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dimethyltryptamine

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https://www.readbyqxmd.com/read/28868040/novel-psychoactive-substances-recent-progress-on-neuropharmacological-mechanisms-of-action-for-selected-drugs
#1
REVIEW
Zurina Hassan, Oliver G Bosch, Darshan Singh, Suresh Narayanan, B Vicknasingam Kasinather, Erich Seifritz, Johannes Kornhuber, Boris B Quednow, Christian P Müller
A feature of human culture is that we can learn to consume chemical compounds, derived from natural plants or synthetic fabrication, for their psychoactive effects. These drugs change the mental state and/or the behavioral performance of an individual and can be instrumentalized for various purposes. After the emergence of a novel psychoactive substance (NPS) and a period of experimental consumption, personal and medical benefits and harm potential of the NPS can be estimated on evidence base. This may lead to a legal classification of the NPS, which may range from limited medical use, controlled availability up to a complete ban of the drug form publically accepted use...
2017: Frontiers in Psychiatry
https://www.readbyqxmd.com/read/28804451/behavioral-changes-over-time-following-ayahuasca-exposure-in-zebrafish
#2
Robson Savoldi, Daniel Polari, Jaquelinne Pinheiro-da-Silva, Priscila F Silva, Bruno Lobao-Soares, Mauricio Yonamine, Fulvio A M Freire, Ana C Luchiari
The combined infusion of Banisteriopsis caapi stem and Psychotria viridis leaves, known as ayahuasca, has been used for centuries by indigenous tribes. The infusion is rich in N, N-dimethyltryptamine (DMT) and monoamine oxidase inhibitors, with properties similar to those of serotonin. Despite substantial progress in the development of new drugs to treat anxiety and depression, current treatments have several limitations. Alternative drugs, such as ayahuasca, may shed light on these disorders. Here, we present time-course behavioral changes induced by ayahuasca in zebrafish, as first step toward establishing an ideal concentration for pre-clinical evaluations...
2017: Frontiers in Behavioral Neuroscience
https://www.readbyqxmd.com/read/28792478/marine-inspired-2-5-halo-1h-indol-3-yl-n-n-dimethylethanamines-as-modulators-of-serotonin-receptors-an-example-illustrating-the-power-of-bromine-as-part-of-the-uniquely-marine-chemical-space
#3
Mohamed A Ibrahim, Abir T El-Alfy, Kelly Ezel, Mohamed O Radwan, Abbas G Shilabin, Anna J Kochanowska-Karamyan, Howaida I Abd-Alla, Masami Otsuka, Mark T Hamann
In previous studies, we have isolated several marine indole alkaloids and evaluated them in the forced swim test (FST) and locomotor activity test, revealing their potential as antidepressant and sedative drug leads. Amongst the reported metabolites to display such activities was 5-bromo-N,N-dimethyltryptamine. Owing to the importance of the judicious introduction of halogens into drug candidates, we synthesized two series built on a 2-(1H-indol-3-yl)-N,N-dimethylethanamine scaffold with different halogen substitutions...
August 9, 2017: Marine Drugs
https://www.readbyqxmd.com/read/28686543/a-physician-s-attempt-to-self-medicate-bipolar-depression-with-n-n-dimethyltryptamine-dmt
#4
Tanida Brown, Wanda Shao, Shehzad Ayub, David Chong, Christian Cornelius
N,N-dimethyltryptamine (DMT) is a psychoactive substance that has been gaining popularity in therapeutic and recreational use. This is a case of a physician who chronically took DMT augmented with phenelzine in an attempt to self-medicate refractory bipolar depression. His presentation of altered mental status, mania, and psychosis is examined in regards to his DMT use. This case discusses DMT, the possible uses of DMT, and the theorized mechanism of DMT in psychosis and treatment of depression, particularly involving its agonist activity at 5-HT1A, 5-HT2A, and 5-HT2C...
July 7, 2017: Journal of Psychoactive Drugs
https://www.readbyqxmd.com/read/28640347/psychotria-viridis-chemical-constituents-from-leaves-and-biological-properties
#5
Débora B S Soares, Lucienir P Duarte, André D Cavalcanti, Fernando C Silva, Ariadne D Braga, Miriam T P Lopes, Jacqueline A Takahashi, Sidney A Vieira-Filho
The phytochemical study of hexane, chloroform and methanol extracts from leaves of Psychotria viridis resulted in the identification of: the pentacyclic triterpenes, ursolic and oleanolic acid; the steroids, 24-methylene-cycloartanol, stigmasterol and β-sitosterol; the glycosylated steroids 3-O-β-D-glucosyl-β-sitosterol and 3-O-β-D-glucosyl-stigmasterol; a polyunsaturated triterpene, squalene; the esters of glycerol, 1-palmitoylglycerol and triacylglycerol; a mixture of long chain hydrocarbons; the aldehyde nonacosanal; the long chain fat acids hentriacontanoic, hexadecanoic and heptadenoic acid; the ester methyl heptadecanoate; the 4-methyl-epi-quinate and two indole alkaloids, N,N-dimethyltryptamine (DMT) and N-methyltryptamine...
April 2017: Anais da Academia Brasileira de Ciências
https://www.readbyqxmd.com/read/28625125/dreams-and-psychedelics-neurophenomenological-comparison-and-therapeutic-implications
#6
Rainer Kraehenmann
A resurgence of neurobiological and clinical research is currently underway into the therapeutic potential of serotonergic or 'classical' psychedelics, such as the prototypical psychedelic drug lysergic acid diethylamide (LSD), psilocybin (4-phosphoryloxy-N,N-dimethyltryptamine), and ayahuasca - a betacarboline- and dimethyltryptamine (DMT)-containing Amazonian beverage. However, the mechanisms of therapeutic action are still not fully explained. Given that an altered state of consciousness is a common denominator that characterizes all classical psychedelics and given that both rapid eye movement sleep (REMS) and psychedelics modulate perception, mental imagery, emotion activation, fear memory extinction, and sense of self and body, in the present article, these two states of consciousness are systematically compared, and therapeutically relevant conclusions are drawn based on available evidence...
June 18, 2017: Current Neuropharmacology
https://www.readbyqxmd.com/read/28602505/proposal-of-5-methoxy-n-methyl-n-isopropyltryptamine-consumption-biomarkers-through-identification-of-in-vivo-metabolites-from-mice
#7
D Fabregat-Safont, M Barneo-Muñoz, F Martinez-Garcia, J V Sancho, F Hernández, M Ibáñez
New psychoactive substances (NPS) are a new breed of synthetically produced substances designed to mimic the effects of traditional illegal drugs. Synthetic cannabinoids and synthetic cathinones are the two most common groups, which try to mimic the effects of the natural compounds (9)Δ-tetrahydrocannabinol and cathinone, respectively. Similarly, synthetic tryptamines are designer compounds which are based on the compounds psilocin, N,N-dimethyltryptamine and 5-methoxy-N,N-dimethyltryptamine found in some mushrooms...
June 5, 2017: Journal of Chromatography. A
https://www.readbyqxmd.com/read/28540034/ayahuasca-dimethyltryptamine-and-psychosis-a-systematic-review-of-human-studies
#8
REVIEW
Rafael G Dos Santos, José Carlos Bouso, Jaime E C Hallak
Ayahuasca is a hallucinogen brew traditionally used for ritual and therapeutic purposes in Northwestern Amazon. It is rich in the tryptamine hallucinogens dimethyltryptamine (DMT), which acts as a serotonin 5-HT2A agonist. This mechanism of action is similar to other compounds such as lysergic acid diethylamide (LSD) and psilocybin. The controlled use of LSD and psilocybin in experimental settings is associated with a low incidence of psychotic episodes, and population studies corroborate these findings. Both the controlled use of DMT in experimental settings and the use of ayahuasca in experimental and ritual settings are not usually associated with psychotic episodes, but little is known regarding ayahuasca or DMT use outside these controlled contexts...
April 2017: Therapeutic Advances in Psychopharmacology
https://www.readbyqxmd.com/read/28525587/assessing-the-psychedelic-after-glow-in-ayahuasca-users-post-acute-neurometabolic-and-functional-connectivity-changes-are-associated-with-enhanced-mindfulness-capacities
#9
Frederic Sampedro, Mario de la Fuente Revenga, Marta Valle, Natalia Roberto, Elisabet Domínguez-Clavé, Matilde Elices, Luís Eduardo Luna, José Alexandre S Crippa, Jaime E C Hallak, Draulio B de Araujo, Pablo Friedlander, Steven A Barker, Enrique Álvarez, Joaquim Soler, Juan C Pascual, Amanda Feilding, Jordi Riba
Background: Ayahuasca is a plant tea containing the psychedelic 5-HT2A agonist N,N-dimethyltryptamine and harmala monoamine-oxidase inhibitors. Acute administration leads to neurophysiological modifications in brain regions of the default mode network, purportedly through a glutamatergic mechanism. Post-acutely, ayahuasca potentiates mindfulness capacities in volunteers and induces rapid and sustained antidepressant effects in treatment-resistant patients. However, the mechanisms underlying these fast and maintained effects are poorly understood...
September 1, 2017: International Journal of Neuropsychopharmacology
https://www.readbyqxmd.com/read/28517235/new-psychoactive-substances-purchasing-and-supply-patterns-in-australia
#10
Rachel Sutherland, Raimondo Bruno, Amy Peacock, Paul Dietze, Courtney Breen, Lucinda Burns, Monica J Barratt
OBJECTIVE: To examine the purchasing and supply patterns of new psychoactive substance (NPS) consumers in Australia. METHOD: Data were obtained from a self-selected sample of 296 past-year NPS consumers, with comparisons made across dimethyltryptamine (n = 104), 2C-x (n = 59), NBOMe (n = 27), and synthetic cannabinoid (n = 22) users. RESULTS: Most consumers (58%) nominated a friend as their main NPS source, and almost half (46%) reported that they had supplied NPS to others in the past year (predominantly "social supply")...
May 18, 2017: Human Psychopharmacology
https://www.readbyqxmd.com/read/28406320/underestimated-impact-of-novel-psychoactive-substances-laboratory-confirmation-of-recreational-drug-toxicity-in-oslo-norway
#11
MULTICENTER STUDY
Odd Martin Vallersnes, Per Sverre Persett, Elisabeth Leere Øiestad, Ritva Karinen, Fridtjof Heyerdahl, Knut Erik Hovda
CONTEXT: Recreational drug toxicity is frequent. Availability of new psychoactive substances is steadily increasing. However, data with verified analyses from clinical settings are limited. To evaluate the impact of novel psychoactive substances (NPS) on recreational drug toxicity in Oslo, Norway, we analysed samples from a selection of patients. METHODS: All the patients presenting with recreational drug toxicity at the Oslo Accident and Emergency Outpatient Clinic (OAEOC) and at the Oslo University Hospital (OUH) were registered from April through September 2014...
August 2017: Clinical Toxicology
https://www.readbyqxmd.com/read/28378435/a-single-administration-of-the-hallucinogen-4-acetoxy-dimethyltryptamine-prevents-the-shift-to-a-drug-dependent-state-and-the-expression-of-withdrawal-aversions-in-rodents
#12
Hector Vargas-Perez, Taryn E Grieder, Ryan Ting-A-Kee, Geith Maal-Bared, Michal Chwalek, Derek van der Kooy
Despite several studies suggesting the therapeutic use of 5-hydroxytryptamine receptors type 2A (5-HT2A ) agonists in the treatment of substance use disorders, the neurobiological basis accounting for such effects are still unknown. It has been observed that chronic exposure to drugs of abuse produces molecular and cellular adaptations in ventral tegmental area (VTA) neurons, mediated by brain-derived neurotrophic factor (BDNF). These BDNF-induced adaptations in the VTA are associated with the establishment of aversive withdrawal motivation that leads to a drug-dependent state...
April 4, 2017: European Journal of Neuroscience
https://www.readbyqxmd.com/read/28315276/the-sigma-1-receptor-a-therapeutic-target-for-the-treatment-of-als
#13
Timur A Mavlyutov, Erin M Baker, Tasher M Losenegger, Jaimie R Kim, Brian Torres, Miles L Epstein, Arnold E Ruoho
The membrane bound 223 amino acid Sigma-1 Receptor (S1R) serves as a molecular chaperone and functional regulator of many signaling proteins. Spinal cord motor neuron activation occurs, in part, via large ventral horn cholinergic synapses called C-boutons/C-terminals. Chronic excitation of motor neurons and alterations in C-terminals has been associated with Amyotrophic Lateral Sclerosis (ALS ). The S1R has an important role in regulating motor neuron function. High levels of the S1R are localized in postsynaptic endoplasmic reticulum (ER) subsurface cisternae within 10-20 nm of the plasma membrane that contain muscarinic type 2 acetylcholine receptors (M2AChR), calcium activated potassium channels (Kv2...
2017: Advances in Experimental Medicine and Biology
https://www.readbyqxmd.com/read/28105971/determination-of-tryptamines-and-%C3%AE-carbolines-in-ayahuasca-beverage-consumed-during-brazilian-religious-ceremonies
#14
Mônica Cardoso Santos, Sandro Navickiene, Alain Gaujac
Ayahuasca is a potent hallucinogenic beverage prepared from Banisteriopsis caapi in combination with other psychoactive plants. N,N-dimethyltryptamine, tryptamine, harmine, harmaline, harmalol, and tetrahydroharmine were quantified in ayahuasca samples using a simple and low-cost method based on SPE and LC with UV diode-array detection. The experimental variables that affect the SPE method, such as type of solid phase and nature of solvent, were optimized. The method showed good linearity (r > 0.9902) and repeatability (RSD < 0...
May 1, 2017: Journal of AOAC International
https://www.readbyqxmd.com/read/27900674/serotonergic-hallucinogen-induced-visual-perceptual-alterations
#15
Michael Kometer, Franz X Vollenweider
Serotonergic hallucinogens, such as lysergic acid diethylamide (LSD), psilocybin, and N,N-dimethyltryptamine (DMT), are famous for their capacity to temporally and profoundly alter an individual's visual experiences. These visual alterations show consistent attributes despite large inter- and intra-individual variances. Many reports document a common perception of colors as more saturated, with increased brightness and contrast in the environment ("Visual Intensifications"). Environmental objects might be altered in size ("Visual illusions") or take on a modified and special meaning for the subject ("Altered self-reference")...
November 30, 2016: Current Topics in Behavioral Neurosciences
https://www.readbyqxmd.com/read/27896660/ayahuasca-exposure-descriptive-analysis-of-calls-to-us-poison-control-centers-from-2005-to-2015
#16
C William Heise, Daniel E Brooks
BACKGROUND: Ayahuasca is a hallucinogenic plant preparation which usually contains the vine Banisteriopsis caapi and the shrub Psychotria viridis. This tea originates from the Amazon Basin where it is used in religious ceremonies. Because interest in these religious groups spreading as well as awareness of use of ayahuasca for therapeutic and recreational purposes, its use is increasing. Banisteriopsis caapi is rich in β-carbolines, especially harmine, tetrahydroharmine and harmaline, which have monoamine oxidase inhibiting (MAOI) activity...
November 28, 2016: Journal of Medical Toxicology: Official Journal of the American College of Medical Toxicology
https://www.readbyqxmd.com/read/27709018/development-of-a-mechanism-based-pharmacokinetic-pharmacodynamic-model-to-characterize-the-thermoregulatory-effects-of-serotonergic-drugs-in-mice
#17
Xi-Ling Jiang, Hong-Wu Shen, Donald E Mager, Stephan Schmidt, Ai-Ming Yu
We have shown recently that concurrent harmaline, a monoamine oxidase-A inhibitor (MAOI), potentiates serotonin (5-HT) receptor agonist 5-methoxy-N,N-dimethyltryptamine (5-MeO-DMT)-induced hyperthermia. The objective of this study was to develop an integrated pharmacokinetic/pharmacodynamic (PK/PD) model to characterize and predict the thermoregulatory effects of such serotonergic drugs in mice. Physiological thermoregulation was described by a mechanism-based indirect-response model with adaptive feedback control...
September 2016: Acta Pharmaceutica Sinica. B
https://www.readbyqxmd.com/read/27683542/the-endogenous-hallucinogen-and-trace-amine-n-n-dimethyltryptamine-dmt-displays-potent-protective-effects-against-hypoxia-via-sigma-1-receptor-activation-in-human-primary-ipsc-derived-cortical-neurons-and-microglia-like-immune-cells
#18
Attila Szabo, Attila Kovacs, Jordi Riba, Srdjan Djurovic, Eva Rajnavolgyi, Ede Frecska
N,N-dimethyltryptamine (DMT) is a potent endogenous hallucinogen present in the brain of humans and other mammals. Despite extensive research, its physiological role remains largely unknown. Recently, DMT has been found to activate the sigma-1 receptor (Sig-1R), an intracellular chaperone fulfilling an interface role between the endoplasmic reticulum (ER) and mitochondria. It ensures the correct transmission of ER stress into the nucleus resulting in the enhanced production of antistress and antioxidant proteins...
2016: Frontiers in Neuroscience
https://www.readbyqxmd.com/read/27471468/a-model-for-the-application-of-target-controlled-intravenous-infusion-for-a-prolonged-immersive-dmt-psychedelic-experience
#19
Andrew R Gallimore, Rick J Strassman
The state of consciousness induced by N,N-dimethyltryptamine (DMT) is one of the most extraordinary of any naturally-occurring psychedelic substance. Users consistently report the complete replacement of normal subjective experience with a novel "alternate universe," often densely populated with a variety of strange objects and other highly complex visual content, including what appear to be sentient "beings." The phenomenology of the DMT state is of great interest to psychology and calls for rigorous academic enquiry...
2016: Frontiers in Pharmacology
https://www.readbyqxmd.com/read/27470427/measuring-the-subjective-revisiting-the-psychometric-properties-of-three-rating-scales-that-assess-the-acute-effects-of-hallucinogens
#20
José Carlos Bouso, Eduardo José Pedrero-Pérez, Sam Gandy, Miguel Ángel Alcázar-Córcoles
OBJECTIVE: In the present study we explored the psychometric properties of three widely used questionnaires to assess the subjective effects of hallucinogens: the Hallucinogen Rating Scale (HRS), the Mystical Experience Questionnaire (MEQ), and the Addiction Research Center Inventory (ARCI). METHODS: These three questionnaires were administered to a sample of 158 subjects (100 men) after taking ayahuasca, a hallucinogen whose main active component is N,N-dimethyltryptamine (DMT)...
September 2016: Human Psychopharmacology
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