Fortschritte der Neurologie · Psychiatrie
July 1, 2017
Tomislav Majić, Henrik Jungaberle, Timo Torsten Schmidt et al.
10 citations
Zusammenfassung Hintergrund Der Einsatz von serotonergen Halluzinogenen (Psychedelika) wie Lysergsäure-Diethylamid (LSD) und Psilocybin und Entaktogenen wie 3,4-Methylendioxymethamphetamin (MDMA) im Rahmen von Psychotherapie ist in den letzten Jahren wieder zunehmend ins Licht des wissenschaftlichen Interesses gerückt. Die vorliegende Arbeit fasst die aktuelle Evidenz zur substanzunterstützten...
Frontiers in Pharmacology
June 28, 2017
Patrick C. Dolder, Edna Grünblatt, Felix Müller et al.
12 citations
Rationale Renewed interest has been seen in the use of lysergic acid diethylamide (LSD) in psychiatric research and practice. The repeated use of LSD leads to tolerance that is believed to result from serotonin (5-HT) 5-HT2A receptor downregulation. In rats, daily LSD administration for 4 days decreased frontal cortex 5-HT2A receptor binding. Additionally, a single dose of LSD acutely increased...
Drug Testing and Analysis
June 5, 2017
Simon D. Brandt, Pierce V. Kavanagh, Brendan Twamley et al.
56 citations
Lysergic acid diethylamide (LSD) is perhaps one of the best‐known psychoactive substances and many structural modifications of this prototypical lysergamide have been investigated. Several lysergamides were recently encountered as ‘research chemicals’ or new psychoactive substances (NPS). Although lysergic acid morpholide (LSM‐775) appeared on the NPS market in 2013, there is disagreement in...
Neuropharmacology
June 2017
Alyssa F DeLarge, Laura L Erwin, Peter J Winsauer
Mephedrone (4-methylmethcathinone), a constituent of the recreational substances known as "bath salts", is a synthetic cathinone that can produce auditory and visual hallucinations, as well as problematic cardiovascular effects. This study compared the discriminative stimulus effects of mephedrone (0.32-10 mg/kg) with other prototypical drugs of abuse: cocaine (0.56-32 mg/kg), d-amphetamine...
Behavioural Pharmacology
June 1, 2017
Jeremy I Webster, David N. Harper, Susan Schenk
Studies that have attributed the discriminative stimulus effects of ±3,4-methylenedioxymethamphetamine (MDMA) to serotonergic mechanisms typically use a relatively low training dose of 1.5 mg/kg. The role of serotonin in the discriminative stimulus effects of higher doses of MDMA is, however, unknown. Separate groups of rats were trained to discriminate MDMA (1.5 or 3.0 mg/kg) from saline using...
Journal of Pharmacology and Experimental Therapeutics
June 2017
Anders A. Jensen, John D. Mccorvy, Sebastian Leth-Petersen et al.
Therapeutic interest in augmentation of 5-hydroxytryptamine2A (5-HT2A) receptor signaling has been renewed by the effectiveness of psychedelic drugs in the treatment of various psychiatric conditions. In this study, we have further characterized the pharmacological properties of the recently developed 5-HT2 receptor agonist N-2-hydroxybenzyl)-2,5-dimethoxy-4-cyanophenylethylamine (25CN-NBOH)...
Behavioural Brain Research
May 1, 2017
Akihiro Mouri, Yukihiro Noda, Minae Niwa et al.
3,4-Methylenedioxymethamphetamine (MDMA) is known to induce dependence and psychosis in humans. Brain-derived neurotrophic factor (BDNF) is involved in the synaptic plasticity and neurotrophy in midbrain dopaminergic neurons. This study aimed to investigate the role of BDNF in MDMA-induced dependence and psychosis. A single dose of MDMA (10mg/kg) induced BDNF mRNA expression in the prefrontal...
Neurochemistry International
May 2017
Linda D Mercer, Gavin C Higgins, Chew L Lau et al.
Toxicity of 3,4-methylenedioxymethamphetamine (MDMA) towards biogenic amine neurons is well documented and in primate brain predominantly affects serotonin (5-HT) neurons. MDMA induces damage of 5-HT axons and nerve fibres and intracytoplasmic inclusions. Whilst its pathobiology involves mitochondrially-mediated oxidative stress, we hypothesised MDMA possessed the capacity to activate...
The FASEB Journal
April 1, 2017
Melodi Ann Bowman, Melissa Vitela, W. Anthony Owens et al.
Twenty percent of adults are diagnosed with major depressive disorder, which is typically treated with selective serotonin reuptake inhibitors. However, this type of medication takes approximately six weeks to produce therapeutic effects. Recently, low doses of ketamine, a noncompetitive N‐methyl‐D‐aspartate (NMDA) receptor antagonist, have been shown to produce rapid and long‐lasting...
The FASEB Journal
April 1, 2017
Michael P Trahan, Sebastian Leth-Petersen, William E Fantegrossi
R (−)‐2,5‐Dimethoxy‐4‐iodoamphetamine (DOI) and other compounds with agonist affinity for serotonergic 5‐HT2A receptors are hallucinogenic drugs of abuse, but also have therapeutic potential in numerous neuropsychiatric conditions, including major depressive disorder, post‐traumatic stress disorder, and in the treatment of migraine and cluster headaches. Thus, commonly abused hallucinogens...
The FASEB Journal
April 1, 2017
Gerald Billac, Charles D. Nichols
There has been a recent resurgence of clinical interest in the application of psychedelic drugs for the treatment of various disease states. While the field is mostly focused on action within the central nervous system, previously published data from our lab supports the use of these 5‐hydroxytryptamine 2A receptor (5‐HT 2A R) agonists as modulators of the inflammatory pathway in the periphery...
The FASEB Journal
April 1, 2017
Thomas W. Flanagan, Melaine N. Sebastian, Charles D. Nichols
2 citations
Only recently has the full therapeutic value of serotonin [5‐hydroxytryptophan (5‐HT)] receptor activation begun to be explored. Currently there are two 5‐HT 2A receptor agonists in human clinical trials for the treatment of depression and obesity. An exciting new therapeutic avenue in which 5‐HT 2A agonists might be employed is the modulation of inflammation in allergic airways disease. Our...
Religion, Brain & Behavior
March 22, 2017
Andrew B. Newberg, Nancy Wintering, David B. Yaden et al.
19 citations
Spiritual retreats are a commonly used intensive program of meditation and prayer, along with other elements, designed to provide participants with opportunities for spiritual and psychological growth. While individual elements of such retreats have been studied, there have been no reports in the literature regarding the neurophysiological effects of these retreats. This preliminary study...
Journal of Medicinal Chemistry
March 15, 2017
Richard A Glennon
The phenylalkylamine, particularly the phenylethylamine, moiety is a common structural feature found embedded in many clinically approved agents. Greater still is its occurrence in drugs of abuse. The simplest phenylethylamine, 2-phenylethylamine itself, is without significant central action when administered at moderate doses, but fairly simple structural modifications profoundly impact its...
The International Journal of Neuropsychopharmacology
February 8, 2017
Alexander Bryson, Olivia Carter, Trevor R. Norman et al.
19 citations
Functional neurological disorders are frequently encountered in clinical practice. They have a poor prognosis and treatment options are limited. Their etiology is unknown, but leading theories propose a disturbance of somatic self-representation: the mind perceives dysfunction of a body region despite intact motor and sensory pathways. Central to this model is the concept of an abnormal...
Current Biology
February 6, 2017
Katrin H. Preller, Marcus Herdener, Thomas Pokorny et al.
A core aspect of the human self is the attribution of personal relevance to everyday stimuli enabling us to experience our environment as meaningful [1]. However, abnormalities in the attribution of personal relevance to sensory experiences are also critical features of many psychiatric disorders [2, 3]. Despite their clinical relevance, the neurochemical and anatomical substrates enabling...
Cell
January 26, 2017
Daniel Wacker, Sheng Wang, John D. Mccorvy et al.
466 citations
SUMMARY The prototypical hallucinogen LSD acts via serotonin receptors, and here we describe the crystal structure of LSD in complex with the human serotonin receptor 5-HT2B. The complex reveals conformational rearrangements to accommodate LSD, providing a structural explanation for the conformational selectivity of LSD’s key diethylamide moiety. LSD dissociates exceptionally slowly from both...
2017
F. H. Zakaria, Norhafidah Abu, Nasir Mohamad
he trend of drug use has changed tremendously in this millennium (Adnan et al., 2014). Over the past decade, opioids are among the primary drug of abuse in worldwide. However the trend towards using amphetamine-type stimulant (ATS) is notably increasing lately. Amphetamine-type stimulants are a group of drugs consisting mainly of amphetamine and metamphetamine; these include methcathinone,...
Neuropharmacology
January 2017
T H Pham, Indira Mendez-David, Céline Defaix et al.
Unlike classic serotonergic antidepressant drugs, ketamine, an NMDA receptor antagonist, exhibits a rapid and persistent antidepressant (AD) activity, at sub-anaesthetic doses in treatment-resistant depressed patients and in preclinical studies in rodents. The mechanisms mediating this activity are unclear. Here, we assessed the role of the brain serotonergic system in the AD-like activity of...
Doklady. Biochemistry and biophysics
2017
E V Kryukova, D S Lebedev, I A Ivanov et al.
Two low-molecular-weight compounds were isolated from the parotid gland secret of the toad Bufo bufo, which by absorption spectra and HPLC-MS/MS chromatography data correspond to di- and trimethyl derivatives of serotonin (5-hydorxytryptamine): bufotenine (confirmed by counter synthesis) and bufotenidine (5-HTQ). In experiments on competitive radioligand binding, these compounds showed a higher...