Search Results - "GLENNON, Richard A"
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Predicting new molecular targets for known drugs
Published in Nature (London) (12-11-2009)“…Although drugs are intended to be selective, at least some bind to several physiological targets, explaining side effects and efficacy. Because many…”
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Binding and functional structure-activity similarities of 4-substituted 2,5-dimethoxyphenyl isopropylamine analogues at 5-HT2A and 5-HT2B serotonin receptors
Published in Frontiers in pharmacology (24-01-2023)“…Certain 4-substituted analogs of 1-(2,5-dimethoxyphenyl)isopropylamine (2,5-DMA) are psychoactive classical hallucinogens or serotonergic psychedelic agents…”
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“Deconstruction” of the Abused Synthetic Cathinone Methylenedioxypyrovalerone (MDPV) and an Examination of Effects at the Human Dopamine Transporter
Published in ACS chemical neuroscience (18-12-2013)“…Synthetic cathinones, β-keto analogues of amphetamine (or, more correctly, of phenylalkylamines), represent a new and growing class of abused substances…”
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Electrical coupling between the human serotonin transporter and voltage-gated Ca2+ channels
Published in Cell calcium (Edinburgh) (01-07-2014)“…Graphical abstract…”
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Neurobiology of 3,4-Methylenedioxypyrovalerone (MDPV) and α-Pyrrolidinovalerophenone (α-PVP)
Published in Brain research bulletin (01-09-2016)“…Highlights • Nomenclature of synthetic cathinones • Mechanism of action of MDPV and α PVP • Structure activity relationships for action as DAT reuptake…”
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3,4-methylenedioxymethamphetamine (MDMA, "Ecstasy") induces fenfluramine-like proliferative actions on human cardiac valvular interstitial cells in vitro
Published in Molecular pharmacology (01-06-2003)“…Recent findings have implicated the 5-hydroxytryptamine 2B (5-HT2B) serotonin receptor in mediating the heart valve fibroplasia [valvular heart disease (VHD)]…”
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A strategy to prioritize emerging drugs of abuse for analysis: Abuse liability testing using intracranial self-stimulation (ICSS) in rats and validation with α-pyrrolidinohexanophenone (α-PHP)
Published in Emerging trends in drugs, addictions, and health (2021)“…Novel psychoactive substances (NPS) threaten public health and safety while also straining the limited resources of forensic laboratories. To efficiently…”
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The 2014 Philip S. Portoghese Medicinal Chemistry Lectureship: The “Phenylalkylaminome” with a Focus on Selected Drugs of Abuse
Published in Journal of medicinal chemistry (13-04-2017)“…The phenylalkylamine, particularly the phenylethylamine, moiety is a common structural feature found embedded in many clinically approved agents. Greater still…”
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Bath salts, mephedrone, and methylenedioxypyrovalerone as emerging illicit drugs that will need targeted therapeutic intervention
Published in Advances in pharmacology (1990) (2014)“…The term "synthetic cathinones" is fairly new, but, although the abuse of synthetic cathinones is a recent problem, research on cathinone analogs dates back…”
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In vitro characterization of ephedrine-related stereoisomers at biogenic amine transporters and the receptorome reveals selective actions as norepinephrine transporter substrates
Published in The Journal of pharmacology and experimental therapeutics (01-10-2003)“…Ephedrine is a long-studied stimulant available both as a prescription and over-the-counter medication, as well as an ingredient in widely marketed herbal…”
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Deconstruction of the α4β2 Nicotinic Acetylcholine Receptor Positive Allosteric Modulator Desformylflustrabromine
Published in Journal of medicinal chemistry (27-10-2011)“…Desformylflustrabromine (dFBr; 1), perhaps the first selective positive allosteric modulator of α4β2 neuronal nicotinic acetylcholine (nACh) receptors, was…”
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12
The medicinal chemistry of 5-HT6 receptor ligands with a focus on arylsulfonyltryptamine analogs
Published in Current topics in medicinal chemistry (01-04-2010)“…Arylsulfonyl analogs of aminopyrimidines (e.g. Ro 04-6790; 2), aminopyridines (e.g. Ro 63-0563; 3), 1-phenylpiperazines (e.g. SB-271046; 4), and tryptamines…”
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Molecular determinants for the interaction of the valvulopathic anorexigen norfenfluramine with the 5-HT2B receptor
Published in Molecular pharmacology (01-07-2005)“…S-(+)-Norfenfluramine (SNF)-an active metabolite of the now-banned anorexigen fenfluramine-has been implicated in the drug's appetite-suppressing actions and…”
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14
Quipazine: Classical hallucinogen? Novel psychedelic?
Published in Critical studies in media communication (02-05-2023)“…Quipazine, first identified in the 1960s, has been the topic of >1000 published papers. On the basis of available 5-HT2 serotonin receptor radioligand binding…”
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Mephedrone and methylenedioxypyrovalerone (MDPV), major constituents of “bath salts,” produce opposite effects at the human dopamine transporter
Published in Psychopharmacology (01-06-2013)“…Rationale Psychoactive “bath salts” represent a relatively new drug of abuse combination that was placed in Schedule I in October 2011. Two common ingredients…”
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1‑(2,5-Dimethoxy-4-iodophenyl)-2-aminopropane (DOI): From an Obscure to Pivotal Member of the DOX Family of Serotonergic Psychedelic Agents – A Review
Published in ACS pharmacology & translational science (14-06-2024)“…1-(2,5-Dimethoxy-4-iodophenyl)-2-aminopropane (DOI, or DOX where X = −I) was first synthesized in 1973 in a structure–activity study to explore the effect of…”
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Bath salts components mephedrone and methylenedioxypyrovalerone (MDPV) act synergistically at the human dopamine transporter
Published in British journal of pharmacology (01-04-2013)“…Background and Purpose Bath salts is the street name for drug combinations that contain synthetic cathinone analogues, among them possibly mephedrone (MEPH)…”
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Behavioral and biochemical investigations of bupropion metabolites
Published in European journal of pharmacology (01-08-2003)“…The stimulus effects of bupropion metabolites were examined in a drug discrimination procedure using (−)nicotine- and (+)amphetamine-trained rats. (+)- and (−)…”
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Synthetic cathinones: Chemical phylogeny, physiology, and neuropharmacology
Published in Life sciences (1973) (27-02-2014)“…This mini-review summarizes the history of cathinone and its synthesized derivatives from early records to the present day, including the appearance of…”
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Non-conserved residues dictate dopamine transporter selectivity for the potent synthetic cathinone and psychostimulant MDPV
Published in Neuropharmacology (01-12-2021)“…Clandestine chemists are currently exploiting the pyrrolidinophenone scaffold to develop new designer drugs that carry the risk of abuse and overdose. These…”
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