Safety and cognitive pharmacodynamics following dose escalations with 3-methylmethcathinone (3-MMC): a first in human, designerdrug study. 3-Methylmethcathinone (3-MMC) is a designerdrug that belongs to the group of synthetic cathinones. The compound has been scheduled in many jurisdictions because of public health concerns associated with excessive use. To date, there are no clinical studies
SynPharm: A Guide to PHARMACOLOGY Database Tool for DesigningDrug Control into Engineered Proteins A major challenge in synthetic biology, particularly for mammalian systems, is the inclusion of adequate external control for the synthetic system activities. Control at the transcriptional level can be achieved by adaptation of bacterial repressor-operator systems (e.g., TetR), but altering
Metabolism of α-PHP and α-PHPP in humans and the effects of alkyl chain lengths on the metabolism of α-pyrrolidinophenone-type designerdrugs This study aims to investigate the urinary metabolites of two common α-pyrrolidinophenones (PPs), α-pyrrolidinohexiophenone (α-PHP) and α-pyrrolidinoheptanophenone (α-PHPP). This report also aims to discuss the effects of alkyl chain lengths
Detection and identification of designerdrugs by nanoparticle-based NMR chemosensing †Electronic supplementary information (ESI) available. See DOI: 10.1039/c8sc01283k Properly designed monolayer-protected nanoparticles (2 nm core diameter) can be used as nanoreceptors for selective detection and identification of phenethylamine derivatives (designerdrugs) in water. The molecular recognition
The DesignerDrug 3-Fluoromethcathinone Induces Oxidative Stress and Activates Autophagy in HT22 Neuronal Cells Synthetic cathinones are psychoactive substances, derivatives of a natural psychostimulant cathinone. Although many synthetic cathinones have lost their legal status in many countries, their abuse still continues worldwide. Recently, they have been reported to exert neurotoxic effects
Fentanyl-related designerdrugs W-18 and W-15 lack appreciable opioid activity in vitro and in vivo W-18 (4-chloro-N-[1-[2-(4-nitrophenyl)ethyl]-2-piperidinylidene]-benzenesulfonamide) and W-15 (4-chloro-N-[1-(2-phenylethyl)-2-piperidinylidene]-benzenesulfonamide) represent two emerging drugs of abuse chemically related to the potent opioid agonist fentanyl (N-(1-(2-phenylethyl)-4-piperidinyl)-N
Synthetic Cathinone and Cannabinoid DesignerDrugs Pose a Major Risk for Public Health As part of an increasing worldwide use of designerdrugs, 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 cannabinoid designerdrugs, their potential for dependence and abuse, and harmful medical and psychiatric effects, there is a need for research and education in the areas of prevention and treatment.
Designingdrug response experiments and quantifying their results We developed a Python package to help in performing drug-response experiments at medium and high throughput and evaluating sensitivity metrics from the resulting data. In this article, we describe the steps involved in (1) generating files necessary for treating cells with the HP D300 drug dispenser, by pin transfer or by manual
The newest cathinone derivatives as designerdrugs: an analytical and toxicological review Currently, among new psychoactive substances, cathinone derivatives constitute the biggest group, which are mainly classified into -alkylated, 3,4-methylenedioxy--alkylated, -pyrrolidinyl, and 3,4-methylenedioxy--pyrrolidinyl derivatives. These derivatives are actively being subjected to minor
The Psychoactive DesignerDrug and Bath Salt Constituent MDPV Causes Widespread Disruption of Brain Functional Connectivity. The abuse of 'bath salts' has raised concerns because of their adverse effects, which include delirium, violent behavior, and suicide ideation in severe cases. The bath salt constituent 3,4-methylenedioxypyrovalerone (MDPV) has been closely linked to these and other adverse
Cre dependent DREADD (Designer Receptors Exclusively Activated by DesignerDrugs) mice DREADDs, designer receptors exclusively activated by designerdrugs, are engineered G protein-coupled receptors (GPCR) which can precisely control GPCR signaling pathways (for example, Gq, Gs, and Gi). This chemogenetic technology for control of GPCR signaling has been successfully applied in a variety
Educated Guesses and Other Ways to Address the Pharmacological Uncertainty of DesignerDrugs: An Exploratory Study of Experimentation Through an Online Drug Forum This study examines how experimentation with is mediated by the Internet. We selected a popular drug forum that presents reports on self-experimentation with little or even completely unexplored designerdrugs to examine: (1) how experiment with designerdrugs, their trust in suppliers and the testimonials of others, the use of ethno-scientific techniques that involve numerical weighing, "allergy dosing," and the use of standardized trip reports. We suggest that these techniques contribute to a sense of control in the face of the possible toxicity of unknown or little-known designerdrugs. The online reporting of effects allows
Resolving Behavioral Output via Chemogenetic Designer Receptors Exclusively Activated by DesignerDrugs Designer receptors exclusively activated by designerdrugs (DREADDs) have proven to be highly effective neuromodulatory tools for the investigation of neural circuits underlying behavioral outputs. They exhibit a number of advantages: they rely on cell-specific manipulations through canonical
5-(Bis(3-(2-hydroxyethyl)-1H-indol-2-yl)methyl)-2-hydroxybenzoic acid (BHIMHA): showing a strategy of designingdrug to block lung metastasis of tumors Early metastasis is still the most recalcitrant factor in the treatment of lung cancer patients. By analyzing the structures and comparing the docking scores of the known pharmacophores, the authors of this paper designed 5-(bis(3-(2-hydroxyethyl
An In Vitro Study of the Neurotoxic Effects of N-Benzylpiperazine: A DesignerDrug of Abuse Recently, the number of new psychoactive substances has significantly increased. Despite the systematic introduction of prohibition in trade of medicinal products which mimic the effects of illegal drugs, the problem concerning this group of drugs is still important although knowledge about the mechanism ) and activation of caspases: -3 and -9 confirmed by Real-Time PCR imply the activation of mitochondrial proapoptotic pathways induced by BZP after 24 h incubation. This study is a novel, preliminary attempt to explain the toxicity of one of the most popular designerdrug of abuse at the cellular level.
Acute effects of the designerdrugs benzylpiperazine (BZP) and trifluoromethylphenylpiperazine (TFMPP) using functional magnetic resonance imaging (fMRI) and the Stroop task-a pilot study. A novel group of designerdrugs containing benzylpiperazine (BZP) and/or trifluoromethylphenylpiperazine (TFMPP) have been available worldwide for more than a decade; however, their effects on human brain
Designerdrugs 2015: assessment and management Recent designerdrugs, also known as "legal highs," include substituted cathinones (e.g., mephedrone, methylone, and methylenedioxypyrovalerone, often referred to as "bath salts"); synthetic cannabinoids (SCs; e.g., Spice); and synthetic hallucinogens (25I-NBOMe, or N-bomb). Compound availability has evolved rapidly to evade legal regulation of designerdrugs. Clinicians should keep designerdrugs in mind when evaluating substance use in young adults or in anyone presenting with acute neuropsychiatric complaints. Treatment of acute intoxication involves supportive care targeting manifesting signs and symptoms. Long-term treatment of designerdrug use disorder can be challenging and is complicated by a lack of evidence to guide treatment.
Effects of Social Interaction and Warm Ambient Temperature on Brain Hyperthermia Induced by the DesignerDrugs Methylone and MDPV. 3,4-Methylenedioxymethcathinone (methylone) and 3,4-methylenedioxypyrovalerone (MDPV) are new drugs of abuse that have gained worldwide popularity. These drugs are structurally similar to 3,4-methylenedioxymethamphetamine (MDMA) and share many of its physiological