Search Results - "Canal, Clinton E"
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Activity of Mitragyna speciosa (“Kratom”) Alkaloids at Serotonin Receptors
Published in Journal of medicinal chemistry (23-09-2021)“…Kratom alkaloids have mostly been evaluated for their opioid activity but less at other targets that could contribute to their physiological effects. Here, we…”
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Amnesia produced by altered release of neurotransmitters after intraamygdala injections of a protein synthesis inhibitor
Published in Proceedings of the National Academy of Sciences - PNAS (24-07-2007)“…Amnesia produced by protein synthesis inhibitors such as anisomycin provides major support for the prevalent view that the formation of long-lasting memories…”
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The serotonin 2C receptor potently modulates the head-twitch response in mice induced by a phenethylamine hallucinogen
Published in Psychopharmacologia (01-04-2010)“…Rationale Hallucinogenic serotonin 2A (5-HT 2A ) receptor partial agonists, such as (±)-1-(2,5-dimethoxy-4-iodophenyl)-2-aminopropane hydrochloride (DOI),…”
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“Selective” serotonin 5-HT2A receptor antagonists
Published in Biochemical pharmacology (01-06-2022)“…[Display omitted] Blockade of the serotonin 5-HT2A G protein-coupled receptor (5-HT2AR) is a fundamental pharmacological characteristic of numerous…”
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Altered brain serotonin 5-HT1A receptor expression and function in juvenile Fmr1 knockout mice
Published in Neuropharmacology (01-03-2024)“…There are no approved pharmacotherapies for fragile X syndrome (FXS), a rare neurodevelopmental disorder caused by a mutation in the FMR1 promoter region that…”
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Classics in Chemical Neuroscience: Aripiprazole
Published in ACS chemical neuroscience (21-06-2017)“…Aripiprazole was the first antipsychotic developed to possess agonist properties at dopamine D2 autoreceptors, a groundbreaking strategy that presented a new…”
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Targeting 5-HT 1A Receptors to Correct Perineuronal Net and Social Behavioral Deficits in Fmr1 Knockout Mice, a Model of Fragile X Syndrome
Published in The FASEB journal (01-05-2022)“…Fragile X syndrome (FXS), caused by FMR1gene silencing and subsequent loss of the RNA-binding protein FMRP, is the leading monogenic cause of intellectual…”
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The serotonin 5-HT2C receptor and the non-addictive nature of classic hallucinogens
Published in Journal of Psychopharmacology (01-01-2017)“…Classic hallucinogens share pharmacology as serotonin 5-HT2A, 5-HT2B, and 5-HT2C receptor agonists. Unique among most other Schedule 1 drugs, they are…”
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Structure-Activity Relationship Study of Psychostimulant Synthetic Cathinones Reveals Nanomolar Antagonist Potency of α-Pyrrolidinohexiophenone at Human Muscarinic M 2 Receptors
Published in ACS chemical neuroscience (18-03-2020)“…Synthetic cathinones (SCs) are designer, psychostimulant drugs of abuse that primarily act on monoamine transporters; little is known about their off-target…”
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The Need To Improve Reporting of the Pharmacological Action of New Molecules
Published in ACS chemical neuroscience (19-01-2022)“…The molecular characterization of bioactive molecules, for example, small molecules targeting G-protein-coupled receptors, is evolving in complexity, impacting…”
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Structure–Activity Relationship Study of Psychostimulant Synthetic Cathinones Reveals Nanomolar Antagonist Potency of α‑Pyrrolidinohexiophenone at Human Muscarinic M2 Receptors
Published in ACS chemical neuroscience (18-03-2020)“…Synthetic cathinones (SCs) are designer, psychostimulant drugs of abuse that primarily act on monoamine transporters; little is known about their off-target…”
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Spontaneous seizures in adult Fmr1 knockout mice: FVB.129P2-Pde6b+Tyrc-chFmr1tm1Cgr/J
Published in Epilepsy research (01-05-2022)“…The prevalence of seizures in individuals with fragile X syndrome (FXS) is ~25%; however, there are no reports of spontaneous seizures in the Fmr1 knockout…”
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Targeting 5‐HT1A Receptors to Correct Neuronal Hyperexcitability in Fmr1 Knockout Mice
Published in The FASEB journal (01-05-2022)“…Fragile X syndrome (FXS)—caused by FMR1 gene silencing—is a severe neurodevelopmental disorder characterized by intellectual disabilities that are often…”
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Spontaneous seizures in adult Fmr1 knockout mice: FVB.129P2-Pde6b+ Tyr Fmr1/J
Published in Epilepsy research (01-05-2022)Get full text
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Ligand-directed serotonin 5-HT2C receptor desensitization and sensitization
Published in European journal of pharmacology (05-04-2019)“…Exposure of G protein–coupled receptors (GPCRs) to agonists can desensitize receptor signaling and lead to drug tolerance, whereas inverse agonists can…”
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Effects of the second-generation "bath salt" cathinone alpha-pyrrolidinopropiophenone (α-PPP) on behavior and monoamine neurochemistry in male mice
Published in Psychopharmacology (01-03-2019)“…Rationale Synthetic cathinones (“bath salts”) are β-ketone analogs of amphetamines, yet few studies have examined their potential neurotoxic effects. Objective…”
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Impact of RNA editing on functions of the serotonin 2C receptor in vivo
Published in Frontiers in neuroscience (01-01-2010)“…Transcripts encoding 5-HT(2C) receptors are modified posttranscriptionally by RNA editing, generating up to 24 protein isoforms. In recombinant cells, the…”
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Synthesis and Structure-Activity Relationships of 2,5-Dimethoxy-4-Substituted Phenethylamines and the Discovery of CYB210010: A Potent, Orally Bioavailable and Long-Acting Serotonin 5-HT 2 Receptor Agonist
Published in Journal of medicinal chemistry (25-04-2024)“…Structure-activity studies of 4-substituted-2,5-dimethoxyphenethylamines led to the discovery of 2,5-dimethoxy-4-thiotrifluoromethylphenethylamines, including…”
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Synthesis and Structure–Activity Relationships of 2,5-Dimethoxy-4-Substituted Phenethylamines and the Discovery of CYB210010: A Potent, Orally Bioavailable and Long-Acting Serotonin 5‑HT2 Receptor Agonist
Published in Journal of medicinal chemistry (25-04-2024)“…Structure–activity studies of 4-substituted-2,5-dimethoxyphenethylamines led to the discovery of 2,5-dimethoxy-4-thiotrifluoromethylphenethylamines,…”
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The Psychedelic N,N‑Dipropyltryptamine Prevents Seizures in a Mouse Model of Fragile X Syndrome via a Mechanism that Appears Independent of Serotonin and Sigma1 Receptors
Published in ACS pharmacology & translational science (13-10-2023)“…The serotonergic psychedelic psilocybin shows efficacy in treating neuropsychiatric disorders, though the mechanism(s) underlying its therapeutic effects…”
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