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https://www.readbyqxmd.com/read/28443529/selective-attention-and-mismatch-negativity-in-antipsychotic-na%C3%A3-ve-first-episode-schizophrenia-patients-before-and-after-6-months-of-antipsychotic-monotherapy
#1
B Oranje, B Aggernaes, H Rasmussen, B H Ebdrup, B Y Glenthøj
BACKGROUND: Attention deficits have been frequently reported in schizophrenia. It has been suggested that treatment with second-generation antipsychotics can ameliorate these deficits. In this study, the influence of 6 months treatment with quetiapine, a compound with less affinity for dopamine D2 receptors than for serotonergic 5-HT2A receptors, on electrophysiological parameters of attention was investigated in a group of antipsychotic-naïve, first-episode schizophrenia patients compared with a group of age- and gender-matched healthy controls...
April 26, 2017: Psychological Medicine
https://www.readbyqxmd.com/read/28428755/pharmacological-analysis-of-the-anti-epileptic-mechanisms-of-fenfluramine-in-scn1a-mutant-zebrafish
#2
Jo Sourbron, Ilse Smolders, Peter de Witte, Lieven Lagae
Dravet syndrome (DS) is a genetic encephalopathy that is characterized by severe seizures and prominent co-morbidities (e.g., physical, intellectual disabilities). More than 85% of the DS patients carry an SCN1A mutation (sodium channel, voltage gated, type I alpha subunit). Although numerous anti-epileptic drugs have entered the market since 1990, these drugs often fail to adequately control seizures in DS patients. Nonetheless, current clinical data shows significant seizure reduction in DS patients treated with the serotonergic (5-hydroxytryptamine, 5-HT) drug fenfluramine (FA)...
2017: Frontiers in Pharmacology
https://www.readbyqxmd.com/read/28425496/3-4-methylenedioxymethamphetamine-increases-affiliative-behaviors-in-squirrel-monkeys-in-a-serotonin-2a-receptor-dependent-manner
#3
Elizabeth G Pitts, Adelaide R Minerva, Erika B Oliver, Jordan N Kohn, Meghan T Logun, Agnieszka Sulima, Kenner C Rice, Leonard L Howell
3,4-methylenedioxymethamphetamine (MDMA) increases sociality in humans and animals. Release of serotonin (5-HT) is thought to play an important role in the increase in social behaviors, but the mechanisms underlying these effects are poorly understood. Despite the advantages of nonhuman primate models, no studies have examined the mechanisms of the social effects of MDMA in nonhuman primates. The behavior and vocalizations of four group-housed squirrel monkeys were examined following administration of MDMA, its enantiomers, and methamphetamine...
April 20, 2017: Neuropsychopharmacology: Official Publication of the American College of Neuropsychopharmacology
https://www.readbyqxmd.com/read/28411124/m3-muscarinic-acetylcholine-receptor-facilitates-the-endocytosis-of-mu-opioid-receptor-mediated-by-morphine-independently-of-the-formation-of-heteromeric-complexes
#4
Juan F Lopez-Gimenez, Elisa Alvarez-Curto, Graeme Milligan
Morphine inefficiency to induce the internalization of mu opioid (MOP) receptors observed in numerous experimental models constitutes a paradigm of G-protein coupled receptor (GPCR) functional selectivity. We recently described that activation of Gαq/11 proteins through 5-HT2A serotonin receptors co-expressed in the same cells facilitates MOP receptor endocytosis promoted by morphine. In order to explore whether a different Gαq/11 coupled GPCR would emulate this effect, a double stable Flp-In T-REx HEK293 cell line permanently expressing MOP-YFP receptors along with FLAG-M3-Cerulean receptors expressed in an inducible manner was generated...
April 11, 2017: Cellular Signalling
https://www.readbyqxmd.com/read/28404690/pharmacologic-characterization-of-valbenazine-nbi-98854-and-its-metabolites
#5
Dimitri E Grigoriadis, Evan Smith, Sam R J Hoare, Ajay Madan, Haig Bozigian
The vesicular monoamine transporter 2 (VMAT2) is an integral presynaptic protein that regulates the packaging and subsequent release of dopamine and other monoamines from neuronal vesicles into the synapse. Valbenazine (NBI-98854), a novel compound that selectively inhibits VMAT2, is being developed for the treatment of tardive dyskinesia. Valbenazine is converted to two significant circulating metabolites in vivo, namely, (+)-α-dihydrotetrabenazine (R,R,R-DHTBZ) and a mono-oxy metabolite, NBI-136110. Radioligand binding studies were conducted to assess and compare valbenazine, tetrabenazine and their respective metabolites in their abilities to selectively and potently inhibit [(3)H]-DHTBZ binding to VMAT2 in rat striatal, rat forebrain, and human platelet homogenates...
April 12, 2017: Journal of Pharmacology and Experimental Therapeutics
https://www.readbyqxmd.com/read/28401524/chemistry-and-structure-activity-relationships-of-psychedelics
#6
David E Nichols
This chapter will summarize structure-activity relationships (SAR) that are known for the classic serotonergic hallucinogens (aka psychedelics), focusing on the three chemical types: tryptamines, ergolines, and phenethylamines. In the brain, the serotonin 5-HT2A receptor plays a key role in regulation of cortical function and cognition, and also appears to be the principal target for hallucinogenic/psychedelic drugs such as LSD. It is one of the most extensively studied of the 14 known types of serotonin receptors...
March 26, 2017: Current Topics in Behavioral Neurosciences
https://www.readbyqxmd.com/read/28397671/-flibanserin-as-pharmacological-therapy-of-inhibited-sexual-desire-in-women
#7
Anne Sofie Eldon, Annamaria Giraldi
Flibanserin was approved by the Food and Drug Administration in the USA in August 2015 as the first drug for the treatment of American women with the dysfunction hypoactive sexual desire disorder (HSDD) and is a 5-HT1A agonist and 5-HT2A antagonist. The neurophysiological effects of flibanserin on these receptors are consistent with the clinical effects, i.e. significantly increasing sexual desire and frequency of satisfying sexual experiences. As such, shifting the balance between inhibitory and excitatory neurotransmitters of importance to sexual desire, flibanserin pharmacologically broaches a possible new approach to the treatment of HSDD...
February 13, 2017: Ugeskrift for Laeger
https://www.readbyqxmd.com/read/28394294/relationship-between-occupational-stress-5-ht2a-receptor-polymorphisms-and-mental-health-in-petroleum-workers-in-the-xinjiang-arid-desert-a-cross-sectional-study
#8
Ting Jiang, Hua Ge, Jian Sun, Rong Li, Rui Han, Jiwen Liu
At present, there is growing interest in research examining the relationship between occupational stress and mental health. Owing to the socioeconomic impact of occupational stress and the unique environment of petroleum workers in Xinjiang, a cross-sectional study was carried out between April and December 2015 to investigate the relationship between occupational stress, 5-hydroxytryptamine receptor (5-HTR2A) genotype, and mental health. A total of 1485 workers were selected. The Symptom Checklist 90 was used to assess nine classes of psychological symptoms...
April 10, 2017: International Journal of Environmental Research and Public Health
https://www.readbyqxmd.com/read/28386699/dreamlike-effects-of-lsd-on-waking-imagery-in-humans-depend-on-serotonin-2a-receptor-activation
#9
Rainer Kraehenmann, Dan Pokorny, Leonie Vollenweider, Katrin H Preller, Thomas Pokorny, Erich Seifritz, Franz X Vollenweider
RATIONALE: Accumulating evidence indicates that the mixed serotonin and dopamine receptor agonist lysergic acid diethylamide (LSD) induces an altered state of consciousness that resembles dreaming. OBJECTIVES: This study aimed to test the hypotheses that LSD produces dreamlike waking imagery and that this imagery depends on 5-HT2A receptor activation and is related to subjective drug effects. METHODS: Twenty-five healthy subjects performed an audiorecorded guided mental imagery task 7 h after drug administration during three drug conditions: placebo, LSD (100 mcg orally) and LSD together with the 5-HT2A receptor antagonist ketanserin (40 mg orally)...
April 7, 2017: Psychopharmacology
https://www.readbyqxmd.com/read/28380327/interaction-between-harmane-a-class-of-%C3%AE-carboline-alkaloids-and-the-ca1-serotonergic-system-in-modulation-of-memory-acquisition
#10
Mohammad Nasehi, Fatemeh Ghadimi, Fatemeh Khakpai, Mohammad-Reza Zarrindast
This study set to assess the involvement of dorsal hippocampus (CA1) serotonergic system on harmane induced memory acquisition deficit. We used one trial step-down inhibitory avoidancetask to evaluate memory retention and then, open field test to evaluate locomotor activity in adult male NMRI mice. The results showed that pre-training intra-peritoneal (i.p.) administration of harmane (12mg/kg) induced impairment of memory acquisition. Pre-training intra-CA1 administration of 5-HT1B/1D receptor agonist (CP94253; 0...
April 2, 2017: Neuroscience Research
https://www.readbyqxmd.com/read/28378435/a-single-administration-of-the-hallucinogen-4-acetoxy-dimethyltryptamine-prevents-the-shift-to-a-drug-dependent-state-and-the-expression-of-withdrawal-aversions-in-rodents
#11
Hector Vargas-Perez, Taryn E Grieder, Ryan Ting-A-Kee, Geith Maal-Bared, Michal Chwalek, Derek van der Kooy
Despite several studies suggesting the therapeutic use of 5-hydroxytryptamine receptors type 2A (5-HT2A ) agonists in the treatment of substance use disorders, the neurobiological basis accounting for such effects are still unknown. It has been observed that chronic exposure to drugs of abuse produces molecular and cellular adaptations in ventral tegmental area (VTA) neurons, mediated by brain-derived neurotrophic factor (BDNF). These BDNF-induced adaptations in the VTA are associated with the establishment of aversive withdrawal motivation that leads to a drug-dependent state...
April 4, 2017: European Journal of Neuroscience
https://www.readbyqxmd.com/read/28375643/pimavanserin
#12
Kevin M Bozymski, Denise K Lowe, Kiersten M Pasternak, Travis L Gatesman, Ericka L Crouse
OBJECTIVE: To review the pharmacology, pharmacokinetics, efficacy, safety, and place in therapy of pimavanserin for the treatment of hallucinations and delusions of Parkinson's disease psychosis (PDP). DATA SOURCES: A comprehensive PubMed search (1966 to January 2017) was conducted using the search terms Parkinson's disease psychosis, hallucinations, delusions, pimavanserin, and ACP-103. Additional data were obtained from references of identified articles, governmental sources, manufacturer product labeling and website, and Clinicaltrials...
February 1, 2017: Annals of Pharmacotherapy
https://www.readbyqxmd.com/read/28373127/rp5063-an-atypical-antipsychotic-drug-with-a-unique-pharmacologic-profile-improves-declarative-memory-and-psychosis-in-mouse-models-of-schizophrenia
#13
Lakshmi Rajagopal, Sunoh Kwon, Mei Huang, Eric Michael, Laxminarayan Bhat, Marc Cantillon, Herbert Y Meltzer
Various types of atypical antipsychotic drugs (AAPDs) modestly improve the cognitive impairment associated with schizophrenia (CIAS). RP5063 is an AAPD with a diverse and unique pharmacology, including partial agonism at dopamine (DA) D2, D3, D4, serotonin (5-HT)1A, and 5-HT2A receptors (Rs), full agonism at α4β2 nicotinic acetylcholine (ACh)R (nAChR), and antagonism at 5-HT2B, 5-HT6, and 5-HT7Rs. Most atypical APDs are 5-HT2A inverse agonists. The efficacy of RP5063 in mouse models of psychosis and episodic memory were studied...
March 31, 2017: Behavioural Brain Research
https://www.readbyqxmd.com/read/28368577/classics-in-chemical-neuroscience-aripiprazole
#14
Austen B Casey, Clinton E Canal
Aripiprazole was the first antipsychotic developed to possess agonist properties at dopamine D2 autoreceptors, a groundbreaking strategy that presented a new vista for schizophrenia drug discovery. The dopamine D2 receptor is the crucial target of all extant antipsychotics, and all developed prior to aripiprazole were D2 receptor antagonists. Extensive blockade of these receptors, however, typically produces extrapyramidal (movement) side effects, which plagued first-generation antipsychotics, such as haloperidol...
April 13, 2017: ACS Chemical Neuroscience
https://www.readbyqxmd.com/read/28361518/ketanserin-and-naftopidil-enhance-the-potentiating-effect-of-alpha-methyl-serotonin-on-the-neurally-induced-contraction-of-human-isolated-urinary-bladder-muscle-strips
#15
Tsuyoshi Hattori, Philippe Lluel, Céline Rouget, Moèz Rekik, Mitsuharu Yoshiyama
PURPOSE: The aim of this study was to assess the potential involvement of a specific subtype of 5-hydroxytryptamine (5-HT), 5HT2 receptors in neurally-induced contractions of the human detrusor. METHODS: Contractile responses to electrical field stimulation (EFS) were examined in human isolated urinary bladder muscle strips. The potentiation of EFS-induced detrusor contraction was examined by adding cumulative concentrations of a 5-HT and 5-HT2 receptor agonist, α-methyl-serotonin (α-Me-5-HT) (1nM-100μM) in the presence or absence of a 5-HT2 antagonist, ketanserin (5-HT2A>5-HT2C) or naftopidil (5-HT2B>5-HT2A) (0...
March 24, 2017: International Neurourology Journal
https://www.readbyqxmd.com/read/28360333/detailed-characterization-of-the-in-vitro-pharmacological-and-pharmacokinetic-properties-of-n-2-hydroxybenzyl-2-5-dimethoxy-4-cyanophenylethylamine-25cn-nboh-a-highly-selective-and-brain-penetrant-5-ht2a-receptor-agonist
#16
Anders A Jensen, John D McCorvy, Sebastian Leth Petersen, Christoffer Bundgaard, Gudrun Liebscher, Terry P Kenakin, Hans Brauner-Osborne, Jan Kehler, Jesper L Kristensen
Therapeutic interest in augmentation of 5-hydroxytryptamine2A (5-HT2A) receptor signaling has been renewed by the effectiveness of psychedelic drugs in the treatment of various psychiatric conditions. In this study, we have further characterized the pharmacological properties of the recently developed 5-HT2 receptor agonist 2-hydroxybenzyl)-2,5-dimethoxy-4-cyanophenylethylamine (25CN-NBOH) and three structural analogs at recombinant 5-HT2A, 5- HT2B and 5-HT2C receptors and investigated the pharmacokinetic properties of the compound...
March 30, 2017: Journal of Pharmacology and Experimental Therapeutics
https://www.readbyqxmd.com/read/28343185/frameworking-memory-and-serotonergic-markers
#17
Alfredo Meneses
The evidence for neural markers and memory is continuously being revised, and as evidence continues to accumulate, herein, we frame earlier and new evidence. Hence, in this work, the aim is to provide an appropriate conceptual framework of serotonergic markers associated with neural activity and memory. Serotonin (5-hydroxytryptamine [5-HT]) has multiple pharmacological tools, well-characterized downstream signaling in mammals' species, and established 5-HT neural markers showing new insights about memory functions and dysfunctions, including receptors (5-HT1A/1B/1D, 5-HT2A/2B/2C, and 5-HT3-7), transporter (serotonin transporter [SERT]) and volume transmission present in brain areas involved in memory...
March 27, 2017: Reviews in the Neurosciences
https://www.readbyqxmd.com/read/28337282/chronic-intermittent-hypoxia-affects-endogenous-serotonergic-inputs-and-expression-of-synaptic-proteins-in-rat-hypoglossal-nucleus
#18
Xu Wu, Huan Lu, Lijuan Hu, Wankun Gong, Juan Wang, Cuiping Fu, Zilong Liu, Shanqun Li
Evidence has shown that hypoxic episodes elicit hypoglossal neuroplasticity which depends on elevated serotonin (5-HT), in contrast to the rationale of obstructive sleep apnea (OSA) that deficient serotonergic input to HMs fails to keep airway patency. Therefore, understanding of the 5-HT dynamic changes at hypoglossal nucleus (HN) during chronic intermittent hypoxia (CIH) will be essential to central pathogenic mechanism and pharmacological therapy of OSA. Moreover, the effect of CIH on BDNF-TrkB signaling proteins was quantified in an attempt to elucidate cellular cascades/synaptic mechanisms following 5-HT alteration...
2017: American Journal of Translational Research
https://www.readbyqxmd.com/read/28332205/evidence-that-5-ht-stimulates-intracellular-ca-2-signalling-and-activates-pannexin-1-currents-in-type-ii-cells-of-the-rat-carotid-body
#19
Sindhubarathi Murali, Min Zhang, Colin A Nurse
Carotid body (CB) chemoreceptor (type I) cells can synthesize and release 5-hydroxytryptamine (5-HT) and increased autocrine-paracrine 5-HT2 receptor signalling contributes to sensory long-term facilitation during chronic intermittent hypoxia (CIH). However, recent studies suggest that adjacent glial-like type II cells can respond to CB paracrine signals by elevating intracellular calcium (Δ[Ca(2+) ]i ) and activating carbenoxolone-sensitive, ATP-permeable, pannexin-1 (Panx-1)-like channels. Here, using dissociated rat CB cultures, we found that 5-HT induced Δ[Ca(2+) ]i responses in a subpopulation of type I cells, and in most (∼67%) type II cells identified by their sensitivity to the P2Y2 receptor agonist, UTP...
March 22, 2017: Journal of Physiology
https://www.readbyqxmd.com/read/28331332/clinical-role-of-brexpiprazole-in-depression-and-schizophrenia
#20
REVIEW
Nishant B Parikh, Diana M Robinson, Anita H Clayton
Brexpiprazole, a serotonin-dopamine activity modulator, is the second D2 partial agonist to come to market and has been approved for the treatment of schizophrenia and as an adjunctive treatment in major depressive disorder. With less intrinsic activity than aripiprazole at the D2 receptor and higher potency at 5-HT2A, 5-HT1A, and α1B receptors, the pharmacological properties of brexpiprazole suggest a more tolerable side effect profile with regard to akathisia, extrapyramidal dysfunction, and sedation. While no head-to-head data are currently available, double-blind placebo-controlled studies show favorable results, with the number needed to treat (NNT) vs placebo of 6-15 for response in acute schizophrenia treatment and 4 for maintenance...
2017: Therapeutics and Clinical Risk Management
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