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Novel Amphetamine

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https://www.readbyqxmd.com/read/29194289/lack-of-detection-of-new-amphetamine-like-drugs-using-conventional-urinary-immunoassays
#1
A Begeman, E J F Franssen
BACKGROUND: The number of reports of serious adverse effects and intoxication after the use of the new drug 4-fluoroamphetamine (4-FA) increases. At the Emergency Department of the OLVG-Oost Hospital in Amsterdam an on-site drug test, the Triage® TOX Drug Screen, is available to assist in a rapid diagnosis. In less urgent cases, an EMIT® II Plus immunoassay is used to determine semi-quantitatively the presence of drugs of abuse. The antibodies in these immunoassays are designed to detect classic drugs of abuse and its urinary metabolites...
November 29, 2017: Therapeutic Drug Monitoring
https://www.readbyqxmd.com/read/29193459/neuropeptide-cart-prevents-memory-loss-attributed-to-withdrawal-of-nicotine-following-chronic-treatment-in-mice
#2
Chandrashekhar D Borkar, Sneha Sagarkar, Amul J Sakharkar, Nishikant K Subhedar, Dadasaheb M Kokare
Although chronic nicotine administration does not affect memory, its withdrawal causes massive cognitive deficits. The underlying mechanisms, however, have not been understood. We test the role of cocaine- and amphetamine-regulated transcript peptide (CART), a neuropeptide known for its procognitive properties, in this process. The mice on chronic nicotine treatment/withdrawal were subjected to novel object recognition task. The capability of the animal to discriminate between the novel and familiar objects was tested and represented as discrimination index (DI); reduction in the index suggested amnesia...
November 29, 2017: Addiction Biology
https://www.readbyqxmd.com/read/29189167/3d-qsar-and-in-silico-studies-of-natural-products-and-related-derivatives-as-monoamine-oxidase-inhibitors
#3
Priyanka Dhiman, Neelam Malik, Anurag Khatkar
The computational development of human monoamine oxidase (MAO) inhibitors led to advancement in drug design and the treatment of many neurodegenerative diseases and neuropsychiatric disorders. Different natural heterocyclic structures are reported to display selective MAO inhibitory activity by preclinical and in-silico modeling. Currently, the major interest is devoted to the study of natural based therapeutic agents from the different categories. Therefore, we presenting the review to critically discuss and outline the recent advances in our knowledge on the importance of natural and natural based ligand-MAO in-silico methods for novel MAO inhibitors...
November 28, 2017: Current Neuropharmacology
https://www.readbyqxmd.com/read/29187755/a-mouse-model-of-the-schizophrenia-associated-1q21-1-microdeletion-syndrome-exhibits-altered-mesolimbic-dopamine-transmission
#4
Jacob Nielsen, Kim Fejgin, Florence Sotty, Vibeke Nielsen, Arne Mørk, Claus T Christoffersen, Leonid Yavich, Jes B Lauridsen, Dorte Clausen, Peter H Larsen, Jan Egebjerg, Thomas M Werge, Pekka Kallunki, Kenneth V Christensen, Michael Didriksen
1q21.1 hemizygous microdeletion is a copy number variant leading to eightfold increased risk of schizophrenia. In order to investigate biological alterations induced by this microdeletion, we generated a novel mouse model (Df(h1q21)/+) and characterized it in a broad test battery focusing on schizophrenia-related assays. Df(h1q21)/+ mice displayed increased hyperactivity in response to amphetamine challenge and increased sensitivity to the disruptive effects of amphetamine and phencyclidine hydrochloride (PCP) on prepulse inhibition...
November 30, 2017: Translational Psychiatry
https://www.readbyqxmd.com/read/29175958/amphetamine-reverses-escalated-cocaine-intake-via-restoration-of-dopamine-transporter-conformation
#5
Cody A Siciliano, Kaustuv Saha, Erin S Calipari, Steve C Fordahl, Rong Chen, Habibeh Khoshbouei, Sara R Jones
Cocaine abuse disrupts dopamine system function, including reduced cocaine inhibition of the dopamine transporter (DAT), which results in tolerance. Although tolerance is a hallmark of cocaine addiction and a DSM-V criteria for substance abuse disorders, the molecular adaptations producing tolerance are unknown, and testing the impact of DAT changes on drug taking behaviors has proven difficult. In regard to treatment, amphetamine has shown efficacy in reducing cocaine intake; however, the mechanisms underlying these effects have not been explored...
November 24, 2017: Journal of Neuroscience: the Official Journal of the Society for Neuroscience
https://www.readbyqxmd.com/read/29163012/iron-oxide-nanoparticle-delivery-of-peptides-to-the-brain-reversal-of-anxiety-during-drug-withdrawal
#6
Nathan Vinzant, Jamie L Scholl, Chia-Ming Wu, Trevor Kindle, Ranjit Koodali, Gina L Forster
Targeting neuropeptide systems is important for future advancements in treatment of neurological and psychiatric illnesses. However, many of the peptides and their analogs do not cross the blood-brain barrier (BBB) efficiently. Nanoparticles such as iron oxide can cross the BBB, and here we describe a novel method for the conjugation of a peptide antisauvagine-30 (ASV-30) to iron oxide nanoparticles. Previous research has shown that direct infusion of ASV-30 into the brain reduces anxiety-like behavior in animal models via actions on corticotropin releasing factor type 2 (CRF2) receptors...
2017: Frontiers in Neuroscience
https://www.readbyqxmd.com/read/29151005/synthesis-of-a-novel-polymeric-magnetic-solid-phase-extraction-adsorbent-for-selective-extraction-of-amphetamine-from-urine-samples-coupled-with-high-performance-liquid-chromatography
#7
Arezou Taghvimi, Marjan Ghorbani, Hamed Hamishehkar
A novel pH-responsive block copolymer (Poly ethylene glycol-b-poly (N,N-dimethylaminoethylmethacrylate-co-maleic acid) was designed for the decoration and stabilization of magnetic nanoparticles (MNPs) to apply as an efficient magnetic nano adsorbent for extraction of amphetamine (AM) from biological urine samples to be determined by high performance liquid chromatography ultra violet detector (HPLC-UV). Full characterization of the synthesized Polymeric magnetic nanoparticles (PMNPs) were followed by various techniques like Fourier transform infrared (FT-IR) spectroscopy, powder x-ray diffraction (XRD), scanning electron microscopy (SEM), and vibrating sample magnetometer (VSM)...
November 18, 2017: Drug Testing and Analysis
https://www.readbyqxmd.com/read/29099402/simultaneous-monitoring-of-electroencephalographic-characteristics-in-animals-subjected-to-behavioral-tests-a-preclinical-investigation
#8
Ramakrishna Nirogi, Saivishal Daripelli, Vijay Benade, Chaitanya Tirumalasetty, Gopinadh Bhyrapuneni, Pradeep Jayarajan
Drug-induced changes in electroencephalographic (EEG) characteristics in animals may be used to predict central activity of drugs in humans. Previous studies have established that drugs affect EEG characteristics in humans and rodents in a similar manner. However, there has been little work to establish correlations between drug effects on behavioral and EEG characteristics in rats. In the current study, we have simultaneously monitored EEG characteristics during a novel object recognition task (NORT) or open field (OF) test in rats...
December 2017: Behavioural Pharmacology
https://www.readbyqxmd.com/read/29091428/heterocyclic-analogues-of-modafinil-as-novel-atypical-dopamine-transporter-inhibitors
#9
Predrag Kalaba, Nilima Y Aher, Marija Ilić, Vladimir Dragačević, Marcus Wieder, Andras G Miklosi, Martin Zehl, Judith Wackerlig, Alexander Roller, Tetyana Beryozkina, Bojana Radoman, Sivaprakasam R Saroja, Wolfgang Lindner, Eduardo Perez Gonzalez, Vasiliy Bakulev, Johann Jakob Leban, Harald H Sitte, Ernst Urban, Thierry Langer, Gert Lubec
Modafinil is a wake promoting compound with high potential for cognitive enhancement. It is targeting the dopamine transporter (DAT) with moderate selectivity, thereby leading to reuptake inhibition and increased dopamine levels in the synaptic cleft. A series of modafinil analogues have been reported so far, but more target-specific analogues remain to be discovered. It was the aim of this study to synthesize and characterize such analogues and, indeed, a series of compounds were showing higher activities on the DAT and a higher selectivity toward DAT versus serotonin and norepinephrine transporters than modafinil...
November 22, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29081089/evaluation-of-the-abuse-potential-of-novel-amphetamine-derivatives-with-modifications-on-the-amine-nbna-and-phenyl-eda-pmea-2-apn-sites
#10
Raly James Perez Custodio, Chrislean Jun Botanas, Seong Shoon Yoon, June Bryan de la Peña, Irene Joy Dela Peña, Mikyung Kim, Taeseon Woo, Joung-Wook Seo, Choon-Gon Jang, Yong Ho Kwon, Nam Yong Kim, Yong Sup Lee, Hee Jin Kim, Jae Hoon Cheong
Recently, there has been a rise in the number of amphetamine derivatives that serve as substitutes for controlled substances (e.g. amphetamine and methamphetamine) on the global illegal drug market. These substances are capable of producing rewarding effects similar to their parent drug. In anticipation of the future rise of new and similar psychoactive substances, we designed and synthesized four novel amphetamine derivatives with N-benzyl, N-benzylamphetamine HCl (NBNA) substituent on the amine region, 1,4-dioxane ring, ethylenedioxy-amphetamine HCl (EDA), methyl, para-methylamphetamine HCl (PMEA), and naphthalene, 2-(aminopropyl) naphthalene HCl (2-APN) substituents on the phenyl site...
November 1, 2017: Biomolecules & Therapeutics
https://www.readbyqxmd.com/read/29057665/medications-for-substance-use-disorders-sud-emerging-approaches
#11
Eduardo R Butelman, Mary Jeanne Kreek
Substance use disorders are a group of chronic relapsing disorders of the brain, which have massive public health and societal impact. In some disorders (e.g., heroin/prescription opioid addictions) approved medications have a major long-term benefit. For other substances (e.g., cocaine, amphetamines and cannabis) there are no approved medications, and for alcohol there are approved treatments, which are not in wide usage. Approved treatments for tobacco use disorders are available, and novel medications are also under study...
October 30, 2017: Expert Opinion on Emerging Drugs
https://www.readbyqxmd.com/read/29030166/mdpv-and-%C3%AE-pvp-use-in-humans-the-twisted-sisters
#12
REVIEW
Laurent Karila, Geneviève Lafaye, Amandine Scocard, Olivier Cottencin, Amine Benyamina
The new psychoactive substances phenomenon continues to represent a considerable public health challenge. Synthetic cathinones are β-keto amphetamine analogues, also known as legal highs, research chemicals, bath salts. These drugs have surfaced as a popular alternative to other illicit drugs of abuse, such as cocaine, MDMA, and methamphetamine, due to their potent psychostimulant and empathogenic effects. Pyrovalerone cathinones (a-pyrrolidinophenones) form a distinct group of designer cathinones, such as MDPV...
October 10, 2017: Neuropharmacology
https://www.readbyqxmd.com/read/28985320/multiple-drug-toxicity-involving-novel-psychoactive-substances-3-fluorophenmetrazine-and-u-47700
#13
Kayla N Ellefsen, Elizabeth A Taylor, Paul Simmons, Vickie Willoughby, Brad J Hall
3-Fluorophenmetrazine (3-FPM) is a stimulant-like novel psychoactive substance (NPS) and fluorinated analog of phenmetrazine that has recently appeared on the recreational drug market, with limited published information. Likewise, the synthetic opioid U-47700 has gained popularity among recreational drug users and is frequently detected in postmortem casework. We present the case history, autopsy and toxicological findings of a fatality involving the designer drugs 3-FPM and U-47700 for the first time in the literature...
July 20, 2017: Journal of Analytical Toxicology
https://www.readbyqxmd.com/read/28950240/prevalence-and-motivations-for-kratom-use-in-a-sample-of-substance-users-enrolled-in-a-residential-treatment-program
#14
Kirsten Elin Smith, Thomas Lawson
BACKGROUND: Kratom use in the West has increased recently, yet the prevalence and motives for use among individuals with a history of substance use disorder (SUD) have not been fully examined. Kratom has been documented as a means of treating chronic pain, mitigating drug dependence, and easing withdrawal symptoms, yet it is unclear if substance users are utilizing kratom as a self-medication. Abuse liability, side effects, and overall appeal of kratom remain uncertain. METHODS: In April 2017, an anonymous survey regarding kratom use and motivations was completed by clients enrolled in a 12-Step-oriented residential program...
November 1, 2017: Drug and Alcohol Dependence
https://www.readbyqxmd.com/read/28910664/the-analysis-of-132-novel-psychoactive-substances-in-human-hair-using-a-single-step-extraction-by-tandem-lc-ms
#15
Vassiliki A Boumba, Matthew Di Rago, Melissa Peka, Olaf H Drummer, Dimitri Gerostamoulos
A rapid LC-MS/MS method for the targeted screening of 132 NPS in hair is described. Drugs include cathinones and synthetic cannabinoids, as well as amphetamine-type stimulants, piperazines and other hallucinogenic compounds. This method utilizes hair pulverization in acidified methanol followed by analysis using liquid chromatography coupled with tandem MS. The limit of detection varied from 0.001 to 0.1ng/mg hair among the various analytes. The method was validated in terms of sensitivity, selectivity, repeatability and stability...
October 2017: Forensic Science International
https://www.readbyqxmd.com/read/28894302/g%C3%AE-%C3%AE-subunit-activation-promotes-dopamine-efflux-through-the-dopamine-transporter
#16
J Garcia-Olivares, T Baust, S Harris, P Hamilton, A Galli, S G Amara, G E Torres
The dopamine transporter (DAT) is an important regulator of brain dopamine (DA) homeostasis, controlling the intensity and duration of DA signaling. DAT is the target for psychostimulants-like cocaine and amphetamine-and plays an important role in neuropsychiatric disorders, including attention-deficit hyperactivity disorder and drug addiction. Thus, a thorough understanding of the mechanisms that regulate DAT function is necessary for the development of clinical interventions to treat DA-related brain disorders...
September 12, 2017: Molecular Psychiatry
https://www.readbyqxmd.com/read/28889212/cocaine-like-discriminative-stimulus-effects-of-norepinephrine-preferring-monoamine-releasers-time-course-and-interaction-studies-in-rhesus-monkeys
#17
Stephen J Kohut, David S Jacobs, Richard B Rothman, John S Partilla, Jack Bergman, Bruce E Blough
RATIONALE: The therapeutic potential of monoamine releasers with prominent dopaminergic effects is hindered by their high abuse liability. OBJECTIVES: The present study examined the effects of several novel "norepinephrine (NE)-preferring" monoamine releasers relative to non-selective monoamine releasers, d-amphetamine and d-methamphetamine, in rhesus monkeys trained to discriminate cocaine. NE-preferring releasers were approximately 13-fold more potent for NE compared to dopamine release and ranged in potency for serotonin release (PAL-329 < l-methamphetamine < PAL-169)...
December 2017: Psychopharmacology
https://www.readbyqxmd.com/read/28879579/novel-selectivity-based-forensic-toxicological-validation-of-a-paper-spray-mass-spectrometry-method-for-the-quantitative-determination-of-eight-amphetamines-in-whole-blood
#18
Sebastiaan F Teunissen, Patrick W Fedick, Bjorn J A Berendsen, Michel W F Nielen, Marcos N Eberlin, R Graham Cooks, Arian C van Asten
Paper spray tandem mass spectrometry is used to identify and quantify eight individual amphetamines in whole blood in 1.3 min. The method has been optimized and fully validated according to forensic toxicology guidelines, for the quantification of amphetamine, methamphetamine, 3,4-methylenedioxyamphetamine (MDA), 3,4-methylenedioxy-N-methylamphetamine (MDMA), 3,4-methylenedioxy-N-ethylamphetamine (MDEA), para-methoxyamphetamine (PMA), para-methoxymethamphetamine (PMMA), and 4-fluoroamphetamine (4-FA). Additionally, a new concept of intrinsic and application-based selectivity is discussed, featuring increased confidence in the power to discriminate the amphetamines from other chemically similar compounds when applying an ambient mass spectrometric method without chromatographic separation...
September 6, 2017: Journal of the American Society for Mass Spectrometry
https://www.readbyqxmd.com/read/28878698/synthetic-cathinone-and-cannabinoid-designer-drugs-pose-a-major-risk-for-public-health
#19
REVIEW
Aviv M Weinstein, Paola Rosca, Liana Fattore, Edythe D London
As part of an increasing worldwide use of designer drugs, recent use of compounds containing cathinones and synthetic cannabinoids is especially prevalent. Here, we reviewed current literature on the prevalence, epidemiology, bio-behavioral effects, and detection of these compounds. Gender differences and clinical effects will also be examined. Chronic use of synthetic cathinone compounds can have major effects on the central nervous system and can induce acute psychosis, hypomania, paranoid ideation, and delusions, similar to the effects of other better-known amphetamine-type stimulants...
2017: Frontiers in Psychiatry
https://www.readbyqxmd.com/read/28865391/discriminative-stimulus-and-locomotor-effects-of-para-substituted-and-benzofuran-analogs-of-amphetamine
#20
Sean B Dolan, Michael J Forster, Michael B Gatch
Novel psychoactive substances have maintained a prominent role in the global drug culture, despite increased regulation by governing bodies. Novel compounds continue to become available on the market, often in "Ecstasy" or "Molly" formulations in lieu of MDMA, at a much faster rate than they can be properly characterized. The current study aimed to investigate the discriminative stimulus and locomotor effects of three putatively entactogenic compounds that have become increasingly prevalent on the drug market: 5-(2-aminopropyl)-benzofuran (5-APB), 6-(2-aminopropryl)-2,3-dihydrobenzofuran (6-APDB), and 4-fluoroamphetamine (4-FA)...
August 24, 2017: Drug and Alcohol Dependence
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