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5 HT receptors

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https://www.readbyqxmd.com/read/27904941/trpa1-substance-p-histamine-and-5-hydroxytryptamine-interact-in-an-interdependent-way-to-induce-nociception
#1
Luana Fischer, Maria Isabel Lavoranti, Mariana de Oliveira Borges, Alana Farias Miksza, Natalia Fantin Sardi, Bruno Jacson Martynhak, Claudia H Tambeli, Carlos Amílcar Parada
BACKGROUND: Although TRPA1, SP, histamine and 5-hydroxytryptamine (5-HT) have recognized contribution to nociceptive mechanisms, little is known about how they interact with each other to mediate inflammatory pain in vivo. In this study we evaluated whether TRPA1, SP, histamine and 5-HT interact, in an interdependent way, to induce nociception in vivo. METHODS AND RESULTS: The subcutaneous injection of the TRPA1 agonist allyl isothiocyanate (AITC) into the rat's hind paw induced a dose-dependent and short lasting behavioral nociceptive response that was blocked by the co-administration of the TRPA1 antagonist, HC030031, or by the pretreatment with antisense ODN against TRPA1...
November 30, 2016: Inflammation Research: Official Journal of the European Histamine Research Society ... [et Al.]
https://www.readbyqxmd.com/read/27904083/novel-sulfonamide-derivatives-carrying-a-biologically-active-3-4-dimethoxyphenyl-moiety-as-vegfr-2-inhibitors
#2
Mostafa Mohammed Ghorab, Mansour Sulaiman Alsaid, Yassin Mohammed Nissan, Abdelkader Elbadawy Ashour, Abdullah Abdulalrahman Al-Mishari, Ashok Kumar, Sheikh Fayaz Ahmed
Novel sulfonamides 3-19 with a biologically active 3,4-dimethoxyphenyl moiety were designed and synthesized. The structures of the synthesized compounds were established using elemental analyses, IR, (1)H-NMR, (13)C-NMR spectral data and mass spectroscopy. All the synthesized compounds were evaluated for their in vitro anticancer activity against four cancer cell lines, namely human hepatocellular carcinoma (HepG2), human medulloblastoma (Daoy), human cervical cancer (HeLa), and human colon cancer (HT-29), by using a 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay and dasatinib as the reference drug...
2016: Chemical & Pharmaceutical Bulletin
https://www.readbyqxmd.com/read/27901065/pharmacological-characterization-of-a-high-affinity-p-tyramine-transporter-in-rat-brain-synaptosomes
#3
Mark D Berry, Shannon Hart, Anthony R Pryor, Samantha Hunter, Danielle Gardiner
p-Tyramine is an archetypal member of the endogenous family of monoamines known as trace amines, and is one of the endogenous agonists for trace amine-associated receptor (TAAR)1. While much work has focused on the function of TAAR1, very little is known about the regulation of the endogenous agonists. We have previously reported that p-tyramine readily crosses lipid bilayers and that its release from synaptosomes is non-exocytotic. Such release, however, showed characteristics of modification by one or more transporters...
November 30, 2016: Scientific Reports
https://www.readbyqxmd.com/read/27897266/evaluation-of-association-of-common-variants-in-htr1a-and-htr5a-with-schizophrenia-and-executive-function
#4
Fanglin Guan, Huali Lin, Gang Chen, Lu Li, Teng Chen, Xinshe Liu, Jiuqiang Han, Tao Li
The 5-HT1A receptor (HTR1A) and the 5-HT5A receptor (HTR5A) are key 5-HT receptors with distinct inhibitory functions. Studies have been conducted to investigate the association of a few HTR1A polymorphisms with schizophrenia, producing conflicting results, and the relationship between HTR5A and schizophrenia has not yet been well investigated. We aimed to examine the association of HTR1A and HTR5A with schizophrenia and executive function. The study included a discovery stage with 1,115 patients and 2,289 controls and a replication stage with 2,128 patients and 3,865 controls...
November 29, 2016: Scientific Reports
https://www.readbyqxmd.com/read/27896310/preservation-of-essential-odor-guided-behaviors-and-odor-based-reversal-learning-after-targeting-adult-brain-serotonin-synthesis
#5
Kaitlin S Carlson, Meredith S Whitney, Marie A Gadziola, Evan S Deneris, Daniel W Wesson
The neurotransmitter serotonin (5-HT) is considered a powerful modulator of sensory system organization and function in a wide range of animals. The olfactory system is innervated by midbrain 5-HT neurons into both its primary and secondary odor-processing stages. Facilitated by this circuitry, 5-HT and its receptors modulate olfactory system function, including odor information input to the olfactory bulb. It is unknown, however, whether the olfactory system requires 5-HT for even its most basic behavioral functions...
September 2016: ENeuro
https://www.readbyqxmd.com/read/27894797/roles-of-the-serotonin-5-ht4-receptor-in-dendrite-formation-of-the-rat-hippocampal-neurons-in-vitro
#6
Naoki Kozono, Akiko Ohtani, Takashi Shiga
Serotonin (5-HT) is involved in various aspects of hippocampal development, although the specific roles of 5-HT receptors are poorly understood. We investigated the roles of 5-HT receptors in the dendrite formation of hippocampal neurons. We focused on the 5-HT4 receptor, which is coupled with Gs protein, and compared the effects with those of the Gi-coupled 5-HT1A receptor. Neurons from rat hippocampi at embryonic day 18 were dissociated and treated for 4 days with the 5-HT4 receptor agonist BIMU8 or the 5-HT1A receptor agonist 8-OH DPAT...
November 25, 2016: Brain Research
https://www.readbyqxmd.com/read/27891703/an-investigation-into-the-inhibitory-function-of-serotonin-in-diffuse-noxious-inhibitory-controls-in-the-neuropathic-rat
#7
K Bannister, S Lockwood, L Goncalves, R Patel, A H Dickenson
BACKGROUND: Following neuropathy α2-adrenoceptor-mediated diffuse noxious inhibitory controls (DNIC), whereby a noxious conditioning stimulus inhibits the activity of spinal wide dynamic range (WDR) neurons, are abolished, and spinal 5-HT7 receptor densities are increased. Here, we manipulate spinal 5-HT content in spinal nerve ligated (SNL) animals and investigate which 5-HT receptor mediated actions predominate. METHODS: Using in vivo electrophysiology we recorded WDR neuronal responses to von frey filaments applied to the hind paw before, and concurrent to, a noxious ear pinch (the conditioning stimulus) in isoflurane-anaesthetised rats...
November 28, 2016: European Journal of Pain: EJP
https://www.readbyqxmd.com/read/27890601/tramadol-effects-on-sexual-behavior-in-male-rats-are-mainly-caused-by-its-5-ht-reuptake-blocking-effects
#8
Jocelien D A Olivier, Diana C Esquivel Franco, Ronald Oosting, Marcel Waldinger, Zoltan Sarnyai, Berend Olivier
Tramadol is a well-known and effective analgesic. Recently it was shown that tramadol is also effective in human premature ejaculation. The inhibitory effect of tramadol on the ejaculation latency is probably due to its mechanism of action as a μ-opioid receptor agonist and noradrenaline/serotonin (5-HT) reuptake inhibitor. In order to test this speculation, we tested several doses of tramadol in a rat model of male sexual behavior and investigated two types of drugs interfering with the μ-opioid and the 5-HT system...
November 24, 2016: Neuropharmacology
https://www.readbyqxmd.com/read/27890559/fluoxetine-and-its-active-metabolite-norfluoxetine-disrupt-estrogen-synthesis-in-a-co-culture-model-of-the-feto-placental-unit
#9
Andrée-Anne Hudon Thibeault, Laetitia Laurent, Sung Vo Duy, Sébastien Sauvé, Patrick Caron, Chantal Guillemette, J Thomas Sanderson, Cathy Vaillancourt
The effects of fluoxetine, one of the most prescribed selective serotonin-reuptake inhibitors (SSRIs) during pregnancy, and its active metabolite norfluoxetine were studied on placental aromatase (CYP19) and feto-placental steroidogenesis Fluoxetine did not alter estrogen secretion in co-culture of fetal-like adrenocortical (H295R) and trophoblast-like (BeWo) cells used as a model of the feto-placental unit, although it induced CYP19 activity, apparently mediated by the serotonin (5-HT) 2A receptor/PKC signalling pathway...
November 24, 2016: Molecular and Cellular Endocrinology
https://www.readbyqxmd.com/read/27888284/attenuation-of-the-anxiogenic-effects-of-cocaine-by-5-ht1b-autoreceptor-stimulation-in-the-bed-nucleus-of-the-stria-terminalis-of-rats
#10
Adam K Klein, Michael A Brito, Sayeh Akhavan, Dylan R Flanagan, Nikki Le, Tatum Ohana, Anand S Patil, Erin M Purvis, Carl Provenzano, Alex Wei, Lucy Zhou, Aaron Ettenberg
RATIONALE: Cocaine produces significant aversive/anxiogenic actions whose underlying neurobiology remains unclear. A possible substrate contributing to these actions is the serotonergic (5-HT) pathway projecting from the dorsal raphé (DRN) to regions of the extended amygdala, including the bed nucleus of the stria terminalis (BNST) which have been implicated in the production of anxiogenic states. OBJECTIVES: The present study examined the contribution of 5-HT signaling within the BNST to the anxiogenic effects of cocaine as measured in a runway model of drug self-administration...
November 25, 2016: Psychopharmacology
https://www.readbyqxmd.com/read/27882537/neurochemical-and-behavioral-effects-of-hypidone-hydrochloride-yl-0919-a-novel-combined-selective-serotonin-reuptake-inhibitor-and-partial-5-ht1a-agonist
#11
Li-Ming Zhang, Xiao-Yun Wang, Nan Zhao, Yu-Lu Wang, Xiao-Xu Hu, Yu-Hua Ran, Yan-Qin Liu, You-Zhi Zhang, Ri-Fang Yang, Yun-Feng Li
The purpose of the present study was to investigate the pharmacology of hypidone hydrochloride (YL-0919), a novel selective serotonin reuptake inhibitor (SSRI) and 5-hydroxytryptamine (5-HT)1A receptor agonist with high affinity for serotonin transporter (SERT) and 5-HT1A receptors. YL-0919 promoted [(35) S]GTPγ S binding at 85% of the magnitude of the full 5-HT1A receptor agonist 8-hydroxy-2-(di-n-propylamino) tetralin (8-OH-DPAT), suggesting that YL-0919 is a high-efficacy partial agonist of 5-HT1A receptors...
November 24, 2016: British Journal of Pharmacology
https://www.readbyqxmd.com/read/27872865/cxcr3-ccr5-and-crth2-chemokine-receptor-expression-in-lymphocytes-infiltrating-thyroid-nodules-with-coincident-hashimoto-s-thyroiditis-obtained-by-fine-needle-aspiration-biopsy
#12
Jan Jiskra, Marie Antošová, Jan Krátký, Hana Vítková, Zdeňka Límanová, Helena Marečková, Eliška Potluková
Objective. To determine the expression of chemokine receptors in lymphocytes from thyroid nodules and peripheral blood in patients with and without Hashimoto's thyroiditis (HT). Patients and Methods. The study included 46 women with thyroid nodules and HT and 60 women with thyroid nodules without HT (controls) who underwent a fine needle aspiration biopsy (FNAB). Expression of chemokine receptors CXCR3, CCR5, and CRTH2 was assessed by flow cytometry in lymphocytes from FNAB samples and from peripheral blood...
2016: Journal of Immunology Research
https://www.readbyqxmd.com/read/27871326/tryptophan-hydroxylase-1-and-5-ht7-receptor-preferentially-expressed-in-triple-negative-breast-cancer-promote-cancer-progression-through-autocrine-serotonin-signaling
#13
Jaya Gautam, Suhrid Banskota, Sushil Chandra Regmi, Subi Ahn, Yong Hyun Jeon, Hyunyoung Jeong, Seung Joo Kim, Tae-Gyu Nam, Byeong-Seon Jeong, Jung-Ae Kim
BACKGROUND: Triple-negative breast cancer (TNBC) has a high risk of relapse and there are few chemotherapy options. Although 5-hydroxytryptamine (5-HT, serotonin) signaling pathways have been suggested as potential targets for anti-cancer drug development, the mechanism responsible for the action of 5-HT in TNBC remains unknown. METHODS: Quantitative real-time polymerase chain reaction (qRT-PCR) and Western blotting were used to measure mRNA and protein levels, respectively...
November 21, 2016: Molecular Cancer
https://www.readbyqxmd.com/read/27866999/the-5-ht1a-1b-receptor-agonist-eltoprazine-increases-both-catecholamine-release-in-the-prefrontal-cortex-and-dopamine-release-in-the-nucleus-accumbens-and-decreases-motivation-for-reward-and-waiting-impulsivity-but-increases-stopping-impulsivity
#14
S Mechiel Korte, Jolanda Prins, Filip S Van den Bergh, Ronald S Oosting, Rudy Dupree, Gerdien A H Korte-Bouws, Koen G C Westphal, Berend Olivier, Damiaan A Denys, Alexis Garland, Onur Güntürkün
The 5-HT1A/1B-receptor agonist eltoprazine has a behavioral drug signature that resembles that of a variety of psychostimulant drugs, despite the differences in receptor binding profile. These psychostimulants are effective in treating impulsivity disorders, most likely because they increase norepinephrine (NE) and dopamine (DA) levels in the prefrontal cortex. Both amphetamine and methylphenidate, however, also increase dopamine levels in the nucleus accumbens (NAc), which has a significant role in motivation, pleasure, and reward...
November 17, 2016: European Journal of Pharmacology
https://www.readbyqxmd.com/read/27862146/maternal-25-hydroxyvitamin-d-is-inversely-correlated-with-fetal-serotonin
#15
Padma Murthi, Miranda Davies-Tuck, Martha Lappas, Harmeet Singh, Joanne Mockler, Rahana Rahman, Rebecca Lim, Bryan Leaw, James Doery, Euan M Wallace, Peter R Ebeling
OBJECTIVE: Maternal vitamin D deficiency during pregnancy has been linked to impaired neurocognitive development in childhood. The mechanism by which vitamin D affects childhood neurocognition is unclear but may be via interactions with serotonin, a neurotransmitter involved in fetal brain development. In this study we aimed to explore associations between maternal and fetal vitamin D concentrations, and fetal serotonin concentrations at term. STUDY DESIGN AND MEASUREMENTS: Serum 25-hydroxyitamin D (25(OH)D, nmol/L) and serotonin (5-HT, nmol/L) concentrations were measured in maternal and umbilical cord blood from mother-infant pairs (n=64)...
November 12, 2016: Clinical Endocrinology
https://www.readbyqxmd.com/read/27861439/trends-in-tramadol-pharmacology-metabolism-and-misuse
#16
Karen Miotto, Arthur K Cho, Mohamed A Khalil, Kirsten Blanco, Jun D Sasaki, Richard Rawson
Tramadol is a unique analgesic medication, available in variety of formulations, with both monoaminergic reuptake inhibitory and opioid receptor agonist activity increasingly prescribed worldwide as an alternative for high-affinity opioid medication in the treatment of acute and chronic pain. It is a prodrug that is metabolized by cytochrome P450 (CYP) enzymes CYP2D6 and CYP3A4 to its more potent opioid analgesic metabolites, particularly the O-demethylation product M1. The opioid analgesic potency of a given dose of tramadol is influenced by an individual's CYP genetics, with poor metabolizers experiencing little conversion to the active M1 opioid metabolite and individuals with a high metabolic profile, or ultra-metabolizers, experiencing the greatest opioid analgesic effects...
November 17, 2016: Anesthesia and Analgesia
https://www.readbyqxmd.com/read/27857753/serotonin-regulates-brain-derived-neurotrophic-factor-expression-in-select-brain-regions-during-acute-psychological-stress
#17
De-Guo Jiang, Shi-Li Jin, Gong-Ying Li, Qing-Qing Li, Zhi-Ruo Li, Hong-Xia Ma, Chuan-Jun Zhuo, Rong-Huan Jiang, Min-Jie Ye
Previous studies suggest that serotonin (5-HT) might interact with brain-derived neurotrophic factor (BDNF) during the stress response. However, the relationship between 5-HT and BDNF expression under purely psychological stress is unclear. In this study, one hour before psychological stress exposure, the 5-HT1A receptor agonist 8-OH-DPAT or antagonist MDL73005, or the 5-HT2A receptor agonist DOI or antagonist ketanserin were administered to rats exposed to psychological stress. Immunohistochemistry and in situ hybridization revealed that after psychological stress, with the exception of the ventral tegmental area, BDNF protein and mRNA expression levels were higher in the 5-HT1A and the 5-HT2A receptor agonist groups compared with the solvent control no-stress or psychological stress group in the CA1 and CA3 of the hippocampus, prefrontal cortex, central amygdaloid nucleus, dorsomedial hypothalamic nucleus, dentate gyrus, shell of the nucleus accumbens and the midbrain periaqueductal gray...
September 2016: Neural Regeneration Research
https://www.readbyqxmd.com/read/27857126/repeated-7-day-treatment-with-the-5-ht2c-agonist-lorcaserin-or-the-5-ht2a-antagonist-pimavanserin-alone-or-in-combination-fails-to-reduce-cocaine-vs-food-choice-in-male-rhesus-monkeys
#18
Matthew L Banks, S Stevens Negus
Cocaine use disorder is a global public health problem for which there are no Food and Drug Administration-approved pharmacotherapies. Emerging preclinical evidence has implicated both serotonin (5-HT) 2C and 2A receptors as potential mechanisms for mediating serotonergic attenuation of cocaine abuse-related neurochemical and behavioral effects. Therefore, the present study aim was to determine whether repeated 7-day treatment with the 5-HT2C agonist lorcaserin (0.1-1.0 mg/kg/day, intramuscular; 0.032-0.1 mg/kg/h, intravenous) or the 5-HT2A inverse agonist/antagonist pimavanserin (0...
November 18, 2016: Neuropsychopharmacology: Official Publication of the American College of Neuropsychopharmacology
https://www.readbyqxmd.com/read/27856786/a-high-resolution-in-vivo-atlas-of-the-human-brain-s-serotonin-system
#19
Vincent Beliveau, Melanie Ganz, Ling Feng, Brice Ozenne, Liselotte Højgaard, Patrick M Fisher, Claus Svarer, Douglas N Greve, Gitte M Knudsen
: The serotonin (5-HT) system modulates many important brain functions and is critically involved in many neuropsychiatric disorders. We here present a high-resolution multi-dimensional in vivo atlas of four of the human brain's 5-HT receptors (5-HT1A, 5-HT1B, 5-HT2A, and 5-HT4) as well as of the 5-HT transporter (5-HTT). The atlas is created from molecular and structural high-resolution neuroimaging data consisting of Positron Emission Tomography (PET) and Magnetic Resonance Imaging (MRI) scans, acquired in a total of 210 healthy individuals...
November 17, 2016: Journal of Neuroscience: the Official Journal of the Society for Neuroscience
https://www.readbyqxmd.com/read/27852128/antagonistic-effects-of-gingko-biloba-and-sophora-japonica-on-cerebral-vasoconstriction-in-response-to-histamine-5-hydroxytryptamine-u46619-and-bradykinin
#20
Ha Thi Thanh Nguyen, Hai Thanh Nguyen, Md Zahorul Islam, Takeshi Obi, Pitchaya Pothinuch, Thanh Van Nguyen, Tuong Manh Nguyen, Cuong Van Dao, Mitsuya Shiraishi, Atsushi Miyamoto
The aim of this study was to evaluate, for the first time, the antagonistic effects of Gingko biloba leaf (GB) and Sophora japonica L. flower bud (SJ) extracts on cerebral vasoconstriction in response to KCl, extracellular Ca[Formula: see text], histamine, 5-hydroxytryptamine (5-HT), 9,11-dideoxy-9[Formula: see text],11[Formula: see text]-methanoepoxy prostaglandin (PG) F[Formula: see text](U46619) and bradykinin (BK), in order to explain their traditional application for diseases associated with cerebral vasospasm...
November 16, 2016: American Journal of Chinese Medicine
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