Pharmacological profiles of aminoindanes, piperazines, and pipradrol derivatives [PDF]
Aminoindanes, piperazines, and pipradrol derivatives are novel psychoactive substances found in "Ecstasy" tablets as replacements for 3,4-methylenedioxymethamphetamine (MDMA) or substances sold as "ivory wave." The pharmacology of these MDMA- and ...
Hoener, Marius C. +4 more
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In vivo evidence for NMDA receptor mediated excitotoxicity in a murine genetic model of Huntington Disease [PDF]
N-methyl-D-aspartate receptor (NMDAR) mediated excitotoxicity is implicated as a proximate cause of neurodegeneration in Huntington Disease (HD). However, this hypothesis has not been tested rigorously in vivo. NMDAR NR2B-subunits are the predominant NR2
Joe Tsien +4 more
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Receptor interaction profiles of novel N-2-methoxybenzyl (NBOMe) derivatives of 2,5-dimethoxy-substituted phenethylamines (2C drugs) [PDF]
N-2-methoxybenzyl-phenethylamines (NBOMe drugs) are newly used psychoactive substances with poorly defined pharmacological properties. The aim of the present study was to characterize the receptor binding profiles of a series of NBOMe drugs compared with
Buchy, Danièle +5 more
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Yohimbine is a 5-HT1A agonist in rats in doses exceeding 1 mg/kg. [PDF]
Yohimbine is a prototypical alpha2-adrenergic receptor antagonist. Due to its relatively high selectivity, yohimbine is often used in experiments whose purpose is to examine the role of these receptors.
DiMicco, Joseph A. +3 more
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Azaadamantane Benzamide 5-HT4 Agonists: Gastrointestinal Prokinetic SC-54750 [PDF]
Azaadamantanone 1 was converted to a series of aminoazaadamantane benzamides 9a–d, which were profiled for serotonin receptor activity. Aminomethylazaadamantane SC-54750 is a potent 5-HT4 agonist and 5-HT3 antagonist with in vivo efficacy in ...
Becker, Daniel +3 more
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Improved synthesis of [ 11 C]methylaminobenzovesamicol [PDF]
An efficient two‐step synthesis of the potential cholinergic neuronal mapping tracer [ 11 C]methylaminobenzovesamicol (MABV) is described. A tert ‐butoxycarbonyl protecting group was used to activate the aniline nitrogen of aminobenzovesamicol toward ...
Ayyangar +16 more
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We tested the ability of the neuroleptic agent spiperone (8-[3-(p-fluorobenzoyl)propyl]-1-phenyl-1,3,8-triazaspiro-[4.5] decan-4- one) to influence the tissue swelling and leukocyte infiltration associated with T-cell--dependent immune responses, i.e., contact hypersensitivity reactions, in mice.
Sharpe, Richard J +4 more
openaire +2 more sources
Receptor interaction profiles of novel psychoactive tryptamines compared with classic hallucinogens [PDF]
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 ...
Hoener, Marius C. +3 more
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Aryltrimethylammonium trifluoromethanesulfonates as precursors to aryl [ 18 F]fluorides: Improved synthesis of [ 18 F]GBR‐13119 [PDF]
Aromatic nucleophilic substitution of various trimethylammonium trifluoromethanesulfonates with [ 18 F]fluoride has been evaluated. Fluorinations were studied over a temperature range of 45–165°C, with decay corrected yields ranging from 20–80%.
Angelini +13 more
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Regulation of Neuromodulator Receptor Efficacy - Implications for Whole-Neuron and Synaptic Plasticity [PDF]
Membrane receptors for neuromodulators (NM) are highly regulated in their distribution and efficacy - a phenomenon which influences the individual cell's response to central signals of NM release.
Scheler, Gabriele
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