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MDMA RECEPTOR

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https://www.readbyqxmd.com/read/27773601/mdma-decreases-glutamic-acid-decarboxylase-gad-67-immunoreactive-neurons-in-the-hippocampus-and-increases-seizure-susceptibility-role-for-glutamate
#1
Courtney L Huff, Rachel L Morano, James P Herman, Bryan K Yamamoto, Gary A Gudelsky
3,4-Methylenedioxy-methamphetamine (MDMA) is a unique psychostimulant that continues to be a popular drug of abuse. It has been well documented that MDMA reduces markers of 5-HT axon terminals in rodents, as well as humans. A loss of parvalbumin-immunoreactive (IR) interneurons in the hippocampus following MDMA treatment has only been documented recently. In the present study, we tested the hypothesis that MDMA reduces glutamic acid decarboxylase (GAD) 67-IR, another biochemical marker of GABA neurons, in the hippocampus and that this reduction in GAD67-IR neurons and an accompanying increase in seizure susceptibility involve glutamate receptor activation...
December 2016: Neurotoxicology
https://www.readbyqxmd.com/read/27725273/mdma-ecstasy-oxytocin-and-vasopressin-modulate-social-preference-in-rats-a-role-for-handling-and-oxytocin-receptors
#2
Linnet Ramos, Callum Hicks, Alex Caminer, Kalliu Couto, Rajeshwar Narlawar, Michael Kassiou, Iain S McGregor
In laboratory rats, peripheral administration of the neuropeptides oxytocin (OT) and vasopressin (AVP) induces similar prosocial effects (i.e. increased adjacent lying) to the party drug 3,4-methylenedioxymethamphetamine (MDMA), which are sensitive to vasopressin V1A receptor (V1AR) antagonism. Here, we employed a social preference paradigm to further compare the prosocial effects of OT, AVP and MDMA. We also investigated the possible involvement of the V1AR and oxytocin receptor (OTR) in rodent social preference...
October 7, 2016: Pharmacology, Biochemistry, and Behavior
https://www.readbyqxmd.com/read/27665759/erratum-to-abuse-potential-of-methylenedioxymethamphetamine-mdma-and-its-derivatives-in-zebrafish-role-of-serotonin-5ht2-type-receptors
#3
Luisa Ponzoni, Daniela Braida, Mariaelvina Sala
No abstract text is available yet for this article.
September 26, 2016: Psychopharmacology
https://www.readbyqxmd.com/read/27650729/neurochemical-binding-profiles-of-novel-indole-and-benzofuran-mdma-analogues
#4
Jakob A Shimshoni, Ilan Winkler, Ezekiel Golan, David Nutt
3,4-Methylenedioxy-N-methylamphetamine (MDMA) has been shown to be effective in the treatment of post-traumatic stress disorder (PTSD) in numerous clinical trials. In the present study, we have characterized the neurochemical binding profiles of three MDMA-benzofuran analogues (1-(benzofuran-5-yl)-propan-2-amine, 5-APB; 1-(benzofuran-6-yl)-N-methylpropan-2-amine, 6-MAPB; 1-(benzofuran-5-yl)-N-methylpropan-2-amine, 5-MAPB) and one MDMA-indole analogue (1-(1H-indol-5-yl)-2-methylamino-propan-1-ol, 5-IT). These compounds were screened as potential second-generation anti-PTSD drugs, against a battery of human and non-human receptors, transporters, and enzymes, and their potencies as 5-HT2 receptor agonist and monoamine uptake inhibitors determined...
September 20, 2016: Naunyn-Schmiedeberg's Archives of Pharmacology
https://www.readbyqxmd.com/read/27608804/retraction-note-to-gene-expression-analysis-indicates-cb1-receptor-upregulation-in-the-hippocampus-and-neurotoxic-effects-in-the-frontal-cortex-3%C3%A2-weeks-after-single-dose-mdma-administration-in-dark-agouti-rats
#5
Peter Petschner, Viola Tamasi, Csaba Adori, Eszter Kirilly, Romeo D Ando, Laszlo Tothfalusi, Gyorgy Bagdy
No abstract text is available yet for this article.
2016: BMC Genomics
https://www.readbyqxmd.com/read/27538886/psychosis-associated-with-acute-recreational-drug-toxicity-a-european-case-series
#6
Odd Martin Vallersnes, Alison M Dines, David M Wood, Christopher Yates, Fridtjof Heyerdahl, Knut Erik Hovda, Isabelle Giraudon, Paul I Dargan
BACKGROUND: Psychosis can be associated with acute recreational drug and novel psychoactive substance (NPS) toxicity. However, there is limited data available on how common this is and which drugs are most frequently implicated. We describe a European case series of psychosis associated with acute recreational drug toxicity, and estimate the frequency of psychosis for different recreational drugs. METHODS: The European Drug Emergencies Network (Euro-DEN) collects data on presentations to Emergency Departments (EDs) with acute recreational drug and NPS toxicity at 16 centres in ten countries...
August 18, 2016: BMC Psychiatry
https://www.readbyqxmd.com/read/27506653/ritanserin-sensitive-receptors-modulate-the-prosocial-and-the-anxiolytic-effect-of-mdma-derivatives-dob-and-pma-in-zebrafish
#7
Luisa Ponzoni, Mariaelvina Sala, Daniela Braida
Little is known about the pharmacological effects of amphetamine derivatives. In the present study, the effect on social preference and anxiety-like behavior of 2,5-dimetoxy-4-bromo-amphetamine hydrobromide (DOB) and para-methoxyamphetamine (PMA), in comparison with 3,4 methylenedioxymethamphetamine (MDMA) was investigated in zebrafish, an emerging model to study emotional behavior in an inexpensive and quick manner. DOB (0.05-2mg/kg), PMA (0.0005-2mg/kg) or MDMA (0.25-20mg/kg), given i.m. to adult zebrafish, progressively increased the time spent in the proximity of nacre fish picture in a social preference test...
November 1, 2016: Behavioural Brain Research
https://www.readbyqxmd.com/read/27373168/comparative-effects-of-amphetamine-like-psychostimulants-on-rat-hippocampal-cell-genesis-at-different-developmental-ages
#8
Rubén García-Cabrerizo, M Julia García-Fuster
The aim of this study was to compare the effects of amphetamine-like psychostimulant drugs (i.e., MDMA, methamphetamine, D-amphetamine) on rat hippocampal cell genesis at different developmental ages (i.e., early adolescence vs. young adulthood) to determine if there were periods of vulnerability to drug-induced brain changes. Although adolescence is a period of great vulnerability to the neurochemical effects of specific drugs of abuse, several reports suggest that adult rats are more susceptible than adolescents to the negative effects of these drugs...
June 29, 2016: Neurotoxicology
https://www.readbyqxmd.com/read/27318987/abuse-potential-of-methylenedioxymethamphetamine-mdma-and-its-derivatives-in-zebrafish-role-of-serotonin-5ht2-type-receptors
#9
Luisa Ponzoni, Braida Daniela, Mariaelvina Sala
RATIONALE: The synthetic phenethylamines are recreational drugs known to produce psychostimulant effects. However, their abuse potential has not been widely studied. OBJECTIVES: Here, we investigated the rewarding and the hallucinatory effects of 2,5-dimetoxy-4-bromo-amphetamine hydrobromide (DOB) and para-methoxyamphetamine (PMA) in comparison with the classical 3,4-methylenedioxymethamphetamine (MDMA). In addition, the role of serotonin 5-HT2-like receptor on the abovementioned effects was evaluated...
August 2016: Psychopharmacology
https://www.readbyqxmd.com/read/27264435/serotonin-antagonists-fail-to-alter-mdma-self-administration-in-rats
#10
Susan Schenk, Jason Foote, Dane Aronsen, Natasha Bukholt, Quenten Highgate, Ross Van de Wetering, Jeremy Webster
Acute exposure to ±3,4-methylenedioxymethamphetamine (MDMA) preferentially increases release of serotonin (5-HT), and a role of 5-HT in many of the behavioral effects of acute exposure to MDMA has been demonstrated. A role of 5-HT in MDMA self-administration in rats has not, however, been adequately determined. Therefore, the present study measured the effect of pharmacological manipulation of some 5-HT receptor subtypes on self-administration of MDMA. Rats received extensive experience with self-administered MDMA prior to tests with 5-HT ligands...
September 2016: Pharmacology, Biochemistry, and Behavior
https://www.readbyqxmd.com/read/27216487/receptor-interaction-profiles-of-novel-psychoactive-tryptamines-compared-with-classic-hallucinogens
#11
Anna Rickli, Olivier D Moning, Marius C Hoener, Matthias E Liechti
The present study investigated interactions between the novel psychoactive tryptamines DiPT, 4-OH-DiPT, 4-OH-MET, 5-MeO-AMT, and 5-MeO-MiPT at monoamine receptors and transporters compared with the classic hallucinogens lysergic acid diethylamide (LSD), psilocin, N,N-dimethyltryptamine (DMT), and mescaline. We investigated binding affinities at human monoamine receptors and determined functional serotonin (5-hydroxytryptamine [5-HT]) 5-HT2A and 5-HT2B receptor activation. Binding at and the inhibition of human monoamine uptake transporters and transporter-mediated monoamine release were also determined...
August 2016: European Neuropsychopharmacology: the Journal of the European College of Neuropsychopharmacology
https://www.readbyqxmd.com/read/27156124/acute-toxicity-associated-with-the-recreational-use-of-the-novel-psychoactive-benzofuran-n-methyl-5-2-aminopropyl-benzofuran
#12
Katharina E Hofer, Katrin Faber, Daniel M Müller, Till Hauffe, Urs Wenger, Hugo Kupferschmidt, Christine Rauber-Lüthy
N-methyl-5-(2 aminopropyl)benzofuran (5-MAPB) is a novel psychoactive benzofuran, created by N-methylation of 5-(2-aminopropyl)benzofuran (5-APB), which shares structural features with methylenedioxymethamphetamine (MDMA). To our knowledge, no case of 5-MAPB-related toxicity has been published in the scientific literature. We report a case of oral 5-MAPB exposure confirmed by liquid chromatography-tandem mass spectrometry in a 24-year-old previously healthy white man. Observed symptoms and signs such as paleness, cold and clammy skin, hypertension, elevated high-sensitive troponin T level, tachycardia, ECG change, diaphoresis, mild hyperthermia, mydriasis, tremor, hyperreflexia, clonus, agitation, disorientation, hallucinations, convulsions, reduced level of consciousness, and creatine kinase level elevation (305 IU/L) were compatible with undesired effects related to 5-APB or MDMA exposure...
April 26, 2016: Annals of Emergency Medicine
https://www.readbyqxmd.com/read/27149913/neurotoxicity-screening-of-illicit-drugs-using-novel-methods-for-analysis-of-microelectrode-array-mea-recordings
#13
L Hondebrink, A H A Verboven, W S Drega, S Schmeink, M W G D M de Groot, R G D M van Kleef, F M J Wijnolts, A de Groot, J Meulenbelt, R H S Westerink
Annual prevalence of the use of common illicit drugs and new psychoactive substances (NPS) is high, despite the often limited knowledge on the health risks of these substances. Recently, cortical cultures grown on multi-well microelectrode arrays (mwMEAs) have been used for neurotoxicity screening of chemicals, pharmaceuticals, and toxins with a high sensitivity and specificity. However, the use of mwMEAs to investigate the effects of illicit drugs on neuronal activity is largely unexplored. We therefore first characterised the cortical cultures using immunocytochemistry and show the presence of astrocytes, glutamatergic and GABAergic neurons...
July 2016: Neurotoxicology
https://www.readbyqxmd.com/read/27079619/contractile-effects-of-3-4-methylenedioxymethamphetamine-on-the-human-internal-mammary-artery
#14
Sónia Silva, Félix Carvalho, Eduarda Fernandes, Manuel J Antunes, Maria Dulce Cotrim
Since the late 1980s numerous reports have detailed adverse reactions to the use of 3,4-methylenedioxymethamphetamine (MDMA) associated with cardiovascular collapse and sudden death, following ventricular tachycardia and hypertension. For a better understanding of the effects of MDMA on the cardiovascular system, it is critical to determine their effects at the vasculature level, including the transporter or neurotransmitter systems that are most affected at the whole range of drug doses. With this purpose in mind, the aim of our study was to evaluate the contractile effect of MDMA in the human internal mammary artery, the contribution of SERT for this effect and the responsiveness of this artery to 5-HT in the presence of MDMA...
August 2016: Toxicology in Vitro: An International Journal Published in Association with BIBRA
https://www.readbyqxmd.com/read/26875756/%C3%AE-9-tetrahydrocannabinol-like-effects-of-novel-synthetic-cannabinoids-in-mice-and-rats
#15
Michael B Gatch, Michael J Forster
RATIONALE: Novel cannabinoid compounds continue to be marketed as "legal" marijuana substitutes, even though little is known about their molecular and behavioral effects. OBJECTIVES: Six of these compounds (ADBICA, ADB-PINACA, THJ-2201, RCS-4, JWH-122, JWH-210) were tested for in vitro and in vivo cannabinoid-like effects to determine their abuse liability. METHODS: Binding to and functional activity at CB1 cannabinoid receptors was tested...
May 2016: Psychopharmacology
https://www.readbyqxmd.com/read/26856854/mdma-self-administration-fails-to-alter-the-behavioral-response-to-5-ht-1a-and-5-ht-1b-agonists
#16
Dane Aronsen, Susan Schenk
RATIONALE: Regular use of the street drug, ecstasy, produces a number of cognitive and behavioral deficits. One possible mechanism for these deficits is functional changes in serotonin (5-HT) receptors as a consequence of prolonged 3,4 methylenedioxymethamphetamine (MDMA)-produced 5-HT release. Of particular interest are the 5-HT(1A) and 5-HT(1B) receptor subtypes since they have been implicated in several of the behaviors that have been shown to be impacted in ecstasy users and in animals exposed to MDMA...
April 2016: Psychopharmacology
https://www.readbyqxmd.com/read/26856853/repeated-administration-of-the-5-ht%C3%A2-b-%C3%A2-a-agonist-ru-24969-facilitates-the-acquisition-of-mdma-self-administration-role-of-5-ht%C3%A2-a-and-5-ht%C3%A2-b-receptor-mechanisms
#17
Dane Aronsen, Natasha Bukholt, Susan Schenk
RATIONALE: 3,4 Methylenedioxymethamphetamine (MDMA) preferentially stimulates the release of serotonin (5-HT) that subsequently produces behavioral responses by activation of post-synaptic receptor mechanisms. The 5-HT1A and 5-HT1B receptors are both well localized to regulate dopamine (DA) release, and have been implicated in modulating the reinforcing effects of many drugs of abuse, but a role in acquisition of self-administration has not been determined. OBJECTIVES: This study was designed to determine the effect of pharmacological manipulation of 5-HT1A and 5-HT1B receptor mechanisms on the acquisition of MDMA self-administration...
April 2016: Psychopharmacology
https://www.readbyqxmd.com/read/26855234/meta-analysis-of-molecular-imaging-of-serotonin-transporters-in-ecstasy-polydrug-users
#18
REVIEW
Carl Alexander Roberts, Andrew Jones, Catharine Montgomery
We conducted a meta-analysis on the available data from studies investigating SERTs in ecstasy users and polydrug using controls. From 7 studies we compared data from 157 ecstasy users and 148 controls across 14 brain regions. The main effect suggested ecstasy/MDMA related SERT reductions (SMD=0.52, 95% CIs [0.40, 0.65]; Z=8.36, p<.01, I(2)=89%). A significant effect of subgroups (X(2)=37.41, df=13, p<.01, I(2)=65.3%) suggested differential effects across brain ROIs. Ecstasy users showed significant SERT reductions in 11 out of the 14 regions, including every neocortical and limbic region analysed...
April 2016: Neuroscience and Biobehavioral Reviews
https://www.readbyqxmd.com/read/26796595/prevention-of-drug-priming-and-cue-induced-reinstatement-of-mdma-seeking-behaviors-by-the-cb1-cannabinoid-receptor-antagonist-am251
#19
Yoko Nawata, Kiyoyuki Kitaichi, Tsuneyuki Yamamoto
BACKGROUND: 3,4-Methylenedioxymethamphetamine (MDMA), a methamphetamine (METH) derivative, exhibits METH-like actions at monoamine transporters and positive reinforcing effects in rodents and primates. The purposes of the present study were to determine whether cross-reinstatement would be observed between MDMA and METH and if the cannabinoid receptor, a receptor known to play critical roles in the brain reward system, could modulate MDMA craving. METHODS: Rats were trained to press a lever for intravenous MDMA (0...
March 1, 2016: Drug and Alcohol Dependence
https://www.readbyqxmd.com/read/26787430/oxytocin-receptor-gene-variation-predicts-subjective-responses-to-mdma
#20
Anya K Bershad, Jessica J Weafer, Matthew G Kirkpatrick, Margaret C Wardle, Melissa A Miller, Harriet de Wit
3,4-Methylenedioxymethamphetamine (MDMA, "ecstasy") enhances desire to socialize and feelings of empathy, which are thought to be related to increased oxytocin levels. Thus, variation in the oxytocin receptor gene (OXTR) may influence responses to the drug. Here, we examined the influence of a single OXTR nucleotide polymorphism (SNP) on responses to MDMA in humans. Based on findings that carriers of the A allele at rs53576 exhibit reduced sensitivity to oxytocin-induced social behavior, we hypothesized that these individuals would show reduced subjective responses to MDMA, including sociability...
December 2016: Social Neuroscience
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