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Serotonin receptor subtype

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https://www.readbyqxmd.com/read/28745513/modulating-the-serotonin-receptor-spectrum-of-pulicatin-natural-products
#1
Zhenjian Lin, Misty D Smith, Gisela P Concepcion, Margo G Haygood, Baldomero M Olivera, Alan Light, Eric W Schmidt
Serotonin (5-HT) receptors are important in health and disease, but the existence of 14 subtypes necessitates selective ligands. Previously, the pulicatins were identified as ligands that specifically bound to the subtype 5-HT2B in the 500 nM to 10 μM range and that exhibited in vitro effects on cultured mouse neurons. Here, we examined the structure-activity relationship of 30 synthetic and natural pulicatin derivatives using binding, receptor functionality, and in vivo assays. The results reveal the 2-arylthiazoline scaffold as a tunable serotonin receptor-targeting pharmacophore...
July 26, 2017: Journal of Natural Products
https://www.readbyqxmd.com/read/28729057/neuropathic-pain-alleviating-effects-of-pyrazole-conjugated-arylsulfonamides-as-5-ht6-receptor-antagonists
#2
Jin Ri Hong, Hyunah Choo, Ghilsoo Nam
A novel series of arylsulfonylaminomethyl-3-(1-phenyl-5-isopropyl)pyrazoles was evaluated for serotonin receptor subtype 6 (5-HT6R) antagonistic effects in vitro. We also investigated their neuropathic pain-alleviating effects in vivo using a rat spinal nerve ligation (SNL) model. Bicyclic aromatic sulfonamino groups, such as naphthalene and quinolin-substituted derivatives, showed good 5-HT6 inhibitory activity in vitro. Among them, selected compounds, 12 and 13, having 8-quinoylsulfonamino groups, showed potent neuropathic pain-alleviating effects in the rat model...
July 11, 2017: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28726540/mechanisms-of-the-analgesic-effect-of-calcitonin-on-chronic-pain-by-alteration-of-receptor-or-channel-expression
#3
Akitoshi Ito, Megumu Yoshimura
The polypeptide hormone calcitonin is well known clinically for its ability to relieve osteoporotic back pain and neuropathic pain such as spinal canal stenosis, diabetic neuropathy, chemotherapy-induced neuropathy, and complex regional pain syndrome. Because the analgesic effects of calcitonin have a broad range, the underlying mechanisms of pain relief by calcitonin are largely unknown. However, recent studies using several types of chronic pain models combined with various methods have been gradually clarifying the mechanism...
January 2017: Molecular Pain
https://www.readbyqxmd.com/read/28720013/the-5-ht1b-serotonin-receptor-regulates-methylphenidate-induced-gene-expression-in-the-striatum-differential-effects-on-immediate-early-genes
#4
David Alter, Joel A Beverley, Ronak Patel, Carlos A Bolaños-Guzmán, Heinz Steiner
Drug combinations that include a psychostimulant such as methylphenidate (Ritalin) and a selective serotonin reuptake inhibitor such as fluoxetine are indicated in several medical conditions. Co-exposure to these drugs also occurs with "cognitive enhancer" use by individuals treated with selective serotonin reuptake inhibitors. Methylphenidate, a dopamine reuptake inhibitor, by itself produces some addiction-related gene regulation in the striatum. We have demonstrated that co-administration of selective serotonin reuptake inhibitors potentiates these methylphenidate-induced molecular effects, thus producing a more "cocaine-like" profile...
July 1, 2017: Journal of Psychopharmacology
https://www.readbyqxmd.com/read/28711602/contribution-of-5-ht2a-receptors-on-diaphragmatic-recovery-after-chronic-cervical-spinal-cord-injury
#5
Kun-Ze Lee, Elisa J Gonzalez-Rothi
Unilateral C2 spinal cord hemisection (C2Hx) interrupts bulbospinal respiratory pathways innervating ipsilateral phrenic motoneurons, resulting in cessation of ipsilateral diaphragm motor output. Plasticity within the spinal neural circuitry controlling the diaphragm can induce partial recovery of phrenic bursting which correlates with the time-dependent return of spinal serotonin (5-HT) immunoreactivity in the vicinity of phrenic motoneurons. The 5-HT2A receptor subtype is present on phrenic motoneurons and its expression is up-regulated after cervical spinal cord injury; however the functional role of these receptors following injury has not been clearly defined...
July 12, 2017: Respiratory Physiology & Neurobiology
https://www.readbyqxmd.com/read/28677096/hallucinogens-and-serotonin-5-ht2a-receptor-mediated-signaling-pathways
#6
Juan F López-Giménez, Javier González-Maeso
The neuropsychological effects of naturally occurring psychoactive chemicals have been recognized for millennia. Hallucinogens, which include naturally occurring chemicals such as mescaline and psilocybin, as well as synthetic compounds, such as lysergic acid diethylamide (LSD), induce profound alterations of human consciousness, emotion, and cognition. The discovery of the hallucinogenic effects of LSD and the observations that LSD and the endogenous ligand serotonin share chemical and pharmacological profiles led to the suggestion that biogenic amines like serotonin were involved in the psychosis of mental disorders such as schizophrenia...
July 5, 2017: Current Topics in Behavioral Neurosciences
https://www.readbyqxmd.com/read/28676029/cardiovascular-concern-of-5-ht2b-receptor-and-recent-vistas-in-the-development-of-its-antagonists
#7
Komal Padhariya, Richie R Bhandare, Daniel Canney, Vinay Velingkar
The serotonin 2B receptor subtype (5-HT2BR), located in central nervous system (CNS), cardiovascular system (CVS) and the gastrointestinal tract (GIT), is an important target for the treatment of migraine, obesity and irritable bowel syndrome. 5-HT2BR is necessary for the myocardial cell proliferation and differentiation at the embroyonic stage for healthy development of heart. Recently, its involvement in drug induced valvulopathy and other myocardial disorders have paved a way for selective antagonist for the treatment of cardiac disorders...
July 3, 2017: Cardiovascular & Hematological Disorders Drug Targets
https://www.readbyqxmd.com/read/28647411/hippocampal-5-ht1a-receptor-expression-changes-in-prodromal-stages-of-alzheimer-s-disease-beneficial-or-deleterious
#8
REVIEW
Mathieu Verdurand, Luc Zimmer
There is increasing evidence that the serotonergic system is highly dysfunctional in Alzheimer's disease (AD), and this could be related to cognitive impairments associated with dementia. Of the various serotonin receptors, 5-HT1A receptors are relevant to AD as they are highly expressed in the human hippocampus and are known to be involved in the regulation of memory processes. This review will discuss the involvement of 5-HT1A receptors in AD at several levels (post-mortem, in-vivo imaging, animal models)...
June 21, 2017: Neuropharmacology
https://www.readbyqxmd.com/read/28637246/effect-of-psilocybin-on-empathy-and-moral-decision-making
#9
Thomas Pokorny, Katrin H Preller, Michael Kometer, Isabel Dziobek, Franz X Vollenweider
Background: Impaired empathic abilities lead to severe negative social consequences and influence the development and treatment of several psychiatric disorders. Furthermore, empathy has been shown to play a crucial role in moral and prosocial behaviour. Although the serotonin (5-HT) system has been implicated in modulating empathy and moral behaviour, the relative contribution of the various 5-HT receptor subtypes is still unknown. Methods: We investigated the acute effect of psilocybin (0...
June 16, 2017: International Journal of Neuropsychopharmacology
https://www.readbyqxmd.com/read/28606760/progress-in-the-discovery-of-small-molecule-modulators-of-the-cys-loop-superfamily-receptors
#10
REVIEW
Brian A Sparling, Erin F DiMauro
The vertebrate Cys-loop family of ligand-gated ion channels (LGICs) are comprised of nicotinic acetylcholine (nAChR), serotonin type 3 (5-HT3R), γ-aminobutyric acid (GABAAR), and glycine (GlyR) receptors. Here, we review efforts to discover selective small molecules targeting one or more Cys-loop receptors, with a focus on state-of-the-art modulators that have been reported over the past five years. Several highlighted compounds offer robust oral bioavailability and central exposure and have thus been useful in delineating pharmacokinetic/pharmacodynamic relationships in pre-clinical disease models...
August 1, 2017: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28606116/characterization-of-serotonin-induced-inhibition-of-excitatory-synaptic-transmission-in-the-anterior-cingulate-cortex
#11
Zhen Tian, Manabu Yamanaka, Matteo Bernabucci, Ming-Gao Zhao, Min Zhuo
Excitatory synaptic transmission in central synapses is modulated by serotonin (5-HT). The anterior cingulate cortex (ACC) is an important cortical region for pain perception and emotion. ACC neurons receive innervation of projecting serotonergic nerve terminals from raphe nuclei, but the possible effect of 5-HT on excitatory transmission in the ACC has not been investigated. In the present study, we investigated the role of 5-HT on glutamate neurotransmission in the ACC slices of adult mice. Bath application of 5-HT produced dose-dependent inhibition of evoked excitatory postsynaptic currents (eEPSCs)...
June 12, 2017: Molecular Brain
https://www.readbyqxmd.com/read/28597539/developmental-effects-of-antipsychotic-drugs-on-serotonin-receptor-subtypes
#12
Yong Kee Choi, Matthew P Gardner, Frank I Tarazi
Antipsychotic medications are increasingly prescribed to pediatric and adolescent patients with psychotic diseases in spite of limited knowledge on the long-term effects of dissimilar antipsychotic drugs on developing brain. In this study, we quantified the levels of two major serotonin 5-HT1A , and 5-HT2A receptors in brain regions of developing rats after 3 weeks of treatment with typical (fluphenazine) and atypical (clozapine and olanzapine) antipsychotics, and compared to similarly treated adult rats treated with olanzapine, risperidone and quetiapine examined in previous studies...
June 8, 2017: Synapse
https://www.readbyqxmd.com/read/28587819/prodepressant-and-anxiogenic-like-effects-of-serotonin-selective-but-not-noradrenaline-selective-antidepressant-agents-in-mice-lacking-%C3%AE-2-containing-gabaa-receptors
#13
Rebecca S Benham, Nishani B Hewage, Raymond F Suckow, Elif Engin, Uwe Rudolph
Deficits in neuronal inhibition via gamma-aminobutyric acid (GABA) type A receptors (GABAA-Rs) are implicated in the pathophysiology of major depressive disorder and the therapeutic effects of current antidepressant treatments, however, the relevant GABAA-R subtype as defined by its alpha subunit is still unknown. We previously reported anxiety- and depressive-like behavior in alpha2+/- and alpha2-/- mice, respectively (Vollenweider, 2011). We sought to determine whether this phenotype could be reversed by chronic antidepressant treatment...
June 3, 2017: Behavioural Brain Research
https://www.readbyqxmd.com/read/28559799/the-effect-of-serotonin-targeting-antidepressants-on-neurogenesis-and-neuronal-maturation-of-the-hippocampus-mediated-via-5-ht1a-and-5-ht4-receptors
#14
REVIEW
Eri Segi-Nishida
Antidepressant drugs such as selective serotonin reuptake inhibitors (SSRIs) specifically increase serotonin (5-HT) levels in the synaptic cleft and are widely used to treat mood and anxiety disorders. There are 14 established subtypes of 5-HT receptors in rodents, each of which has regionally different expression patterns. Many preclinical studies have suggested that the hippocampus, which contains abundant 5-HT1A and 5-HT4 receptor subtypes in the dentate gyrus (DG), is critically involved in the mechanisms of action of antidepressants...
2017: Frontiers in Cellular Neuroscience
https://www.readbyqxmd.com/read/28555112/caveolin-1-functional-insights-into-its-role-in-muscarine-and-serotonin-induced-smooth-muscle-constriction-in-murine-airways
#15
Maryam Keshavarz, Heike Schwarz, Petra Hartmann, Silke Wiegand, Melanie Skill, Mike Althaus, Wolfgang Kummer, Gabriela Krasteva-Christ
An increased bronchoconstrictor response is a hallmark in the progression of obstructive airway diseases. Acetylcholine and 5-hydroxytryptamine (5-HT, serotonin) are the major bronchoconstrictors. There is evidence that both cholinergic and serotonergic signaling in airway smooth muscle (ASM) involve caveolae. We hypothesized that caveolin-1 (cav-1), a structural protein of caveolae, plays an important regulatory role in ASM contraction. We analyzed airway contraction in different tracheal segments and extra- and intrapulmonary bronchi in cav-1 deficient (cav-1-/-) and wild-type mice using organ bath recordings and videomorphometry of methyl-beta-cyclodextrin (MCD) treated and non-treated precision-cut lung slices (PCLS)...
2017: Frontiers in Physiology
https://www.readbyqxmd.com/read/28553207/dm5-ht2b-pharmacological-characterization-of-the-fifth-serotonin-receptor-subtype-of-drosophila-melanogaster
#16
Wolfgang Blenau, Stöppler Daniel, Sabine Balfanz, Markus Thamm, Arnd Baumann
Serotonin (5-hydroxytryptamine, 5-HT) is an important regulator of physiological and behavioral processes in both protostomes (e.g., insects) and deuterostomes (e.g., mammals). In insects, serotonin has been found to modulate the heart rate and to control secretory processes, development, circadian rhythms, aggressive behavior, as well as to contribute to learning and memory. Serotonin exerts its activity by binding to and activating specific membrane receptors. The clear majority of these receptors belong to the superfamily of G-protein-coupled receptors...
2017: Frontiers in Systems Neuroscience
https://www.readbyqxmd.com/read/28553205/dopamine-and-serotonin-induced-modulation-of-gabaergic-and-glutamatergic-transmission-in-the-striatum-and-basal-forebrain
#17
REVIEW
Toshihiko Momiyama, Takuma Nishijo
Catecholamine receptor-mediated modulation of glutamatergic or GABAergic transmission in the striatum as well as basal forebrain (BF) has been intensively studied during these two decades. In the striatum, activation of dopamine (DA) D2 receptors in GABAergic terminals inhibits GABA release onto cholinergic interneurons by selective blockade of N-type calcium channels. In the BF, glutamatergic transmission onto cholinergic projection neurons is inhibited via DA D1-like receptors by selective blockade of P/Q-type calcium channels...
2017: Frontiers in Neuroanatomy
https://www.readbyqxmd.com/read/28550249/avn-492-a-novel-highly-selective-5-ht6r-antagonist-preclinical-evaluation
#18
Alexandre V Ivachtchenko, Ilya Okun, Vladimir Aladinskiy, Yan Ivanenkov, Angela Koryakova, Ruben Karapetyan, Oleg Mitkin, Ramiz Salimov, Andrey Ivashchenko
Discovery of 5-HT6 receptor subtype and its exclusive localization within the central nervous system led to extensive investigations of its role in Alzheimer's disease, schizophrenia, and obesity. In the present study, we present preclinical evaluation of a novel highly-potent and highly-selective 5-HT6R antagonist, AVN-492. The affinity of AVN-492 to bind to 5-HT6R (Ki = 91 pM) was more than three orders of magnitude higher than that to bind to the only other target, 5-HT2BR, (Ki = 170 nM). Thus, the compound displayed great 5-HT6R selectivity against all other serotonin receptor subtypes, and is extremely specific against any other receptors such as adrenergic, GABAergic, dopaminergic, histaminergic, etc...
2017: Journal of Alzheimer's Disease: JAD
https://www.readbyqxmd.com/read/28544903/estrogen-receptor-%C3%AE-deficiency-impairs-bdnf-5-ht2a-signaling-in-the-hippocampus-of-female-brain-a-possible-mechanism-for-menopausal-depression
#19
Anindit Chhibber, Sarah K Woody, M A Karim Rumi, Michael J Soares, Liqin Zhao
Depression currently affects 350 million people worldwide and 19 million Americans each year. Women are 2.5 times more likely to experience major depression than men, with some women appearing to be at a heightened risk during the menopausal transition. Estrogen signaling has been implicated in the pathophysiology of mood disorders including depression; however, the underlying mechanisms are poorly understood. In this study, the role of estrogen receptor (ER) subtypes, ERα and ERβ, in the regulation of brain-derived neurotrophic factor (BDNF) and serotonin (5-HT) signaling was investigated; two pathways that have been hypothesized to be interrelated in the etiology of depression...
August 2017: Psychoneuroendocrinology
https://www.readbyqxmd.com/read/28483714/purposeless-oral-activity-induced-by-meta-chlorophenylpiperazine-m-cpp-undefined-tic-like-behaviors
#20
Deborah S Kreiss, Philippe De Deurwaerdère
BACKGROUND: The pathophysiological hypothesis underlying tic disorders in Tourette syndrome (TS) is that basal ganglia are not capable of properly filtering cortical information, leading patients with difficulties in inhibiting unwanted behaviors or impulses. One of the main challenges for furthering such a hypothesis is to find appropriate animal models summarizing some aspects of the disease. METHODS: It has been established for more than 25 years in rodents that the prototypical serotonin (5-HT) agonist meta-chlorophenylpiperazine (m-CPP) elicits purposeless oral movements including chewing behavior...
May 5, 2017: Journal of Neuroscience Methods
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