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https://www.readbyqxmd.com/read/28059046/long-term-effects-of-aripiprazole-exposure-on-monoaminergic-and-glutamatergic-receptor-subtypes-comparison-with-cariprazine
#1
Yong Kee Choi, Nika Adham, Béla Kiss, István Gyertyán, Frank I Tarazi
OBJECTIVE: This study examined the chronic effects of aripiprazole and cariprazine on serotonin (5-HT1A and 5-HT2A) and glutamate (NMDA and AMPA) receptor subtypes. In addition, the effects of aripiprazole on D2 and D3 receptors were tested and compared with previously reported cariprazine data. METHODS: Rats received vehicle, aripiprazole (2, 5, or 15 mg/kg), or cariprazine (0.06, 0.2, or 0.6 mg/kg) for 28 days. Receptor levels were quantified using autoradiographic assays on brain sections from the medial prefrontal cortex (MPC), dorsolateral frontal cortex (DFC), nucleus accumbens (NAc), caudate-putamen medial (CPu-M), caudate-putamen lateral (CPu-L), hippocampal CA1 (HIPP-CA1) and CA3 (HIPP-CA3) regions, and the entorhinal cortex (EC)...
January 6, 2017: CNS Spectrums
https://www.readbyqxmd.com/read/28054193/personality-as-an-intermediate-phenotype-for-genetic-dissection-of-alcohol-use-disorder
#2
REVIEW
Lars Oreland, Gianvito Lagravinese, Simone Toffoletto, Kent W Nilsson, Jaanus Harro, C Robert Cloninger, Erika Comasco
Genetic and environmental interactive influences on predisposition to develop alcohol use disorder (AUD) account for the high heterogeneity among AUD patients and make research on the risk and resiliency factors complicated. Several attempts have been made to identify the genetic basis of AUD; however, only few genetic polymorphisms have consistently been associated with AUD. Intermediate phenotypes are expected to be in-between proxies of basic neuronal biological processes and nosological symptoms of AUD...
January 4, 2017: Journal of Neural Transmission
https://www.readbyqxmd.com/read/28054012/localization-of-muscarinic-acetylcholine-receptor-2-to-the-intestinal-crypt-stem-cell-compartment
#3
Eleanor D Muise, Neeru Gandotra, John J Tackett, Michaela C Bamdad, Robert A Cowles
The data presented in this article are related to the research article entitled "Distribution of muscarinic acetylcholine receptor subtypes in the murine small intestine" (E.D. Muise, N. Gandotra, J.J. Tackett, M.C. Bamdad, R.A. Cowles, 2016) [1]. We recently demonstrated that neuronal serotonin stimulates intestinal crypt cell division, and induces villus growth and crypt depth (E.R. Gross, M.D. Gershon, K.G. Margolis, Z.V. Gertsberg, Z. Li, R.A. Cowles, 2012; M.D. Gershon, 2013) [2], [3]. Scopolamine, a nonspecific muscarinic receptor antagonist, inhibited serotonin-induced intestinal mucosal growth [2]...
February 2017: Data in Brief
https://www.readbyqxmd.com/read/28040566/marked-sexual-dimorphism-in-5-ht1-receptors-mediating-pronociceptive-effects-of-sumatriptan
#4
Dioneia Araldi, Luiz F Ferrari, Paul Green, Jon D Levine
Amongst the side effects of triptans, a substantial percentage of patients experience injection site pain and tenderness, the underlying mechanism of which is unknown. We found that the dose range from 10fg to 1000ng (intradermal) of sumatriptan induced a complex dose-dependent mechanical hyperalgesia in male rats, with distinct peaks, at 1pg and 10ng, but no hyperalgesia at 1ng. In contrast, in females, there was 1 broad peak. The highest dose (1000ng) did not produce hyperalgesia in either sex. We evaluated the receptors mediating sumatriptan hyperalgesia (1pg, 1 and 10ng)...
December 29, 2016: Neuroscience
https://www.readbyqxmd.com/read/28012414/the-effect-of-sertraline-and-8-oh-dpat-on-the-ptz_induced-seizure-threshold-role-of-the-nitrergic-system
#5
Azhdar Heydari, Shima Davoudi
PURPOSE: Serotonin is a key regulatory neurotransmitter in the CNS which plays an important role in seizure through different receptors, especially the 5HT1A subtype. The role of sertraline through the 5HT1A receptor and nitric oxide interaction on the PTZ-induced seizure threshold was investigated in this study. METHOD: In this study, 70 white male mice were randomly divided into 10 groups including intact control, sham-control and eight experimental groups which received sertraline, 8-OH-DPAT, WAY100635, WAY100635+sertraline, WAY100635+8-OH-DPAT, L-NAME, L-NAME+sertraline and L-NAME+8-OH-DPAT...
December 15, 2016: Seizure: the Journal of the British Epilepsy Association
https://www.readbyqxmd.com/read/28011743/5-ht2c-receptor-knockdown-in-the-amygdala-inhibits-neuropathic-pain-related-plasticity-and-behaviors
#6
Guangchen Ji, Wei Zhang, Lenin Mahimainathan, Madhusudhanan Narasimhan, Takaki Kiritoshi, Xiuzhen Fan, Jigong Wang, Thomas A Green, Volker Neugebauer
: Neuroplasticity in the amygdala drives pain-related behaviors. The central nucleus (CeA) serves major amygdala output functions and can generate emotional-affective behaviors and modulate nocifensive responses. The CeA receives excitatory and inhibitory inputs from the basolateral nucleus (BLA), and serotonin receptor subtype 5-HT2CR in the BLA, but not CeA, has been implicated anxiogenic behaviors and anxiety disorders. Here we tested the hypothesis that 5-HT2CR in the BLA plays a critical role in CeA plasticity and neuropathic pain behaviors in the rat spinal nerve ligation (SNL) model...
December 23, 2016: Journal of Neuroscience: the Official Journal of the Society for Neuroscience
https://www.readbyqxmd.com/read/27981607/synthesis-and-docking-of-novel-3-indolylpropyl-derivatives-as-new-polypharmacological-agents-displaying-affinity-for-5-ht1a-r-sert
#7
Hernán Pessoa-Mahana, Paul Silva-Matus, C David Pessoa-Mahana, Hery Chung, Patricio Iturriaga-Vásquez, Gabriel Quiroz, Patricia Möller-Acuña, Gerald Zapata-Torres, Claudio Saitz-Barría, Ramiro Araya-Maturana, Miguel Reyes-Parada
A series of novel 3-indolylpropyl derivatives was synthesized and evaluated for their binding affinities at the serotonin-1A receptor subtype (5-HT1A R) and the 5-HT transporter (SERT). Compounds 11b and 14b exhibited the highest affinities at the 5-HT1A R (Ki  = 43 and 56 nM), whereas compounds 11c and 14a were the most potent analogs at the SERT (Ki  = 34 and 17 nM). On the other hand, compounds 14b and 11d showed potent activity at both targets, displaying a profile that makes them promising leads for the search for novel potent ligands with a dual mechanism of action...
December 16, 2016: Archiv der Pharmazie
https://www.readbyqxmd.com/read/27979722/apomorphine-pharmacological-properties-and-clinical-trials-in-parkinson-s-disease
#8
Peter Jenner, Regina Katzenschlager
Apomorphine is often considered an archetypal dopamine agonist used in the treatment of Parkinson's disease (PD). However, it can be clearly differentiated from most other commonly used dopamine agonists on the basis of its pharmacology and on its unique clinical profile. Like levodopa and dopamine, apomorphine acts as a potent, direct and broad spectrum dopamine agonist activating all dopamine receptor subtypes. It also has affinity for serotonin receptors, and α-adrenergic receptors. Apomorphine is usually titrated to a dose that provides an equivalent antiparkinsonian response to that provided by levodopa, and its subcutaneous delivery allows a rapid onset of action, usually within 7-10 min...
December 2016: Parkinsonism & related Disorders
https://www.readbyqxmd.com/read/27960027/visualization-of-5-ht-receptors-using-radioligand-binding-autoradiography
#9
Roser Cortés, M Teresa Vilaró, Guadalupe Mengod
Described in this unit are techniques to visualize the majority of serotonin (5-hydroxytryptamine, 5-HT) receptor subtypes in sections of frozen brain tissue using receptor autoradiography. Protocols for brain extraction and sectioning, radioligand exposure, autoradiogram generation, and data quantification are provided, as are the optimal incubation conditions for the autoradiographic visualization of receptors using agonist and antagonist radioligands. © 2016 by John Wiley & Sons, Inc.
December 13, 2016: Current Protocols in Pharmacology
https://www.readbyqxmd.com/read/27866962/distribution-of-muscarinic-acetylcholine-receptor-subtypes-in-the-murine-small-intestine
#10
Eleanor D Muise, Neeru Gandotra, John J Tackett, Michaela C Bamdad, Robert A Cowles
AIMS: Serotonin stimulates enterocyte turnover in the small intestine and studies suggest this is mediated by neuronal signaling via a cholinergic pathway. Distribution of the five known muscarinic receptor subtypes (mAChRs) in the small intestine has not been fully studied, and their role in intestinal growth is unknown. We hypothesized that mAChRs have distinct anatomic distributions within the bowel, and that mAChRs present within intestinal crypts mediate the effects of acetylcholine on the small intestinal mucosa...
November 17, 2016: Life Sciences
https://www.readbyqxmd.com/read/27821848/depression-like-phenotype-by-deletion-of-%C3%AE-7-nicotinic-acetylcholine-receptor-role-of-bdnf-trkb-in-nucleus-accumbens
#11
Ji-Chun Zhang, Wei Yao, Qian Ren, Chun Yang, Chao Dong, Min Ma, Jin Wu, Kenji Hashimoto
The α7 subtype of nicotinic acetylcholine receptor (nAChR) plays a role in the inflammation which is implicated in depression. This study was undertaken to examine the role of α7 nAChR in depression using α7 nAChR knock-out (KO) mice. Serum levels of tumor necrosis factor-α and interlukin-1β in KO mice were higher than wild-type mice, suggesting an inflammatory process in KO mice. α7 nAChR KO mice showed depression-like phenotype. Furthermore, KO mice showed increased brain-derived neurotrophic factor (BDNF) and its receptor TrkB signaling, as well as increased synaptogenesis and spine density in the nucleus accumbens (NAc), although BDNF-TrkB signaling and synaptogenesis were not altered in the prefrontal cortex and hippocampus...
November 8, 2016: Scientific Reports
https://www.readbyqxmd.com/read/27769892/bimodal-modulation-of-store-operated-ca-2-channels-by-clozapine-in-astrocytes
#12
Yuzuki Kanda, Miho Okada, Rina Ikarashi, Eri Morioka, Takashi Kondo, Masayuki Ikeda
Clozapine (Clz) and olanzapine (Olz) are second generation (atypical) antipsychotics, used widely for treating schizophrenia and bipolar disorder. These drugs share multiple sites of actions, however their mechanisms remain incompletely understood. Here, we analyzed the effects of these drugs on primary cultures of rat cortical astrocytes and C6 glioma cells using fura-2-based Ca(2+) imaging. C6 cells, but not cortical astrocytes, express the serotonin 2A receptor subtype, which couples to phospholipase C. Clz (1μM) significantly blocked serotonin-induced Ca(2+) transients in C6 cells, consistent with known antagonistic actions of Clz...
December 2, 2016: Neuroscience Letters
https://www.readbyqxmd.com/read/27763704/the-human-serotonin-type-3-receptor-gene-htr3a-e-allelic-variant-database
#13
Jacopo Celli, Gudrun Rappold, Beate Niesler
Serotonin type 3 (5-HT3 ) receptors are ligand-gated ion channels formed by five subunits (5-HT3A-E), which are encoded by the HTR3A, HTR3B, HTR3C, HTR3D, and HTR3E genes. Functional receptors are pentameric complexes of diverse composition. Different receptor subtypes confer a predisposition to nausea and vomiting during chemotherapy, pregnancy, and following surgery. In addition, different subtypes contribute to neurogastroenterologic disorders such irritable bowel syndrome (IBS) and eating disorders as well as comorbid psychiatric conditions...
February 2017: Human Mutation
https://www.readbyqxmd.com/read/27746521/postoperative-nausea-and-vomiting-a-simple-yet-complex-problem
#14
REVIEW
Safiya Imtiaz Shaikh, D Nagarekha, Ganapati Hegade, M Marutheesh
Postoperative nausea and vomiting (PONV) is one of the complex and significant problems in anesthesia practice, with growing trend toward ambulatory and day care surgeries. This review focuses on pathophysiology, pharmacological prophylaxis, and rescue therapy for PONV. We searched the Medline and PubMed database for articles published in English from 1991 to 2014 while writing this review using "postoperative nausea and vomiting, PONV, nausea-vomiting, PONV prophylaxis, and rescue" as keywords. PONV is influenced by multiple factors which are related to the patient, surgery, and pre-, intra-, and post-operative anesthesia factors...
September 2016: Anesthesia, Essays and Researches
https://www.readbyqxmd.com/read/27743549/serotonergic-agents-act-on-5-ht3-receptors-in-the-brain-to-block-seizure-induced-respiratory-arrest-in-the-dba-1-mouse-model-of-sudep
#15
Carl L Faingold, Marcus Randall, Chang Zeng, Shifang Peng, Xiaoyan Long, Hua-Jun Feng
Drugs that enhance the action of serotonin (5-hydroxytrypamine, 5-HT), including several selective serotonin reuptake inhibitors (SSRIs), reduce susceptibility to seizure-induced respiratory arrest (S-IRA) that leads to death in the DBA/1 mouse model of sudden unexpected death in epilepsy (SUDEP). However, it is not clear if specific 5-HT receptors are important in the action of these drugs and whether the brain is the major site of action of these agents in this SUDEP model. The current study examined the actions of agents that affect the 5-HT3 receptor subtype on S-IRA and whether intracerebroventricular (ICV) microinjection of an SSRI would reduce S-IRA susceptibility in DBA/1 mice...
November 2016: Epilepsy & Behavior: E&B
https://www.readbyqxmd.com/read/27703829/development-of-tinnitus-at-a-low-dose-of-sertraline-clinical-course-and-proposed-mechanisms
#16
Christopher W T Miller
Introduction. Serotonin is involved in filtering of auditory stimuli. Cochlear input is processed through complex interactions between serotonergic, glutamatergic, and GABAergic neurotransmitter systems. Options for treatment of tinnitus include selective serotonin reuptake inhibitors (SSRIs); however in rare instances this symptom may occur as a side effect of this class of medications. Case Presentation. A 50-year-old woman developed bilateral tinnitus after several weeks of being treated with sertraline 50 mg...
2016: Case Reports in Psychiatry
https://www.readbyqxmd.com/read/27690134/induced-obsessive-compulsive-symptoms-ocs-in-schizophrenia-patients-under-atypical-2-antipsychotics-aaps-review-and-hypotheses
#17
REVIEW
Diane Grillault Laroche, Adeline Gaillard
The prevalence of OCS and OCD is higher in schizophrenic patients than in the general population. These disorders are sometimes induced by AAPs. There is higher frequency of OCS and greater severity in patients treated with antipsychotics with predominant anti-serotoninergic profiles opposed to those with predominant dopaminergic blockade. Induced OCS may be due to complex neuromodulation involving many serotonin, dopamine and glutamate receptors and several subtypes. Concerning connectivity, AAPs differentially influence the BOLD signal, depending on the intensity of D2 receptor blockade...
December 30, 2016: Psychiatry Research
https://www.readbyqxmd.com/read/27663700/divergent-camp-signaling-differentially-regulates-serotonin-induced-spinal-motor-plasticity
#18
D P Fields, G S Mitchell
Spinal metabotropic serotonin receptors encode transient experiences into long-lasting changes in motor behavior (i.e. motor plasticity). While interactions between serotonin receptor subtypes are known to regulate plasticity, the significance of molecular divergence in downstream G protein coupled receptor signaling is not well understood. Here we tested the hypothesis that distinct cAMP dependent signaling pathways differentially regulate serotonin-induced phrenic motor facilitation (pMF); a well-studied model of spinal motor plasticity...
February 2017: Neuropharmacology
https://www.readbyqxmd.com/read/27649637/psychedelics-recruit-multiple-cellular-types-and-produce-complex-transcriptional-responses-within-the-brain
#19
David A Martin, Charles D Nichols
There has recently been a resurgence of interest in psychedelics, substances that profoundly alter perception and cognition and have recently demonstrated therapeutic efficacy to treat anxiety, depression, and addiction in the clinic. The receptor mechanisms that drive their molecular and behavioral effects involve activation of cortical serotonin 5-HT2A receptors, but the responses of specific cellular populations remain unknown. Here, we provide evidence that a small subset of 5-HT2A-expressing excitatory neurons is directly activated by psychedelics and subsequently recruits other select cell types including subpopulations of inhibitory somatostatin and parvalbumin GABAergic interneurons, as well as astrocytes, to produce distinct and regional responses...
September 2016: EBioMedicine
https://www.readbyqxmd.com/read/27640338/characterization-of-the-discriminative-stimulus-effects-of-lorcaserin-in-rats
#20
Katherine M Serafine, Kenner C Rice, Charles P France
Lorcaserin is approved by the Food and Drug Administration for treating obesity and is under consideration for treating substance use disorders; it has agonist properties at serotonin (5-HT)2C receptors and might also have agonist properties at other 5-HT receptor subtypes. This study used drug discrimination to investigate the mechanism(s) of action of lorcaserin. Male Sprague-Dawley rats discriminated 0.56 mg/kg i.p. lorcaserin from saline while responding under a fixed-ratio 5 schedule for food. Lorcaserin (0...
September 2016: Journal of the Experimental Analysis of Behavior
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