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5 HT receptors

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https://www.readbyqxmd.com/read/28103616/l-lysine-acts-as-a-serotonin-type-4-receptor-antagonist-to-counteract-in-vitro-and-in-vivo-the-stimulatory-effect-of-serotonergic-agents-on-aldosterone-secretion-in-man
#1
C Duparc, C André, J Ménard, B Godouet-Getti, J Wils, A F Cailleux, L Moreau-Grangé, E Louiset, H Lefebvre
In the normal human adrenal gland, serotonin (5-HT) stimulates aldosterone secretion through the 5-HT4 receptor (5-HT4R). However, the physiological role of the serotonergic control of adrenocortical function is not known. In the present study, we have investigated the ability of l-Lysine, which has been shown to act as a 5-HT4 receptor antagonist, to counteract in vitro and in vivo the stimulatory effect of 5-HT4R agonists on aldosterone production. l-Lysine was found to inhibit aldosterone production induced by 5-HT and the 5-HT4R agonists BIMU8 from cultured human adrenocortical cells...
January 19, 2017: Hormone and Metabolic Research, Hormon- und Stoffwechselforschung, Hormones et Métabolisme
https://www.readbyqxmd.com/read/28103158/serotonin-receptor-targeted-therapy-for-migraine-treatment-an-overview-of-drugs-in-phase-i-and-ii-clinical-development
#2
P Barbanti, C Aurilia, G Egeo, L Fofi, R Palmirotta
Research has focused on serotonin (5-HT) 5-HT1D and 5-HT1F receptors to develop drugs acting through non-vasoconstrictive mechanisms for treating acute migraine and those targeting 5-HT2B and 5-HT7 receptors for preventing migraine. Areas covered: This paper reviews antimigraine drugs targeting 5-HT receptors in one phase I trial (sumatriptan iontophoretic transdermal system, TDS) and five phase II clinical trials (PNU-142633, LY334370, lasmiditan, NOX-188). Expert opinion: Data from our overview on investigational drugs in phase I and II clinical trials using the 5-HT1B/1D receptor agonist (sumatriptan TDS), 5-HT1D receptor agonist (PNU-142633), 5-HT1F receptor agonists (LY334370, lasmiditan) and a combined 5-HT1B/1D receptor agonist with nNOS inhibition (NOX-188) provided encouraging data for sumatriptan TDS and lasmiditan, disappointing results for PNU-142633, and promising findings for NOX-188...
January 19, 2017: Expert Opinion on Investigational Drugs
https://www.readbyqxmd.com/read/28087766/control-of-amygdala-circuits-by-5-ht-neurons-via-5-ht-and-glutamate-co-transmission
#3
Ayesha Sengupta, Marco Bocchio, David M Bannerman, Trevor Sharp, Marco Capogna
: The serotonin (5-HT) system and the amygdala are key regulators of emotional behavior. Several lines of evidence suggest that 5-HT transmission in the amygdala is implicated in the susceptibility and drug treatment of mood disorders. Thus, elucidating the physiological mechanisms through which midbrain 5-HT neurons modulate amygdala circuits could be pivotal in understanding emotional regulation in health and disease. To shed light on these mechanisms, we performed patch-clamp recordings from basal amygdala (BA) neurons in brain slices from mice with channelrhodopsin (ChR2) genetically targeted to 5-HT neurons...
January 13, 2017: Journal of Neuroscience: the Official Journal of the Society for Neuroscience
https://www.readbyqxmd.com/read/28076682/effect-of-maternal-%C3%A2-citalopram-exposure-on-p11-expression-and-neurogenesis-in-the-mouse-fetal-brain
#4
Jennifer R King, Juan C Velasquez, Masaaki Torii, Alexandre Bonnin
Fetal exposure to selective serotonin reuptake inhibitors (SSRI) has been associated with increased risk of adverse neurodevelopmental outcomes. In the adult brain, SSRI therapy regulates p11 (s100a10) expression and alters neurogenesis. The protein p11 indirectly regulates 5-HT signaling through 5-HT1B/D receptors. In the fetal brain, signaling through these receptors modulates axonal circuit formation. We determined whether p11 is expressed in the fetal mouse brain, and whether maternal SSRI exposure affects fetal p11 expression and neurogenesis...
January 13, 2017: ACS Chemical Neuroscience
https://www.readbyqxmd.com/read/28075185/cerebellar-heterogeneity-and-its-impact-on-pet-data-quantification-of-5-ht-receptor-radioligands
#5
Melanie Ganz, Ling Feng, Hanne Demant Hansen, Vincent Beliveau, Claus Svarer, Gitte M Knudsen, Douglas N Greve
In the quantification of positron emission tomography (PET) radiotracer binding, a commonly used method is reference tissue modeling (RTM). RTM necessitates a proper reference and a ubiquitous choice for G-protein coupled receptors is the cerebellum. We investigated regional differences in uptake within the grey matter of the cerebellar hemispheres (CH), the cerebellar white matter (CW), and the cerebellar vermis (CV) for five PET radioligands targeting the serotonin system. Furthermore, we evaluated the impact of choosing different reference regions when quantifying neocortical binding...
January 1, 2017: Journal of Cerebral Blood Flow and Metabolism
https://www.readbyqxmd.com/read/28074670/metabolism-of-psilocybin-and-psilocin-clinical-and-forensic-toxicological-relevance
#6
Ricardo Jorge Dinis-Oliveira
Psilocybin and psilocin are controlled substances in many countries. These are the two main hallucinogenic compounds of the "magic mushrooms" and both act as agonists or partial agonists at 5-hydroxytryptamine (5-HT)2A subtype receptors. During the last few years, psilocybin and psilocin have gained therapeutic relevance but considerable physiological variability between individuals that can influence dose-response and toxicological profile has been reported. This review aims to discuss metabolism of psilocybin and psilocin, by presenting all major and minor psychoactive metabolites...
January 11, 2017: Drug Metabolism Reviews
https://www.readbyqxmd.com/read/28059140/identification-and-functional-characterisation-of-5-ht4-receptor-in-sea-cucumber-apostichopus-japonicus-selenka
#7
Tianming Wang, Zhen Yang, Naiming Zhou, Lina Sun, Zhenming Lv, Changwen Wu
Serotonin (5-HT) is an important neurotransmitter and neuromodulator that controls a variety of sensory and motor functions through 5-HT receptors (5-HTRs). The 5-HT4R subfamily is linked to Gs proteins, which activate adenylyl cyclases (ACs), and is involved in many responses in peripheral organs. In this study, the 5-HT4R from Apostichopus japonicus (Aj5-HT4R) was identified and characterised. The cloned full-length Aj5-HT4R cDNA is 1,544 bp long and contains an open reading frame 1,011 bp in length encoding 336 amino acid proteins...
January 6, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28058604/distribution-of-serotonin-and-fmrf-amide-in-the-nervous-system-of-different-zooidal-types-of-cheilostome-bryozoa-a-case-study-of-arctonula-arctica
#8
K M Serova, A E Vishnyakov, O V Zaitseva, A N Ostrovsky
In the White Sea bryozoans Arctonula arctica, the structure of the nervous system and distribution of 5-hydroxytryptamine (5-HT) and FMRF-amide were studied for the first time using immunohistochemical methods and confocal scanning microscopy. The neurotransmitters studied have been actively involved into the integrative processes, gut functioning, and regulation of motion activity. In avicularia, 5-HT and FMRF-amide receptors are capable of performing the same functions, except for participation in the gut functioning, because they have no digestive system...
November 2016: Doklady Biological Sciences: Proceedings of the Academy of Sciences of the USSR, Biological Sciences Sections
https://www.readbyqxmd.com/read/28057524/involvement-of-presynaptic-5-ht1a-receptors-in-the-low-propensity-of-brexpiprazole-to-induce-extrapyramidal-side-effects-in-rats
#9
Cedric Mombereau, Jørn Arnt, Arne Mørk
Previous studies have shown that partial and full 5-HT1A receptor agonists reduce antipsychotic-induced catalepsy. Consequently, some antipsychotics combining balanced efficacy between dopamine (DA) D2 antagonism or partial agonism and 5-HT1A receptor agonism have a low propensity to induce extrapyramidal side effects (EPS), as reflected by low cataleptogenic activity in rodents. In the present experiments, we attempted to explore the importance of pre- and postsynaptic 5-HT1A agonistic properties of brexpiprazole and aripiprazole in the context of neurological side-effect liabilities...
January 3, 2017: Pharmacology, Biochemistry, and Behavior
https://www.readbyqxmd.com/read/28053817/pretreatment-with-ginseng-fruit-saponins-affects-serotonin-expression-in-an-experimental-comorbidity-model-of-myocardial-infarction-and-depression
#10
Mei-Yan Liu, Yan-Ping Ren, Li-Jun Zhang, Jamie Y Ding
We previously demonstrated that serotonin (5-HT) and 5-HT2A receptor (5-HT2AR) levels in platelets were up- or down-regulated after myocardial infarction (MI) associated with depression. In this study, we further evaluated the effects of pretreatment with ginseng fruit saponins (GFS) on the expression of 5-HT and 5-HT2AR in MI with or without depression. Eighty Sprague-Dawley (SD) rats were treated with saline and GFS (n=40 per group). The animals were then randomly divided into four subgroups: sham, MI, depression, and MI + depression (n=10 per subgroup)...
December 2016: Aging and Disease
https://www.readbyqxmd.com/read/28053035/a-high-resolution-in-vivo-atlas-of-the-human-brain-s-serotonin-system
#11
Vincent Beliveau, Melanie Ganz, Ling Feng, Brice Ozenne, Liselotte Højgaard, Patrick M Fisher, Claus Svarer, Douglas N Greve, Gitte M Knudsen
: The serotonin (5-hydroxytryptamine, 5-HT) system modulates many important brain functions and is critically involved in many neuropsychiatric disorders. Here, we present a high-resolution, multidimensional, in vivo atlas of four of the human brain's 5-HT receptors (5-HT1A, 5-HT1B, 5-HT2A, and 5-HT4) and 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...
January 4, 2017: Journal of Neuroscience: the Official Journal of the Society for Neuroscience
https://www.readbyqxmd.com/read/28049192/combined-memantine-and-donepezil-treatment-improves-behavioral-and-psychological-symptoms-of-dementia-like-behaviors-in-olfactory-bulbectomized-mice
#12
Yasushi Yabuki, Kazuya Matsuo, Koga Hirano, Yasuharu Shinoda, Shigeki Moriguchi, Kohji Fukunaga
Memantine, an uncompetitive N-methyl-D-aspartate receptor antagonist, and the cholinesterase inhibitor, donepezil, are approved in most countries for treating moderate-to-severe Alzheimer's disease (AD). These drugs have different molecular targets; thus, it is expected that the effects of combined treatment would be synergistic. Some reports do show memantine/donepezil synergy in ameliorating cognition in AD model animals, but their combined effects on behavioral and psychological symptoms of dementia (BPSD)-like behaviors have not been addressed...
January 4, 2017: Pharmacology
https://www.readbyqxmd.com/read/28040566/marked-sexual-dimorphism-in-5-ht1-receptors-mediating-pronociceptive-effects-of-sumatriptan
#13
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/28034961/role-of-prefrontal-serotonergic-and-dopaminergic-systems-in-encounter-induced-hyperactivity-in-methamphetamine-sensitized-mice
#14
Tatsunori Tanaka, Yukio Ago, Chiaki Umehara, Emina Imoto, Shigeru Hasebe, Hitoshi Hashimoto, Kazuhiro Takuma, Toshio Matsuda
BACKGROUND: Isolation-reared mice show social encounter-induced hyperactivity with activation of prefrontal serotonergic and dopaminergic systems, but it is not known whether this stress response is observed in other pathological conditions. Here we examined whether the social encounter stimulation induces abnormal behavior during withdrawal in chronic methamphetamine (METH)-treated mice. METHODS: To induce METH-induced behavioral sensitization, male mice were injected with METH (1 mg/kg) once daily for 7 days...
December 29, 2016: International Journal of Neuropsychopharmacology
https://www.readbyqxmd.com/read/28034785/modulation-of-the-consolidation-and-reconsolidation-of-fear-memory-by-three-different-serotonin-receptors-in-hippocampus
#15
S D Schmidt, C R G Furini, C G Zinn, L E Cavalcante, F F Ferreira, J A K Behling, J C Myskiw, I Izquierdo
The process of memory formation is complex and highly dynamic. During learning, the newly acquired information is found in a fragile and labile state. Through a process known as consolidation, which requires specific mechanisms such as protein synthesis, the memory trace is stored and stabilized. It is known that when a consolidated memory is recalled, it again becomes labile and sensitive to disruption. To be maintained, this memory must undergo an additional process of restabilization called reconsolidation, which requires another phase of protein synthesis...
December 27, 2016: Neurobiology of Learning and Memory
https://www.readbyqxmd.com/read/28025094/serotonergic-mechanisms-of-trigeminal-meningeal-nociception-implications-for-migraine-pain
#16
Erkan Kilinc, Cindy Guerrero-Toro, Andrey Zakharov, Carmela Vitale, Max Gubert-Olive, Ksenia Koroleva, Arina Timonina, Liliana L Luz, Irina Shelukhina, Raisa Giniatullina, Fatma Tore, Boris V Safronov, Rashid Giniatullin
Serotonergic mechanisms play a central role in migraine pathology. However, the region-specific effects of serotonin (5-HT) mediated via multiple types of receptors in the nociceptive system are poorly understood. Using extracellular and patch-clamp recordings, we studied the action of 5-HT on the excitability of peripheral and central terminals of trigeminal afferents. 5-HT evoked long-lasting TTX-sensitive firing in the peripheral terminals of meningeal afferents, the origin site of migraine pain. Cluster analysis revealed that in majority of nociceptive fibers 5-HT induced either transient or persistent spiking activity with prevailing delta and theta rhythms...
December 23, 2016: Neuropharmacology
https://www.readbyqxmd.com/read/28017279/cardiovascular-remodeling-and-the-peripheral-serotonergic-system
#17
REVIEW
Estelle Ayme-Dietrich, Gaëlle Aubertin-Kirch, Luc Maroteaux, Laurent Monassier
Plasma 5-hydroxytryptamine (5-HT; serotonin), released from blood platelets, plays a major role in the human cardiovascular system. Besides the effect of endogenous serotonin, many drugs targeting serotonergic receptors are widely used in the general population (antiobesity agents, antidepressants, antipsychotics, antimigraine agents), and may enhance the cardiovascular risk. Depending on the type of serotonin receptor activated and its location, the use of these compounds triggers acute and chronic effects...
December 21, 2016: Archives of Cardiovascular Diseases
https://www.readbyqxmd.com/read/28013061/voltage-and-receptor-mediated-activation-of-a-non-selective-cation-channel-in-rat-carotid-body-glomus-cells
#18
Jiaju Wang, James O Hogan, Donghee Kim
A recent study showed that hypoxia activates a Ca(2+)-sensitive, Na(+)-permeable non-selective cation channel (NSC) in carotid body glomus cells. We studied the effects of mitochondrial inhibitors that increase Ca(2+) influx via Ca(2+) channel (Cav), and receptor agonists that release Ca(2+) from endoplasmic reticulum (ER) on NSC. Mitochondrial inhibitors (NaCN, FCCP, H2S, NO) elevated [Ca(2+)]i and activated NSC. Angiotensin II and acetylcholine that elevate [Ca(2+)]i via the Gq-IP3 pathway activated NSC. However, endothelin-1 (Gq) and 5-HT (Gq) showed little or no effect on [Ca(2+)]i and did not activate NSC...
December 21, 2016: Respiratory Physiology & Neurobiology
https://www.readbyqxmd.com/read/28013000/galanin-contributes-to-monoaminergic-dysfunction-and-to-dependent-neurobehavioral-comorbidities-of-epilepsy
#19
Jesus-Servando Medel-Matus, Don Shin, Raman Sankar, Andrey Mazarati
Status epilepticus (SE) in rats, along with chronic epilepsy, leads to the development of behavioral impairments resembling depressive disorder and/or attention deficit/hyperactivity disorder (ADHD), thus reflecting respective comorbidities in epilepsy patients. Suppressed neurotransmitter tone in the raphe nucleus (RN)-prefrontal cortex (PFC) serotonergic pathway and in the locus coeruleus (LC)-PFC noradrenergic pathway underlies depressive- and impulsive-like behavioral deficits respectively. We examined possible mechanisms leading to the monoamine dysfunction in brainstem efferents, namely modulatory effects of the neuropeptide galanin on serotonin (5-HT) and norepinephrine (NE) signaling...
December 22, 2016: Experimental Neurology
https://www.readbyqxmd.com/read/28012846/neuroprotection-of-agomelatine-against-cerebral-ischemia-reperfusion-injury-through-an-antiapoptotic-pathway-in-rat
#20
Wijitra Chumboatong, Sarinthorn Thummayot, Piyarat Govitrapong, Chainarong Tocharus, Jinatta Jittiwat, Jiraporn Tocharus
Agomelatine is an agonist of the melatonergic MT1/MT2 receptors and an antagonist of the serotonergic 5-HT receptors. Its actions mimic melatonin in antioxidative and anti-inflammation. However, the protective mechanism of agomelatine in ischemic/reperfusion (I/R) injury has not been investigated. In this study, cerebral I/R injury rats were induced by middle cerebral artery occlusion (MCAO) for 2 h followed by reperfusion. The rats were randomly divided into 6 groups (12 rats per group): sham-operated; vehicle-treated I/R; 20 mg/kg, 40 mg/kg, and 80 mg/kg agomelatine-treated I/R; and 10 mg/kg melatonin-treated I/R...
January 2017: Neurochemistry International
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