Read by QxMD icon Read

5 HT receptors

Yu Shi, Wenguang Liu, Maoxian He
Bivalve mollusks exhibit hermaphroditism and sex reversal/differentiation. Studies generally focus on transcriptional profiling and specific genes related to sex determination and differentiation. Few studies on sex reversal/differentiation have been reported. A combination analysis of gonad proteomics and transcriptomics was conducted on Chlamys nobilis to provide a systematic understanding of sex reversal/differentiation in bivalves. We obtained 4258 unique peptides and 93,731 unigenes with good correlation between messenger RNA and protein levels...
March 15, 2018: Marine Biotechnology
Mikael Tiger, Katarina Varnäs, Yoshiro Okubo, Johan Lundberg
Major depressive disorder (MDD) is the leading cause of disability worldwide. The serotonin hypothesis may be the model of MDD pathophysiology with the most support. The majority of antidepressants enhance synaptic serotonin levels quickly, while it usually takes weeks to discern MDD treatment effect. It has been hypothesized that the time lag between serotonin increase and reduction of MDD symptoms is due to downregulation of inhibitory receptors such as the serotonin 1B receptor (5-HT1BR). The research on 5-HT1BR has previously been hampered by a lack of selective ligands for the receptor...
March 15, 2018: Psychopharmacology
Magdalena Kolasa, Joanna Solich, Agata Faron-Górecka, Dariusz Żurawek, Paulina Pabian, Sylwia Łukasiewicz, Maciej Kuśmider, Kinga Szafran-Pilch, Marta Szlachta, Marta Dziedzicka-Wasylewska
Recently, it has been shown that serotonin 5-HT1A receptor interacts with dopamine D2 receptor in vitro. However, the existence of 5-HT1A -D2 heteromers in native tissue remains unexplored. In the present study, we investigated 5-HT1A -D2 receptor heteromerization in mice treated acutely or chronically with paroxetine (10 mg/kg) or risperidone (0.05 mg/kg). Receptor heteromerization was visualized and quantified in the mouse brain by in situ proximity ligation assay (PLA). Additionally, we aimed to determine the cellular localization of 5-HT1A -D2 receptor heteromers in mouse adult primary neuronal cells by immunofluorescent staining with markers for astrocytes (GFAP) and neurons (NeuN and MAP2)...
March 12, 2018: Neuroscience
Alexander V Kulikov, Raul R Gainetdinov, Evgeni Ponimaskin, Allan V Kalueff, Vladimir S Naumenko, Nina K Popova
Selective serotonin reuptake inhibitors (SSRIs) are the most effective and most used antidepressant drugs. Acting by inhibiting serotonin (5-HT) transporter, SSRIs display a typical 3-4-week delay in their therapeutic effects, with nearly 40% of depressed patients remaining treatment-resistant. Recent evidence suggests complex interplay between 5-HT receptors and key proteins of 5-HT metabolism in molecular mechanisms of such delay and resistance to SSRIs. Area covered: This paper concentrates on the interplay between 5-HT receptors in the delay of therapeutic effect of SSRIs, and the interaction between tryptophan hydroxylase 2 and 5-HT transporter in the SSRI resistance...
March 15, 2018: Expert Opinion on Therapeutic Targets
Fanxing Zeng, Jonathon A Nye, Ronald J Voll, Leonard Howell, Mark M Goodman
Nine pyridyloxypyridyl indole carboxamides were synthesized and displayed high affinities for 5-HT2C receptors and high selectivity over 5-HT2A and 5-HT2B . Among them, 6-methyl- N -[6-[(2-methyl-3-pyridinyl)oxy]-3-pyridinyl]1 H -indole-3-carboxamide ( 8 ) exhibits the highest 5-HT2C binding affinity ( K i = 1.3 nM) and high selectivity over 5-HT2A (∼1000 times) and 5-HT2B (∼140 times). [11 C] 8 was synthesized by palladium-catalyzed coupling reaction between pinacolboranate 16 and [11 C]CH3 I with an average radiochemical yield of 27 ± 4% ( n = 8, decay-corrected from end of [11 C]CH3 I synthesis)...
March 8, 2018: ACS Medicinal Chemistry Letters
Joshua S Elmore, Michael H Baumann
Naphthalen-1-yl-(1-pentylindol-3-yl)methanone (JWH-018) is a synthetic compound found in psychoactive "spice" products that activates cannabinoid receptors. Preclinical evidence suggests that exposure to synthetic cannabinoids increases 5-HT2A/2C receptor function in the brain, an effect which might contribute to psychotic symptoms. Here, we hypothesized that repeated exposures to JWH-018 would enhance behavioral responsiveness to the 5-HT2A/2C receptor agonist DOI. Male Sprague-Dawley rats fitted with subcutaneously (sc) temperature transponders received daily injections of JWH-018 (1...
2018: Frontiers in Psychiatry
Patrick D Ganzer, Carl R Beringer, Jed S Shumsky, Chiemela Nwaobasi, Karen A Moxon
Severe spinal cord injury (SCI) damages descending motor and serotonin (5-HT) fiber projections leading to paralysis and serotonin depletion. 5-HT receptors (5-HTRs) subsequently upregulate following 5-HT fiber degeneration, and dendritic density decreases indicative of atrophy. 5-HT pharmacotherapy or exercise can improve locomotor behavior after SCI. One might expect that 5-HT pharmacotherapy acts on upregulated spinal 5-HTRs to enhance function, and that exercise alone can influence dendritic atrophy. In the current study, we assessed locomotor recovery and spinal proteins influenced by SCI and therapy...
March 8, 2018: Experimental Neurology
Xuke Han, Huangan Wu, Ping Yin, Zeqin Chen, Xiaohua Cao, Yanhong Duan, Jian Xu, Lixing Lao, Shifen Xu
OBJECTIVE: The study aimed to determine the effect of electroacupuncture (EA) on Wistar Kyoto (WKY) depressive model rats and explore the possible mechanism of EA on hippocampal CA1 region neuronal synaptic plasticity. METHODS: The male WKY rats were randomized to three experimental groups (EA, Sham EA, and Model group, n = 8/group), and Wistar rats as the normal control group (n = 8). EA treatment was administered once daily for 3 weeks at acupuncture points Baihui (GV20) and Yintang (EX-HN3)...
March 7, 2018: Brain Research Bulletin
Colin A Nurse, Erin M Leonard, Shaima Salman
Mammalian carotid bodies (CB) are chemosensory organs that mediate compensatory cardiorespiratory reflexes in response to low blood PO2 (hypoxemia) and elevated CO2 /H+ (acid hypercapnia). The chemoreceptors are glomus or type I cells which occur in clusters enveloped by neighboring glial-like type II cells. During chemoexcitation type I cells depolarize, leading to Ca2+ -dependent release of several neurotransmitters, some excitatory and others inhibitory, which help shape the afferent carotid sinus nerve (CSN) discharge...
March 9, 2018: Physiological Genomics
Lianwei Mu, Dong Dong Xia, Teresa Michalkiewicz, Matthew Hodges, Gary Mouradian, Girija G Konduri, Margaret T T Wong-Riley
We have identified a critical period of respiratory development in rats at postnatal days P12-13, when inhibitory influence dominates and when the response to hypoxia is at its weakest. This critical period has significant implications for Sudden Infant Death Syndrome (SIDS), the cause of which remains elusive. One of the known risk factors for SIDS is prematurity. A common intervention used in premature infants is hyperoxic therapy, which, if prolonged, can alter the ventilatory response to hypoxia and induce sustained inhibition of lung alveolar growth and pulmonary remodeling...
March 2018: Physiological Reports
S D Dolzani, M V Baratta, J M Moss, N L Leslie, S G Tilden, A T Sørensen, L R Watkins, Y Lin, S F Maier
Stress is a potent etiological factor in the onset of major depressive disorder and posttraumatic stress disorder (PTSD). Therefore, significant efforts have been made to identify factors that produce resilience to the outcomes of a later stressor, in hopes of preventing untoward clinical outcomes. The NMDA receptor antagonist ketamine has recently emerged as a prophylactic capable of preventing neurochemical and behavioral outcomes of a future stressor. Despite promising results of preclinical studies performed in male rats, the effects of proactive ketamine in female rats remains unknown...
January 2018: ENeuro
Kerry L Price, Sarah C R Lummis
Cys-loop receptors are major sites of action for many important therapeutically active compounds, but the sites of action of those that do not act at the orthosteric binding site or at the pore are mostly poorly understood. To help understand these, we here describe a chimeric receptor consisting of the extracellular domain of the 5-HT3 A receptor and the transmembrane domain of a prokaryotic homologue, ELIC. Alterations of some residues at the coupling interface are required for function, but the resulting receptor expresses well and responds to 5-HT with a lower EC50 (0...
March 6, 2018: ACS Chemical Neuroscience
Julien Volle, Tatiana Bregman, Brian Scott, Mustansir Diwan, Roger Raymond, Paul J Fletcher, José N Nobrega, Clement Hamani
Both selective serotonin reuptake inhibitors (SSRIs) and ventromedial prefrontal cortex (vmPFC) deep brain stimulation (DBS) modulate serotonergic activity. We compared the acute (1 day) and long-term (12 days) effects of vmPFC stimulation and fluoxetine on serotonin (5-HT) release and receptor expression in rats. Samples to measure serotonin levels were collected from the hippocampus using microdialysis. Serotonin transporter (SERT), 5-HT1A and 5-HT1B mRNA were measured using in situ hybridization. [3 H]8-OH-DPAT and [125 I]cyanopindolol autoradiography were used to measure 5-HT1A and 5-HT1B binding...
March 2, 2018: Neuropharmacology
Tadashi Tsubouchi, Takeshi Kunimatsu, Shinji Tsujimoto, Akihiko Kiyoshi, Yasunori Katsura, Seiko Oku, Kazuhiro Chihara, Yukiko Mine, Toru Yamada, Isao Shimizu, Kiyoko Bando
The pharmacological activity of DSP-6952, a novel compound was investigated, compared to that of clinically efficacious gastrointestinal (GI) prokinetic 5-hydroxytryptamine4 (5-HT4 ) receptor agonists. DSP-6952 had a strong affinity of Ki=51.9nM for 5-HT4(b) receptor, and produced contraction in the isolated guinea pig colon with EC50 of 271.6nM and low intrinsic activity of 57%, similar to tegaserod and mosapride. In the development of the 5-HT4 receptor agonists, cardiovascular risk was deliberately evaluated, because some related prokinetics were reported to cause with cardiovascular adverse events, such as ventricular arrhythmias or ischemia...
March 1, 2018: European Journal of Pharmacology
V P Nikitin, S V Solntseva, S A Kozyrev, P V Nikitin, A V Shevelkin
Elucidation of amnesia mechanisms is one of the central problems in neuroscience with immense practical application. Previously, we found that conditioned food presentation combined with injection of a neurotransmitter receptor antagonist or protein synthesis inhibitor led to amnesia induction. In the present study, we investigated the time course and features of two amnesias: induced by impairment of memory reconsolidation using an NMDA glutamate receptor antagonist (MK-801) and a serotonin receptor antagonist (methiothepin, MET) on snails trained with food aversion conditioning...
February 27, 2018: Behavioural Brain Research
Guendalina Olivero, Massimo Grilli, Matteo Vergassola, Tommaso Bonfiglio, Cristina Padolecchia, Beatrice Garrone, Francesco Paolo Di Giorgio, Stefania Tongiani, Cesare Usai, Mario Marchi, Anna Pittaluga
Presynaptic mGlu2/3 autoreceptors exist in rat spinal cord nerve terminals as suggested by the finding that LY379268 inhibited the 15 mM KCl-evoked release of [3 H]D-aspartate ([3 H]D-Asp) in a LY341495-sensitive manner. Spinal cord glutamatergic nerve terminals also possess presynaptic release-regulating 5-HT2A heteroreceptors. Actually, the 15 mM KCl-evoked [3 H]D-Asp exocytosis from spinal cord synaptosomes was reduced by the 5-HT2A agonist (±)DOI, an effect reversed by the 5-HT2A antagonists MDL11,939, MDL100907, ketanserin and trazodone (TZD)...
February 27, 2018: Neuropharmacology
Paul J Fletcher, Zhaoxia Li, Leo B Silenieks, Cam MacMillan, Ines DeLannoy, Guy A Higgins
Varenicline, a nicotinic acetylcholine receptor partial agonist, is used to treat nicotine dependence. Lorcaserin, a 5-HT2C receptor agonist has been approved in some countries to treat obesity. Based on preclinical and preliminary clinical evidence, lorcaserin may have potential to treat nicotine dependence. These experiments examined in rats the effects of combining varenicline (0.5 or 1 mg/kg) and lorcaserin (0.3, 0.6 and 1 mg/kg) on nicotine self-administration, reinstatement of nicotine seeking, responding for food and impulsive action...
March 2, 2018: Addiction Biology
Marta Szlachta, Maciej Kuśmider, Paulina Pabian, Joanna Solich, Magdalena Kolasa, Dariusz Żurawek, Marta Dziedzicka-Wasylewska, Agata Faron-Górecka
G-protein-coupled receptor (GPCR) heterodimers are new targets for the treatment of schizophrenia. Dopamine D2 receptors and serotonin 5-HT1A and 5-HT2A receptors play an important role in neurotransmission and have been implicated in many human psychiatric disorders, including schizophrenia. Therefore, in this study, we investigated whether antipsychotic drugs (clozapine (CLZ) and haloperidol (HAL)) affected the formation of heterodimers of D2 -5-HT1A receptors as well as 5-HT1A -5-HT2A receptors. Proximity ligation assay (PLA) was used to accurately visualize, for the first time, GPCR heterodimers both at in vitro and ex vivo levels...
2018: Frontiers in Molecular Neuroscience
Yu Kyong Kim, Kwang-Hee Shin, Jeffrey Alderman, Kyung-Sang Yu, In-Jin Jang, SeungHwan Lee
Background: Migraine is one of the most common headache disorders that greatly affect the quality of life. Selective serotonin (5-HT) receptor agonists such as triptamine-based drugs called triptans are used for treatment of migraine. Purpose: This study aimed to evaluate the pharmacokinetic (PK) and tolerability profiles of eletriptan hydrobromide (eletriptan HBr), a selective 5-hydroxytryptamine (also known as serotonin) 1B/1D receptor agonist, in Koreans and compare the results to those observed in non-Koreans in a previously published study...
2018: Drug Design, Development and Therapy
Mustapha Abubakar, Jenny Chang-Claude, H Raza Ali, Nilangan Chatterjee, Penny Coulson, Frances Daley, Fiona Blows, Javier Benitez, Roger L Milne, Hermann Brenner, Christa Stegmaier, Arto Mannermaa, Anja Rudolph, Peter Sinn, Fergus J Couch, Peter Devilee, Rob Aem Tollenaar, Caroline Seynaeve, Jonine Figueroa, Jolanta Lissowska, Stephen Hewitt, Maartje J Hooning, Antoinette Hollestelle, Renée Foekens, Linetta B Koppert, kConFab Investigators, Manjeet K Bolla, Qin Wang, Michael E Jones, Minouk J Schoemaker, Renske Keeman, Douglas F Easton, Anthony J Swerdlow, Mark E Sherman, Marjanka K Schmidt, Paul D Pharoah, Montserrat Garcia-Closas
Limited epidemiological evidence suggests that the etiology of hormone receptor positive (HR+) breast cancer may differ by levels of histologic grade and proliferation. We pooled risk factor and pathology data on 5,905 HR+ breast cancer cases and 26,281 controls from 11 epidemiological studies. Proliferation was determined by centralized automated measures of KI67 in tissue microarrays. Odds ratios (OR), 95% confidence intervals (CI) and p-values for case-case and case-control comparisons for risk factors in relation to levels of grade and quartiles (Q1-Q4) of KI67 were estimated using polytomous logistic regression models...
March 1, 2018: International Journal of Cancer. Journal International du Cancer
Fetch more papers »
Fetching more papers... Fetching...
Read by QxMD. Sign in or create an account to discover new knowledge that matter to you.
Remove bar
Read by QxMD icon Read

Search Tips

Use Boolean operators: AND/OR

diabetic AND foot
diabetes OR diabetic

Exclude a word using the 'minus' sign

Virchow -triad

Use Parentheses

water AND (cup OR glass)

Add an asterisk (*) at end of a word to include word stems

Neuro* will search for Neurology, Neuroscientist, Neurological, and so on

Use quotes to search for an exact phrase

"primary prevention of cancer"
(heart or cardiac or cardio*) AND arrest -"American Heart Association"