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Gongyin Ye - One of the best experts on this subject based on the ideXlab platform.
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larvae of the small white butterfly pieris rapae express a novel serotonin Receptor
Journal of Neurochemistry, 2014Co-Authors: Yixiang Qi, Yasu Wu, David Stanley, Jia Huang, Gongyin YeAbstract:: The biogenic amine serotonin (5-hydroxytryptamine, 5-HT) is a neurotransmitter in vertebrates and invertebrates. It acts in regulation and modulation of many physiological and behavioral processes through G-protein-coupled Receptors. Five 5-HT Receptor subtypes have been reported in Drosophila that share high similarity with mammalian 5-HT1A, 5-HT1B, 5-HT2A, 5-HT2B, and 5-HT7 Receptors. We isolated a cDNA (Pr5-HT8 ) from larval Pieris rapae, which shares relatively low similarity to the known 5-HT Receptor classes. After heterologous expression in HEK293 cells, Pr5-HT8 mediated increased [Ca(2+)]i in response to low concentrations ( 10 μM) of 5-HT. Dopamine, octopamine, and tyramine did not influence Receptor signaling. Pr5-HT8 was also activated by various 5-HT Receptor agonists including 5-methoxytryptamine, (±)-8-Hydroxy-2-(dipropylamino) tetralin, and 5-carboxamidotryptamine. Methiothepin, a non-selective 5-HT Receptor antagonist, activated Pr5-HT8 . WAY 10635, a 5-HT1A antagonist, but not SB-269970, SB-216641, or RS-127445, inhibited 5-HT-induced [Ca(2+)]i increases. We infer that Pr5-HT8 represents the first recognized member of a novel 5-HT Receptor class with a unique pharmacological profile. We found orthologs of Pr5-HT8 in some insect pests and vectors such as beetles and mosquitoes, but not in the genomes of honeybee or parasitoid wasps. This is likely to be an invertebrate-specific Receptor because there were no similar Receptors in mammals. We isolated a cDNA (Pr5-HT8) from larval Pieris rapae, which shares relatively low similarity to the known GPCRs. After heterologous expression in HEK293 cells, Pr5-HT8 mediated increased [Ca(2+)]i in response to low concentrations (< 10 nM) of 5-HT and various 5-HT Receptor agonists. We found orthologs of Pr5-HT8 in some insect pests and vectors such as beetles and mosquitoes, but not in the genomes of honeybee, parasitoid wasps, or mammals.
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larvae of the small white butterfly pieris rapae express a novel serotonin Receptor
Journal of Neurochemistry, 2014Co-Authors: Yixiang Qi, Yasu Wu, David Stanley, Jia Huang, Gongyin YeAbstract:: The biogenic amine serotonin (5-hydroxytryptamine, 5-HT) is a neurotransmitter in vertebrates and invertebrates. It acts in regulation and modulation of many physiological and behavioral processes through G-protein-coupled Receptors. Five 5-HT Receptor subtypes have been reported in Drosophila that share high similarity with mammalian 5-HT1A, 5-HT1B, 5-HT2A, 5-HT2B, and 5-HT7 Receptors. We isolated a cDNA (Pr5-HT8 ) from larval Pieris rapae, which shares relatively low similarity to the known 5-HT Receptor classes. After heterologous expression in HEK293 cells, Pr5-HT8 mediated increased [Ca(2+)]i in response to low concentrations ( 10 μM) of 5-HT. Dopamine, octopamine, and tyramine did not influence Receptor signaling. Pr5-HT8 was also activated by various 5-HT Receptor agonists including 5-methoxytryptamine, (±)-8-Hydroxy-2-(dipropylamino) tetralin, and 5-carboxamidotryptamine. Methiothepin, a non-selective 5-HT Receptor antagonist, activated Pr5-HT8 . WAY 10635, a 5-HT1A antagonist, but not SB-269970, SB-216641, or RS-127445, inhibited 5-HT-induced [Ca(2+)]i increases. We infer that Pr5-HT8 represents the first recognized member of a novel 5-HT Receptor class with a unique pharmacological profile. We found orthologs of Pr5-HT8 in some insect pests and vectors such as beetles and mosquitoes, but not in the genomes of honeybee or parasitoid wasps. This is likely to be an invertebrate-specific Receptor because there were no similar Receptors in mammals. We isolated a cDNA (Pr5-HT8) from larval Pieris rapae, which shares relatively low similarity to the known GPCRs. After heterologous expression in HEK293 cells, Pr5-HT8 mediated increased [Ca(2+)]i in response to low concentrations (< 10 nM) of 5-HT and various 5-HT Receptor agonists. We found orthologs of Pr5-HT8 in some insect pests and vectors such as beetles and mosquitoes, but not in the genomes of honeybee, parasitoid wasps, or mammals.
Kenner C Rice - One of the best experts on this subject based on the ideXlab platform.
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modification of the behavioral effects of morphine in rats by serotonin 5 ht 1a and 5 ht2a Receptor agonists antinociception drug discrimination and locomotor activity
Psychopharmacology, 2013Co-Authors: Aparna Shah, Sunny K Patel, Kenner C RiceAbstract:Rationale Indirect-acting serotonin (5-HT) Receptor agonists can enhance the antinociceptive effects of morphine; however, the specific 5-HT Receptor subtype(s) mediating this enhancement is not established.
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effects of serotonin 5 ht 1a and 5 ht2a Receptor agonists on schedule controlled responding in rats drug combination studies
Psychopharmacology, 2011Co-Authors: Junxu Li, Kenner C Rice, Wouter Koek, Caroline CrockerAbstract:Rationale Indirect-acting serotonin (5-HT) Receptor agonists (e.g., selective 5-HT reuptake inhibitors [SSRI]) stimulate multiple 5-HT Receptors, although the role of particular Receptors as well as interaction(s) among different Receptors in the therapeutic effects of SSRIs is not fully understood.
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discriminative stimulus effects of 1 2 5 dimethoxy 4 methylphenyl 2 aminopropane in rhesus monkeys antagonism and apparent pa2 analyses
Journal of Pharmacology and Experimental Therapeutics, 2009Co-Authors: Kenner C RiceAbstract:Discriminative stimulus effects of the serotonin (5-HT) Receptor agonist 1-(2,5-dimethoxy-4-methylphenyl)-2-aminopropane (DOM) have been studied in rats and, more recently, in rhesus monkeys. This study examined DOM, 2,5-dimethoxy-4-(n)-propylthiophenethylamine (2C-T-7), and dipropyltryptamine hydrochloride (DPT) alone and in combination with three antagonists, MDL100907 [(±)2,3-dimethoxyphenyl-1-[2-(4-piperidine)-methanol]], ketanserin [3-[2-[4-(4-fluorobenzoyl)piperidin-1-yl]ethyl]-1H-quinazoline-2,4-dione], and ritanserin [6-[2-[4-[bis(4-fluorophenyl)methylidene]piperidin-1-yl]ethyl]-7-methyl-[1,3]thiazolo[2,3-b]pyrimidin-5-one], to identify the 5-HT Receptor subtype(s) that mediates the discriminative stimulus effects of these 5-HT Receptor agonists. Four adult rhesus monkeys discriminated between 0.32 mg/kg s.c. DOM and vehicle while responding under a fixed ratio 5 schedule of stimulus shock termination. DOM, 2C-T-7, and DPT dose-dependently increased responding on the DOM-associated lever. MDL100907 (0.001-0.01 mg/kg), ketanserin (0.01-0.1 mg/kg), and ritanserin (0.01-0.1 mg/kg) each shifted the dose-response curves of DOM, 2C-T-7, and DPT rightward in a parallel manner. Schild analysis of each drug combination was consistent with a simple, competitive, and reversible interaction. Similar apparent affinity (pA2) values were obtained for MDL100907 in combination with DOM (8.61), 2C-T-7 (8.58), or DPT (8.50), for ketanserin with DOM (7.67), 2C-T-7 (7.75), or DPT (7.71), and for ritanserin with DOM (7.65), 2C-T-7 (7.75), or DPT (7.65). Potency of antagonists in this study was correlated with binding affinity at 5-HT2A Receptors and not at 5-HT2C or α1 adrenergic Receptors. This study used Schild analysis to examine Receptor mechanisms mediating the discriminative stimulus effects of hallucinogenic drugs acting at 5-HT Receptors; results provide quantitative evidence for the predominant, if not exclusive, role of 5-HT2A Receptors in the discriminative stimulus effects of DOM, 2C-T-7, and DPT in rhesus monkeys.
Yixiang Qi - One of the best experts on this subject based on the ideXlab platform.
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larvae of the small white butterfly pieris rapae express a novel serotonin Receptor
Journal of Neurochemistry, 2014Co-Authors: Yixiang Qi, Yasu Wu, David Stanley, Jia Huang, Gongyin YeAbstract:: The biogenic amine serotonin (5-hydroxytryptamine, 5-HT) is a neurotransmitter in vertebrates and invertebrates. It acts in regulation and modulation of many physiological and behavioral processes through G-protein-coupled Receptors. Five 5-HT Receptor subtypes have been reported in Drosophila that share high similarity with mammalian 5-HT1A, 5-HT1B, 5-HT2A, 5-HT2B, and 5-HT7 Receptors. We isolated a cDNA (Pr5-HT8 ) from larval Pieris rapae, which shares relatively low similarity to the known 5-HT Receptor classes. After heterologous expression in HEK293 cells, Pr5-HT8 mediated increased [Ca(2+)]i in response to low concentrations ( 10 μM) of 5-HT. Dopamine, octopamine, and tyramine did not influence Receptor signaling. Pr5-HT8 was also activated by various 5-HT Receptor agonists including 5-methoxytryptamine, (±)-8-Hydroxy-2-(dipropylamino) tetralin, and 5-carboxamidotryptamine. Methiothepin, a non-selective 5-HT Receptor antagonist, activated Pr5-HT8 . WAY 10635, a 5-HT1A antagonist, but not SB-269970, SB-216641, or RS-127445, inhibited 5-HT-induced [Ca(2+)]i increases. We infer that Pr5-HT8 represents the first recognized member of a novel 5-HT Receptor class with a unique pharmacological profile. We found orthologs of Pr5-HT8 in some insect pests and vectors such as beetles and mosquitoes, but not in the genomes of honeybee or parasitoid wasps. This is likely to be an invertebrate-specific Receptor because there were no similar Receptors in mammals. We isolated a cDNA (Pr5-HT8) from larval Pieris rapae, which shares relatively low similarity to the known GPCRs. After heterologous expression in HEK293 cells, Pr5-HT8 mediated increased [Ca(2+)]i in response to low concentrations (< 10 nM) of 5-HT and various 5-HT Receptor agonists. We found orthologs of Pr5-HT8 in some insect pests and vectors such as beetles and mosquitoes, but not in the genomes of honeybee, parasitoid wasps, or mammals.
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larvae of the small white butterfly pieris rapae express a novel serotonin Receptor
Journal of Neurochemistry, 2014Co-Authors: Yixiang Qi, Yasu Wu, David Stanley, Jia Huang, Gongyin YeAbstract:: The biogenic amine serotonin (5-hydroxytryptamine, 5-HT) is a neurotransmitter in vertebrates and invertebrates. It acts in regulation and modulation of many physiological and behavioral processes through G-protein-coupled Receptors. Five 5-HT Receptor subtypes have been reported in Drosophila that share high similarity with mammalian 5-HT1A, 5-HT1B, 5-HT2A, 5-HT2B, and 5-HT7 Receptors. We isolated a cDNA (Pr5-HT8 ) from larval Pieris rapae, which shares relatively low similarity to the known 5-HT Receptor classes. After heterologous expression in HEK293 cells, Pr5-HT8 mediated increased [Ca(2+)]i in response to low concentrations ( 10 μM) of 5-HT. Dopamine, octopamine, and tyramine did not influence Receptor signaling. Pr5-HT8 was also activated by various 5-HT Receptor agonists including 5-methoxytryptamine, (±)-8-Hydroxy-2-(dipropylamino) tetralin, and 5-carboxamidotryptamine. Methiothepin, a non-selective 5-HT Receptor antagonist, activated Pr5-HT8 . WAY 10635, a 5-HT1A antagonist, but not SB-269970, SB-216641, or RS-127445, inhibited 5-HT-induced [Ca(2+)]i increases. We infer that Pr5-HT8 represents the first recognized member of a novel 5-HT Receptor class with a unique pharmacological profile. We found orthologs of Pr5-HT8 in some insect pests and vectors such as beetles and mosquitoes, but not in the genomes of honeybee or parasitoid wasps. This is likely to be an invertebrate-specific Receptor because there were no similar Receptors in mammals. We isolated a cDNA (Pr5-HT8) from larval Pieris rapae, which shares relatively low similarity to the known GPCRs. After heterologous expression in HEK293 cells, Pr5-HT8 mediated increased [Ca(2+)]i in response to low concentrations (< 10 nM) of 5-HT and various 5-HT Receptor agonists. We found orthologs of Pr5-HT8 in some insect pests and vectors such as beetles and mosquitoes, but not in the genomes of honeybee, parasitoid wasps, or mammals.
Connie Sanchez - One of the best experts on this subject based on the ideXlab platform.
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effects of serotonin in the hippocampus how ssris and multimodal antidepressants might regulate pyramidal cell function
Cns Spectrums, 2016Co-Authors: Elena Dale, Steven C Leiser, Alan L Pehrson, Gennady N Smagin, Theepica Jeyarajah, Yan Li, Christina Kurre Olsen, Connie SanchezAbstract:The hippocampus plays an important role in emotional and cognitive processing, and both of these domains are affected in patients with major depressive disorder (MDD). Extensive preclinical research and the notion that modulation of serotonin (5-HT) neurotransmission plays a key role in the therapeutic efficacy of selective serotonin reuptake inhibitors (SSRIs) support the view that 5-HT is important for hippocampal function in normal and disease-like conditions. The hippocampus is densely innervated by serotonergic fibers, and the majority of 5-HT Receptor subtypes are expressed there. Furthermore, hippocampal cells often co-express multiple 5-HT Receptor subtypes that can have either complementary or opposing effects on cell function, adding to the complexity of 5-HT neurotransmission. Here we review the current knowledge of how 5-HT, through its various Receptor subtypes, modulates hippocampal output and the activity of hippocampal pyramidal cells in rodents. In addition, we discuss the relevance of 5-HT modulation for cognitive processing in rodents and possible clinical implications of these results in patients with MDD. Finally, we review the data on how SSRIs and vortioxetine, an antidepressant with multimodal activity, affect hippocampal function, including cognitive processing, from both a preclinical and clinical perspective.
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serotonergic regulation of prefrontal cortical circuitries involved in cognitive processing a review of individual 5 ht Receptor mechanisms and concerted effects of 5 ht Receptors exemplified by the multimodal antidepressant vortioxetine
ACS Chemical Neuroscience, 2015Co-Authors: Steven C Leiser, Alan L Pehrson, Elena Dale, Gennady N Smagin, Connie SanchezAbstract:It has been known for several decades that serotonergic neurotransmission is a key regulator of cognitive function, mood, and sleep. Yet with the relatively recent discoveries of novel serotonin (5-HT) Receptor subtypes, as well as an expanding knowledge of their expression level in certain brain regions and localization on certain cell types, their involvement in cognitive processes is still emerging. Of particular interest are cognitive processes impacted in neuropsychiatric and neurodegenerative disorders. The prefrontal cortex (PFC) is critical to normal cognitive processes, including attention, impulsivity, planning, decision-making, working memory, and learning or recall of learned memories. Furthermore, serotonergic dysregulation within the PFC is implicated in many neuropsychiatric disorders associated with prominent symptoms of cognitive dysfunction. Thus, it is important to better understand the overall makeup of serotonergic Receptors in the PFC and on which cell types these Receptors mediate t...
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vortioxetine but not escitalopram or duloxetine reverses memory impairment induced by central 5 ht depletion in rats evidence for direct 5 ht Receptor modulation
European Neuropsychopharmacology, 2014Co-Authors: Jesper Borno Jensen, Gennady N Smagin, Connie Sanchez, Kristian Gaarn Du Jardin, Dekun Song, David P Budac, Alan L PehrsonAbstract:Depressed patients suffer from cognitive dysfunction, including memory deficits. Acute serotonin (5-HT) depletion impairs memory and mood in vulnerable patients. The investigational multimodal acting antidepressant vortioxetine is a 5-HT3 ,5 -HT 7 and 5-HT1D Receptor antagonist, 5-HT1B Receptor partial agonist, 5-HT1A Receptor agonist and 5-HT transporter (SERT) inhibitor that enhances memory in normal rats in novel object recognition (NOR) and conditioned fear (Mork et al., 2013). We hypothesized that vortioxetine's 5-HT Receptor mechanisms are involved in its memory effects, and therefore investigated these effects in 5-HT depleted rats. Four injections of the irreversible tryptophan hydroxylase inhibitor 4-chloro-DL-phenylalanine methyl ester hydrochloride (PCPA, 86 mg/kg, s.c.) induced 5-HT depletion, as measured in hippocampal homogenate and microdialysate. The effects of acute challenge with vortioxetine or the 5-HT releaser fenfluramine on extracellular 5-HT were measured in PCPA-treated and control rats. PCPA's effects on NOR and spontaneous alternation (SA) performance were assessed along with the effects of acute treatment with 5-hydroxy-L-tryptophan (5-HTP), vortioxetine, the selective 5-HT reuptake inhibitor escitalopram, or the 5-HT norepinephrine reuptake inhibitor duloxetine. SERT occupancies were estimated by ex vivo autoradiography. PCPA depleted central 5-HT by 490% in tissue and microdialysate, and impaired NOR and SA performance. Restoring central 5-HT with 5-HTP reversed these deficits. At similar SERT occupancies (490%) vortioxetine, but not escitalopram or duloxetine, restored memory performance. Acute fenfluramine significantly
Jia Huang - One of the best experts on this subject based on the ideXlab platform.
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larvae of the small white butterfly pieris rapae express a novel serotonin Receptor
Journal of Neurochemistry, 2014Co-Authors: Yixiang Qi, Yasu Wu, David Stanley, Jia Huang, Gongyin YeAbstract:: The biogenic amine serotonin (5-hydroxytryptamine, 5-HT) is a neurotransmitter in vertebrates and invertebrates. It acts in regulation and modulation of many physiological and behavioral processes through G-protein-coupled Receptors. Five 5-HT Receptor subtypes have been reported in Drosophila that share high similarity with mammalian 5-HT1A, 5-HT1B, 5-HT2A, 5-HT2B, and 5-HT7 Receptors. We isolated a cDNA (Pr5-HT8 ) from larval Pieris rapae, which shares relatively low similarity to the known 5-HT Receptor classes. After heterologous expression in HEK293 cells, Pr5-HT8 mediated increased [Ca(2+)]i in response to low concentrations ( 10 μM) of 5-HT. Dopamine, octopamine, and tyramine did not influence Receptor signaling. Pr5-HT8 was also activated by various 5-HT Receptor agonists including 5-methoxytryptamine, (±)-8-Hydroxy-2-(dipropylamino) tetralin, and 5-carboxamidotryptamine. Methiothepin, a non-selective 5-HT Receptor antagonist, activated Pr5-HT8 . WAY 10635, a 5-HT1A antagonist, but not SB-269970, SB-216641, or RS-127445, inhibited 5-HT-induced [Ca(2+)]i increases. We infer that Pr5-HT8 represents the first recognized member of a novel 5-HT Receptor class with a unique pharmacological profile. We found orthologs of Pr5-HT8 in some insect pests and vectors such as beetles and mosquitoes, but not in the genomes of honeybee or parasitoid wasps. This is likely to be an invertebrate-specific Receptor because there were no similar Receptors in mammals. We isolated a cDNA (Pr5-HT8) from larval Pieris rapae, which shares relatively low similarity to the known GPCRs. After heterologous expression in HEK293 cells, Pr5-HT8 mediated increased [Ca(2+)]i in response to low concentrations (< 10 nM) of 5-HT and various 5-HT Receptor agonists. We found orthologs of Pr5-HT8 in some insect pests and vectors such as beetles and mosquitoes, but not in the genomes of honeybee, parasitoid wasps, or mammals.
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larvae of the small white butterfly pieris rapae express a novel serotonin Receptor
Journal of Neurochemistry, 2014Co-Authors: Yixiang Qi, Yasu Wu, David Stanley, Jia Huang, Gongyin YeAbstract:: The biogenic amine serotonin (5-hydroxytryptamine, 5-HT) is a neurotransmitter in vertebrates and invertebrates. It acts in regulation and modulation of many physiological and behavioral processes through G-protein-coupled Receptors. Five 5-HT Receptor subtypes have been reported in Drosophila that share high similarity with mammalian 5-HT1A, 5-HT1B, 5-HT2A, 5-HT2B, and 5-HT7 Receptors. We isolated a cDNA (Pr5-HT8 ) from larval Pieris rapae, which shares relatively low similarity to the known 5-HT Receptor classes. After heterologous expression in HEK293 cells, Pr5-HT8 mediated increased [Ca(2+)]i in response to low concentrations ( 10 μM) of 5-HT. Dopamine, octopamine, and tyramine did not influence Receptor signaling. Pr5-HT8 was also activated by various 5-HT Receptor agonists including 5-methoxytryptamine, (±)-8-Hydroxy-2-(dipropylamino) tetralin, and 5-carboxamidotryptamine. Methiothepin, a non-selective 5-HT Receptor antagonist, activated Pr5-HT8 . WAY 10635, a 5-HT1A antagonist, but not SB-269970, SB-216641, or RS-127445, inhibited 5-HT-induced [Ca(2+)]i increases. We infer that Pr5-HT8 represents the first recognized member of a novel 5-HT Receptor class with a unique pharmacological profile. We found orthologs of Pr5-HT8 in some insect pests and vectors such as beetles and mosquitoes, but not in the genomes of honeybee or parasitoid wasps. This is likely to be an invertebrate-specific Receptor because there were no similar Receptors in mammals. We isolated a cDNA (Pr5-HT8) from larval Pieris rapae, which shares relatively low similarity to the known GPCRs. After heterologous expression in HEK293 cells, Pr5-HT8 mediated increased [Ca(2+)]i in response to low concentrations (< 10 nM) of 5-HT and various 5-HT Receptor agonists. We found orthologs of Pr5-HT8 in some insect pests and vectors such as beetles and mosquitoes, but not in the genomes of honeybee, parasitoid wasps, or mammals.
