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https://www.readbyqxmd.com/read/27869315/aminoalkyl-derivatives-of-8-alkoxypurine-2-6-diones-multifunctional-5-ht1a-5-ht7-receptor-ligands-and-pde-inhibitors-with-antidepressant-activity
#1
Grażyna Chłoń-Rzepa, Agnieszka Zagórska, Paweł Żmudzki, Adam Bucki, Marcin Kołaczkowski, Anna Partyka, Anna Wesołowska, Grzegorz Kazek, Monika Głuch-Lutwin, Agata Siwek, Gabriela Starowicz, Maciej Pawłowski
In the search for potential psychotropic agents, a new series of 3,7-dimethyl- and 1,3-dimethyl-8-alkoxypurine-2,6-dione derivatives of arylpiperazines, perhydroisoquinolines, or tetrahydroisoquinolines with flexible alkylene spacers (5-16 and 21-32) were synthesized and evaluated for 5-HT1A /5-HT7 receptor affinities as well as PDE4B1 and PDE10A inhibitory properties. The 1-(4-(4-(2-hydroxyphenyl)piperazin-1-yl)butyl)-3,7-dimethyl-8-propoxypurine-2,6-dione (16) and 7-(2-hydroxyphenyl)piperazinylalkyl-1,3-dimethyl-8-ethoxypurine-2,6-diones (31 and 32) as potent dual 5-HT1A /5-HT7 receptor ligands with antagonistic activity produced an antidepressant-like effect in the forced swim test in mice...
December 2016: Archiv der Pharmazie
https://www.readbyqxmd.com/read/27777567/distribution-of-5-ht1f-receptors-in-monkey-vestibular-and-trigeminal-ganglion-cells
#2
Habiba O Usman, Carey D Balaban
BACKGROUND: Evidence of serotonergic involvement in vestibular pathway contributions to migraine and balance disorders is compelling. Serotonergic 5-HT1B and 5-HT1D receptors are expressed extensively in inner ear ganglia of monkeys and rats. The serotonergic 5-HT1F receptor is also a target of triptans. This study describes its distribution in vestibular and trigeminal ganglia of monkeys. METHODS: Using primary polyclonal antibodies raised against oligopeptides specific for the human 5-HT1F receptor, neuronal somatic area and intensity of immunoreactive vestibular and trigeminal ganglia were quantified...
2016: Frontiers in Neurology
https://www.readbyqxmd.com/read/27676327/chronic-sarpogrelate-treatment-reveals-5-ht7-receptor-in-the-serotonergic-inhibition-of-the-rat-vagal-bradycardia
#3
José Ángel García-Pedraza, Mónica García, María Luisa Martín, Nélida Eleno, Asunción Morán
5-hydroxytryptamine (5-HT) modulates the cardiac parasympathetic neurotransmission, inhibiting the bradyarrhythmia by 5-HT2 receptor activation. We aimed to determine whether the chronic selective 5-HT2 blockade (sarpogrelate) could modify the serotonergic modulation on vagal cardiac outflow in pithed rat. Bradycardic responses in rats treated with sarpogrelate (30 mg/kg.day; p.o.) were obtained by electrical stimulation of the vagal fibers (3, 6, and 9 Hz) or i.v. injections of acetylcholine (ACh; 1, 5, and 10 μg/kg)...
September 20, 2016: Journal of Cardiovascular Pharmacology
https://www.readbyqxmd.com/read/27570173/zerumbone-alleviates-chronic-constriction-injury-induced-allodynia-and-hyperalgesia-through-serotonin-5-ht-receptors
#4
Jasmine Siew Min Chia, Ahmad Akira Omar Farouk, Azam Shah Mohamad, Mohd Roslan Sulaiman, Enoch Kumar Perimal
Zerumbone, a bioactive sesquiterpene isolated from Zingiber zerumbet (Smith), has shown to exert antiallodynic and antihyperalgesic effects in neuropathic pain mice model in our recent study. The mechanism through which zerumbone alleviates neuropathic pain has yet to be elucidated. Thus, this study aimed to determine whether the serotonergic system, part of the descending pain modulation pathway, contributes to the antineuropathic effect of zerumbone. Participation of the serotonergic system in zerumbone-induced antiallodynia and antihyperalgesia was assessed using Dynamic Plantar Aesthesiometer von Frey test and Hargreaves plantar test respectively in chronic-constriction injury mice model...
August 25, 2016: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/27544651/the-hallucinogen-d-lysergic-diethylamide-lsd-decreases-dopamine-firing-activity-through-5-ht1a-d2-and-taar1-receptors
#5
Danilo De Gregorio, Luca Posa, Rafael Ochoa-Sanchez, Ryan McLaughlin, Sabatino Maione, Stefano Comai, Gabriella Gobbi
d-lysergic diethylamide (LSD) is a hallucinogenic drug that interacts with the serotonin (5-HT) system binding to 5-HT1 and 5-HT2 receptors. Little is known about its potential interactions with the dopamine (DA) neurons of the ventral tegmental area (VTA). Using in-vivo electrophysiology in male adult rats, we evaluated the effects of cumulative doses of LSD on VTA DA neuronal activity, compared these effects to those produced on 5-HT neurons in the dorsal raphe nucleus (DRN), and attempted to identify the mechanism of action mediating the effects of LSD on VTA DA neurons...
August 17, 2016: Pharmacological Research: the Official Journal of the Italian Pharmacological Society
https://www.readbyqxmd.com/read/27531585/5-ht2a-receptor-enhancement-of-contractile-activity-of-the-porcine-urothelium-and-lamina-propria
#6
Christian Moro, Lily Edwards, Russ Chess-Williams
OBJECTIVES: To examine the effect of 5-hydroxytryptamine (5-HT; serotonin) on the contractile properties of the urothelium and lamina propria, as a better understanding of bladder physiology might aid the development of new treatments. METHODS: Strips of porcine urothelium and lamina propria were suspended in gassed Krebs-bicarbonate solution, and cumulative concentration-response curves for 5-HT were generated in the absence and presence of 5-HT antagonists, Nω-nitro-l-arginine and indomethacin...
August 16, 2016: International Journal of Urology: Official Journal of the Japanese Urological Association
https://www.readbyqxmd.com/read/27449278/the-potential-role-of-serotonergic-mechanisms-in-the-spinal-oxytocin-induced-antinociception
#7
Beatriz Godínez-Chaparro, Guadalupe Martínez-Lorenzana, Javier Rodríguez-Jiménez, Alfredo Manzano-García, Gerardo Rojas-Piloni, Miguel Condés-Lara, Abimael González-Hernández
The role of oxytocin (OXT) in pain modulation has been suggested. Indeed, hypothalamic paraventricular nuclei (PVN) electrical stimuli reduce the nociceptive neuronal activity (i.e., neuronal discharge associated with activation of Aδ- and C-fibers) of the spinal dorsal horn wide dynamic range (WDR) cells and nociceptive behavior. Furthermore, raphe magnus nuclei lesion reduces the PVN-induced antinociception, suggesting a functional interaction between the OXT and the serotoninergic system. The present study investigated in Wistar rats the potential role of spinal serotonergic mechanisms in the OXT- and PVN-induced antinociception...
December 2016: Neuropeptides
https://www.readbyqxmd.com/read/27411565/the-electroacupuncture-induced-analgesic-effect-mediated-by-5-ht1-5-ht3-receptor-and-muscarinic-cholinergic-receptors-in-rat-model-of-collagenase-induced-osteoarthritis
#8
Byung-Kwan Seo, Won-Suk Sung, Yeon-Cheol Park, Yong-Hyeon Baek
BACKGROUND: Osteoarthritis (OA) is an degenerative disease characterized by chronic joint pain. Complementary and alternative treatment such as acupuncture have been utilized to alleviate pain. The objective of this study was to investigate the analgesic mechanisms of electroacupuncture (EA) in the collagenase-induced osteoarthritis (CIOA) rat model. METHODS: Four weeks after inducing CIOA by injecting collagenase solution into the left knee of 5-week-old male Sprague-Dawley rats, 2 Hz and 100 Hz EA on Zusanli (ST 36) was performed...
2016: BMC Complementary and Alternative Medicine
https://www.readbyqxmd.com/read/27317942/the-serotonergic-5-ht4-receptor-a-unique-modulator-of-hippocampal-synaptic-information-processing-and-cognition
#9
Hardy Hagena, Denise Manahan-Vaughan
Serotonin (5-hydroxytryptamine, 5-HT) contributes in multifarious ways to the regulation of brain function, spanning key aspects such as the sleep-wake cycle, appetite, mood and mental health. The 5-HT receptors comprise seven receptor families (5-HT1-7) that are further subdivided into 14 receptor subtypes. The role of the 5-HT receptor in the modulation of neuronal excitability has been well documented. Recently, however, it has become apparent that the 5-HT4 receptor may contribute significantly to cognition function and regulates less ostensible aspects of brain function: it engages in metaplastic regulation of synaptic responsiveness in key brain structures such as the hippocampus, thereby specifically promoting persistent forms of synaptic plasticity, and influences the direction of change in synaptic strength in selected hippocampal subfields...
June 15, 2016: Neurobiology of Learning and Memory
https://www.readbyqxmd.com/read/27298498/effect-of-drugs-modulating-serotonergic-system-on-the-analgesic-action-of-paracetamol-in-mice
#10
Yogita S Karandikar, Peeyush Belsare, Aditi Panditrao
OBJECTIVE: The underlying mechanisms for the analgesic action of paracetamol (PCT) are still under considerable debate. It has been recently proposed that PCT may act by modulating the Serotonin system. This study was conducted to verify the influence of Serotonin modulating drugs (buspirone, ondansetron, and fluoxetine) on the analgesic effect of PCT. MATERIALS AND METHODS: Thirty adult albino mice were assigned to five groups: Normal saline, PCT, fluoxetine selective serotonin reuptake inhibitor (SSRI) + PCT, buspirone (5-HT1A Agonist) + PCT, and ondansetron (5HT3 antagonist) + PCT...
May 2016: Indian Journal of Pharmacology
https://www.readbyqxmd.com/read/27260496/calcitonin-alleviates-hyperalgesia-in-osteoporotic-rats-by-modulating-serotonin-transporter-activity
#11
C-B Yeh, S-J Weng, K-W Chang, J Y-H Chan, S-M Huang, T-H Chu, N-K Wei, H-S Ma, J-T Cheng, K-H Ma, T-H Chen, J-F Shyu
: Calcitonin may relieve pain by modulating central serotonin activity. Calcitonin partly reversed the hypersensitivity to pain induced by ovariectomy. This suggests that the anti-nociceptive effects of calcitonin in the treatment of osteoporosis may be mediated by alterations in neural serotonin transporter (SERT) activity. INTRODUCTION: This study used a rat model of osteoporosis to evaluate the role of the cerebral serotonin system in the anti-nociceptive effect of calcitonin, a drug used to treat post-menopausal osteoporosis...
June 3, 2016: Osteoporosis International
https://www.readbyqxmd.com/read/27224020/anxiolytic-effect-of-the-gpr103-receptor-agonist-peptide-p550-homolog-of-neuropeptide-26rfa-in-mice-involvement-of-neurotransmitters
#12
Miklos Palotai, Gyula Telegdy
The GPR103 receptor is a G protein-coupled receptor, which plays a role in several physiological functions. However, the role of the GPR103 receptor in anxiety has not been clarified. The first aim of our study was to elucidate the involvement of the GPR103 receptor in anxious behavior. Mice were treated with peptide P550, which is the mouse homolog of neuropeptide 26RFa and has similar activity for the GPR103 receptor as neuropeptide 26RFa. The anxious behavior was investigated using an elevated plus-maze paradigm...
August 2016: Peptides
https://www.readbyqxmd.com/read/27194102/serotonin-induced-contractile-responses-of-esophageal-smooth-muscle-in-the-house-musk-shrew-suncus-murinus
#13
T Shiina, K Naitou, H Nakamori, Y Suzuki, K Horii, Y Sano, H Shimaoka, Y Shimizu
BACKGROUND: Serotonin (5-hydroxytryptamine, 5-HT) is a regulatory factor in motility of the gastrointestinal tract including the esophagus. Although we proposed that vagal cholinergic and mast cell-derived non-cholinergic components including serotonin coordinately shorten the esophagus, the precise mechanism of serotonin-induced contractions in the suncus esophagus is still unclear. Therefore, the aims of this study were to determine characteristics of contractile responses induced by serotonin and to identify 5-HT receptor subtypes responsible for regulating motility in the suncus esophagus...
May 18, 2016: Neurogastroenterology and Motility: the Official Journal of the European Gastrointestinal Motility Society
https://www.readbyqxmd.com/read/27123427/comparative-study-of-different-combinational-mucoadhesive-formulations-of-sumatriptan-metoclopramide
#14
Mitra Jelvehgari, Hadi Valizadeh, Sanam Ziapour, Mahdieh Rahmani, Seyed Hassan Montazam, Saieede Soltani
PURPOSE: Sumatriptan succinate (Sum) is a Serotonin 5- HT1 receptor agonist, used in the treatment of migraine. It is absorbed rapidly but incompletely when taken orally and underwent first - pass metabolism, resulting in a low bioavailability of about 15%. The aim was to design mucoadhesive buccal discs and sublingual films of Sum and metoclopramide (Met) combined to improve their bioavailability. METHODS: In the current study, the microparticles and films were prepared by emulsion solvent diffusion (ESD) and solvent casting methods, respectively...
March 2016: Advanced Pharmaceutical Bulletin
https://www.readbyqxmd.com/read/27112704/-the-pharmacological-basis-of-the-serotonin-system-application-to-antidepressant-response
#15
D J David, A M Gardier
If serotonin (5-hydroxytryptamin [5-HT]) is well known for its role in mood regulation, it also impacts numerous physiological functions at periphery. Serotonin is synthetized at the periphery into the gut by intestinal enterochromaffin cells and in the central nervous system (CNS) in the raphe nucleus from the essential amino acid tryptophan. Physiological effects of 5-HT are mediated by about 15 serotoninergic receptors grouped into seven broad families (5-HT1, 5-HT2, 5-HT3, 5-HT4, 5-HT5, 5-HT6, 5-HT7 receptor families)...
June 2016: L'Encéphale
https://www.readbyqxmd.com/read/27109474/serotonin-5-ht-and-5-ht2a-receptor-agonists-suppress-lipolysis-in-primary-rat-adipose-cells
#16
Björn Hansson, Anya Medina, Claes Fryklund, Malin Fex, Karin G Stenkula
Serotonin (5-HT) is a biogenic monoamine that functions both as a neurotransmitter and a circulating hormone. Recently, the metabolic effects of 5-HT have gained interest and peripheral 5-HT has been proposed to influence lipid metabolism in various ways. Here, we investigated the metabolic effects of 5-HT in isolated, primary rat adipose cells. Incubation with 5-HT suppressed β-adrenergically stimulated glycerol release and decreased phosphorylation of protein kinase A (PKA)-dependent substrates, hormone sensitive lipase (Ser563) and perilipin (Ser522)...
May 27, 2016: Biochemical and Biophysical Research Communications
https://www.readbyqxmd.com/read/27034327/dominant-and-recessive-mutations-in-the-raf-like-kinase-ht1-gene-completely-disrupt-stomatal-responses-to-co2-in-arabidopsis
#17
Mimi Hashimoto-Sugimoto, Juntaro Negi, Keina Monda, Takumi Higaki, Yasuhiro Isogai, Toshiaki Nakano, Seiichiro Hasezawa, Koh Iba
HT1 (HIGH LEAF TEMPERATURE 1) is the first component associated with changes in stomatal aperture in response to CO2 to be isolated by forward genetic screening. The HT1 gene encodes a protein kinase expressed mainly in guard cells. The loss-of-function ht1-1 and ht1-2 mutants in Arabidopsis thaliana have CO2-hypersensitive stomatal closure with concomitant reductions in their kinase activities in vitro In addition to these mutants, in this study we isolate or obtaine five new ht1 alleles (ht1-3, ht1-4, ht1-5, ht1-6, and ht1-7)...
May 2016: Journal of Experimental Botany
https://www.readbyqxmd.com/read/26876117/dopamine-d2-and-serotonin-5-ht1a-receptor-interaction-in-the-context-of-the-effects-of-antipsychotics-in%C3%A2-vitro-studies
#18
Sylwia Łukasiewicz, Ewa Błasiak, Kinga Szafran-Pilch, Marta Dziedzicka-Wasylewska
The serotonin 5-HT1A receptor (5-HT1 A R) and dopamine D2 receptor (D2 R) have been implicated as important sites of action in antipsychotics. Several lines of evidence indicate the key role of G protein-coupled receptors (GPCRs) heteromers in pathophysiology of schizophrenia and highlight these complexes as novel drug targets. Because heterodimers can form only on those cells co-expressing constituent receptors, they present a target of high pharmacological specificity in the context of biochemical effects induced by antipsychotic drugs...
May 2016: Journal of Neurochemistry
https://www.readbyqxmd.com/read/26875644/pharmacological-characteristics-of-artemisia-vulgaris-l-in-isolated-porcine-basilar-artery
#19
Ha Thi Thanh Nguyen, Hai Thanh Nguyen, Md Zahorul Islam, Takeshi Obi, Pitchaya Pothinuch, Phyu Phyu Khine Zar, De Xing Hou, Thanh Van Nguyen, Tuong Manh Nguyen, Cuong Van Dao, Mitsuya Shiraishi, Atsushi Miyamoto
ETHNOPHARMACOLOGICAL RELEVANCE: In Vietnamese traditional herbalism, there are conflicting opinions about the effect of Artemisia vulgaris L. (AVL, English name: mugwort) on hypertension. Some ethnic doctors recommend the use of AVL for treatment of hypertension, whereas others advise against it. The purpose of this study was to clarify the pharmacological characteristics of AVL in isolated arteries to explain the conflicts surrounding the use of AVL for treatment of hypertension. MATERIALS AND METHODS: We initially performed a functional study using an organ bath system to investigate the effect of AVL extract on isolated porcine basilar artery...
April 22, 2016: Journal of Ethnopharmacology
https://www.readbyqxmd.com/read/26847342/serotonin-promotes-exploitation-in-complex-environments-by-accelerating-decision-making
#20
Shachar Iwanir, Adam S Brown, Stanislav Nagy, Dana Najjar, Alexander Kazakov, Kyung Suk Lee, Alon Zaslaver, Erel Levine, David Biron
BACKGROUND: Fast responses can provide a competitive advantage when resources are inhomogeneously distributed. The nematode Caenorhabditis elegans was shown to modulate locomotion on a lawn of bacterial food in serotonin (5-HT)-dependent manners. However, potential roles for serotonergic signaling in responding to food discovery are poorly understood. RESULTS: We found that 5-HT signaling in C. elegans facilitates efficient exploitation in complex environments by mediating a rapid response upon encountering food...
2016: BMC Biology
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