids, fentanyl analogs, stimulants, benzodiazepines and hallucinogens) were evaluated in whole blood for their cross-reactivity on commercially available ELISA kits...

Mania is associated with disturbed dopaminergic transmission in frontotemporal regions. D-amphetamine (AMPH) causes increased extracellular DA levels, considered an acknowledged mania model in rodents. Doxycycline (DOXY) is a second-generation tetracycline with promising neuroprotective properties. Here, we tested the hypothesis that DOXY alone or combined with Lithium (Li) could reverse AMPH-induced mania-like behavioral alterations in mice by the modulation of monoamine levels in brain areas related to mood regulation, as well as cytoprotective and antioxidant effects in hippocampal neurons...

The goal of this research is the development of multiple monolithic fiber-solid phase microextraction (MMF-SPME) using a new integrated fiber for the determination of amphetamine derivatives and modafinil from unauthorized medicinal supplements. For this purpose, a monolithic fiber of metal organic framework MIL-Al (53)-deep eutectic solvent (DES)/molecularly imprinted polymers (MOF-DES/MIP) was synthesized. To find optimum microextraction conditions gas chromatography-mass spectrometer (GC-MS) was used and the influences of effective variables were investigated using one factor at a time method...

I report an unusual case in Saudi Arabia of a 28-year-old man who had bipolar disorder due to a traumatic brain injury suffered 10 years previously. He had been evaluated and diagnosed with schizoaffective disorder as well as amphetamine and hash use disorder until recently, when the team noticed a poor response to treatment and the continuation of his cognitive features. After a reevaluation of the history and evidence of the brain lesions on the MRI, the diagnosis was changed to bipolar disorder due to a traumatic brain injury...

Amphetamines, as psychoactive drugs, are extensively abused in society and cause serious mental and physical disorders among young people. Furthermore, the extremely euphoric and excited sense of stimulant consumption leads to dramatic social problems. Determination of various analytes and related metabolites in the complex biological matrices at trace levels has made sample preparation an indispensable part of forensic sciences. According to the problems above, providing high sensitivity, solving some analytical problems like matrix effects in LCMS-MS, and needing a cleaner extract are remarkable aspects of novel sample preparation methods in drug analysis...

Abuse of novel arylcyclohexylamines (ACX) poses risks for toxicities including adverse neurocognitive effects. In vivo effects of ring-substituted analogs of phencyclidine (PCP), eticyclidine (PCE), and ketamine are understudied. Adult male NIH Swiss mice were used to assess locomotor effects of PCP and its 3-OH, 3-MeO, 3-Cl and 4-MeO analogs; PCE and its 3-OH and 3-MeO analogs; and ketamine and its deschloro and 2F-deschloro analogs, in comparison to those of methamphetamine (METH), 3,4-methylenedioxymethamphetamine (MDMA), and two benzofuran analogs of MDMA...


Most methods for partial volume correction (PVC) of positron emission tomography (PET) data employ anatomical segmentation of images into regions of interest, an approach that is not optimal for exploratory functional imaging beyond regional hypotheses. We describe a novel method for unbiased voxel-wise PVC.
Approach:
B-spline basis functions were combined with geometric transfer matrices to enable a method (bsGTM) that provides PVC or alternatively provides smoothing with minimal regional crosstalk...

IMPORTANCE: Plasma cell orificial mucositis (PCOM) associated with cocaine use is an emerging, rare condition that has become a concern in Spain in recent years. Limited knowledge exists regarding this novel condition. OBJECTIVES: To delineate the clinicopathologic characteristics of this emerging entity and establish a novel approach in the differential diagnosis of cocaine-associated lesions. DESIGN, SETTING, AND PARTICIPANTS: A descriptive, retrospective, multicenter case series of 10 patients diagnosed with cocaine-associated PCOM was conducted in Spain from April 2020 to March 2023...

The rapid serial visual presentation (RSVP) task and continuous performance tasks (CPT) are used to assess attentional impairments in patients with psychiatric and neurological conditions. This study developed a novel touchscreen task for rats based on the structure of a human RSVP task and used pharmacological manipulations to investigate their effects on different performance measures. Normal animals were trained to respond to a target image and withhold responding to distractor images presented within a continuous sequence...

Neuropathic pain is a devastating condition where current therapeutics offer little to no pain relief. Novel nonnarcotic therapeutic targets are needed to address this growing medical problem. Our work identified the G-protein-coupled receptor 160 (GPR160) as a potential target for therapeutic intervention. However, the lack of small-molecule ligands for GPR160 hampers our understanding of its role in health and disease. To address this void, we generated a global Gpr160 knockout (KO) mouse using CRISPR-Cas9 genome editing technology to validate the contributions of GPR160 in nociceptive behaviors in mice...

In this study, a novel supramolecular deep eutectic solvent consisting of sulfated-β-CD and citric acid (S-β-CD-CA) is reported for the first time. This innovative system was evaluated as a sole chiral selector in capillary electrophoresis for the enantioseparation of six fluorine-substituted amphetamine analogs, yielding remarkable outcomes. Baseline separations of all amphetamine analogs under study were achieved in less than 21.00 min using the S-β-CD-CA as the chiral selector. It was observed that the addition of 0...

Substitutions to the phenethylamine structure give rise to numerous amphetamines and cathinones, contributing to an ever-growing number of abused novel psychoactive substances. Understanding how various substitutions affect the pharmacology of phenethylamines may help lawmakers and scientists predict the effects of newly emerging drugs. Here, we established structure-activity relationships for locomotor stimulant and monoamine transporter effects of 12 phenethylamines with combinations of para-chloro, β-keto, N-methyl, or N-ethyl additions...

Neuropeptides and G protein-coupled receptors (GPCRs) have long been, and continue to be, one of the most popular target classes for drug discovery in CNS disorders, including alcohol use disorder (AUD). Yet, orphaned neuropeptide systems and receptors (oGPCR), that have no known cognate receptor or ligand, remain understudied in drug discovery and development. Orphan neuropeptides and oGPCRs are abundantly expressed within the brain and represent an unprecedented opportunity to address brain function and may hold potential as novel treatments for disease...

INTRODUCTION: The renewed interest in considering a range of stimulants, psychedelics and dissociatives as therapeutics emphasizes the need to draft an updated overview of these drugs' clinical and pharmacological issues. AREAS COVERED: The focus here was on: stimulants (e.g. amphetamines, methamphetamine, and pseudoephedrine; phenethylamines; synthetic cathinones; benzofurans; piperazines; aminoindanes; aminorex derivatives; phenmetrazine derivatives; phenidates); classical (e...

The Agilent QuickProbe gas chromatograph/mass spectrometer (QP-GCMS) is a rapid analytical instrument requiring minimal sample preparation. The instrument was considered for the screening of samples for potential implementation at New Zealand's border screening laboratory. One of the project's primary aims was to validate the method for the analysis of border seizures, including drug concealments, novel psychoactive substances (NPS), low-dose drugs and unknown substances. For the application to be useful beyond the capabilities of current handheld point-of-contact (POC) devices, the initial evaluation has included the analysis of a large variety of compounds in a large variety of matrices...