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https://www.readbyqxmd.com/read/29775777/antidepressant-potential-of-novel-flavonoids-derivatives-from-sweet-violet-viola-odorata-l-pharmacological-biochemical-and-computational-evidences-for-possible-involvement-of-serotonergic-mechanism
#1
Nasiara Karim, Imran Khan, Abeer Abdelhalim, Ajmal Khan, Sobia Ahsan Halim
Plant-derived natural constituents are of great interest in modern drug discovery due to their natural diversity. Viola odorata L has been traditionally used for the treatment of neuropsychiatric disorders. The present study was undertaken to isolate phytoconstituents including three flavonoids 5,7-Dihydroxy-3,6-dimethoxyflavone[1] 5,7,4'-trihydroxy-3',5'dimethoxyflavone [2] and 5,7,4'-trihydroxy-3'-methoxyflavone [3] from the whole plant of Viola odorata L and to investigate the antidepressant-like effects of these compounds and their possible mechanism of action using antagonists of the serotonergic, dopaminergic and adrenergic system...
May 15, 2018: Fitoterapia
https://www.readbyqxmd.com/read/29763291/classics-in-neuroimaging-the-serotonergic-2a-receptor-system-from-discovery-to-modern-molecular-imaging
#2
Elina T L'Estrade, Hanne D Hansen, Maria Erlandsson, Tomas G Ohlsson, Gitte M Knudsen, Matthias M Herth
Already in 1953, Woolley and Shaw speculated that serotonin could be involved in a range of central nervous system (CNS) disorders. Lysergic acid diethylamide (LSD) displayed an important role in this respect. It was used not only to antagonize biological effects of serotonin and to study the system itself, but also to identify serotonergic subtype receptors. The 5-HT2A receptor was discovered in the 1970s and identified as the responsible receptor mediating psychedelic effects of LSD. The development of positron emission tomography (PET) allowed to study this receptor system in vivo...
May 15, 2018: ACS Chemical Neuroscience
https://www.readbyqxmd.com/read/29762664/behavioral-and-serotonergic-changes-in-the-frontal-cortex-following-methamphetamine-self-administration
#3
Lisa M McFadden, Rebecca Cordie, Tamee Livermont, Andrew Johansen
Background: Methamphetamine (METH) use is associated with a variety of negative health outcomes including psychosis. The frontal cortex serotonin (5-HT)-2 receptors are thought to contribute to psychosis-like behaviors. This study investigated changes in serotonergic markers in the frontal cortex following METH self-administration and hallucinogenic drug-induced behavior. Methods: Consistent with previously published studies, freely-cycling male and female rats were allowed to self-administer METH (Males: 0...
May 14, 2018: International Journal of Neuropsychopharmacology
https://www.readbyqxmd.com/read/29758999/movement-disorders-associated-with-antipsychotic-medication-in-people-with-schizophrenia-an-overview-of-cochrane-reviews-and-meta-analysis
#4
Davide Martino, Vikram Karnik, Sydney Osland, Thomas R E Barnes, Tamara M Pringsheim
Movement disorders associated with antipsychotic medications are relatively common, stigmatising, and potentially disabling. Their prevalence in people with psychosis who are prescribed second-generation antipsychotics (SGAs) is uncertain, as is their level of recognition by clinicinas. We conducted meta-analyses of randomised controlled trials included in the Cochrane Database of Systematic Reviews on schizophrenia and schizophrenia-like psychoses to estimate the prevalence of new-onset dystonia, akathisia, parkinsonism, and tremor with SGAs (amisulpride, asenapine, aripiprazole, clozapine, olanzapine, paliperidone, quetiapine, risperidone, L-sulpiride, and ziprasidone) approved in Canada and the UK, comparing them with haloperidol and chlorpromazine...
January 1, 2018: Canadian Journal of Psychiatry. Revue Canadienne de Psychiatrie
https://www.readbyqxmd.com/read/29753748/the-abuse-potential-of-medical-psilocybin-according-to-the-8-factors-of-the-controlled-substances-act
#5
REVIEW
Matthew W Johnson, Roland R Griffiths, Peter S Hendricks, Jack E Henningfield
This review assesses the abuse potential of medically-administered psilocybin, following the structure of the 8 factors of the US Controlled Substances Act (CSA). Research suggests the potential safety and efficacy of psilocybin in treating cancer-related psychiatric distress and substance use disorders, setting the occasion for this review. A more extensive assessment of abuse potential according to an 8 factor analysis would eventually be required to guide appropriate schedule placement. Psilocybin, like other 5-HT2A agonist classic psychedelics, has limited reinforcing effects, supporting marginal, transient non-human self-administration...
May 10, 2018: Neuropharmacology
https://www.readbyqxmd.com/read/29748632/chronic-cannabis-promotes-pro-hallucinogenic-signaling-of-5-ht2a-receptors-through-akt-mtor-pathway
#6
Inés Ibarra-Lecue, Irene Mollinedo-Gajate, J Javier Meana, Luis F Callado, Rebeca Diez-Alarcia, Leyre Urigüen
Long-term use of potent cannabis during adolescence increases the risk of developing schizophrenia later in life, but to date, the mechanisms involved remain unknown. Several findings suggest that the functional selectivity of serotonin 2A receptor (5-HT2AR) through inhibitory G-proteins is involved in the molecular mechanisms responsible for psychotic symptoms. Moreover, this receptor is dysregulated in the frontal cortex of schizophrenia patients. In this context, studies involving cannabis exposure and 5-HT2AR are scarce...
April 27, 2018: Neuropsychopharmacology: Official Publication of the American College of Neuropsychopharmacology
https://www.readbyqxmd.com/read/29734370/correction-anatomical-relationships-between-serotonin-5-ht2a-and-dopamine-d2-receptors-in-living-human-brain
#7
Tatsuya Ishii, Yasuyuki Kimura, Masanori Ichise, Keisuke Takahata, Soichiro Kitamura, Sho Moriguchi, Manabu Kubota, Ming-Rong Zhang, Makiko Yamada, Makoto Higuchi, Yoshiro Okubo, Tetsuya Suhara
[This corrects the article DOI: 10.1371/journal.pone.0189318.].
2018: PloS One
https://www.readbyqxmd.com/read/29730027/synthesis-and-activity-of-di-or-trisubstituted-n-phenoxyalkyl-or-n-2-2-phenoxy-ethoxy-ethyl-piperazine-derivatives-on-the-central-nervous-system
#8
Katarzyna Pańczyk, Karolina Pytka, Magdalena Jakubczyk, Anna Rapacz, Kinga Sałat, Anna Furgała, Agata Siwek, Monika Głuch-Lutwin, Anna Gryboś, Karolina Słoczyńska, Elżbieta Pękala, Paweł Żmudzki, Adam Bucki, Marcin Kołaczkowski, Dorota Żelaszczyk, Henryk Marona, Anna M Waszkielewicz
Aim of the study was evaluation of anxiolytic, antidepressant, anticonvulsant and analgesic activity in a series of a consistent group of compounds. A series of eleven new N-(phenoxyalkyl)- or N-{2-[2-(phenoxy)ethoxy]ethyl}piperazine derivatives has been obtained. Their affinity towards 5-HT1A , 5-HT2A , 5-HT6 , 5-HT7 , D2 and α1 receptors has been assessed, and then functional assays were performed. The compounds were evaluated in mice, i.p. for their antidepressant-like (forced swim test), locomotor, anxiolytic-like (four-plate test) activities as well as - at higher doses - for anticonvulsant potential (MES) and neurotoxicity (rotarod)...
April 25, 2018: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/29723640/dual-radiotracer-translational-spect-neuroimaging-comparison-of-three-methods-for-the-simultaneous-brain-imaging-of-d-2-3-and-5-ht-2a-receptors
#9
Stergios Tsartsalis, Benjamin B Tournier, Selim Habiby, Meriem Ben Hamadi, Cristina Barca, Nathalie Ginovart, Philippe Millet
PURPOSE: SPECT imaging with two radiotracers at the same time is feasible if two different radioisotopes are employed, given their distinct energy emission spectra. In the case of 123 I and 125 I, dual SPECT imaging is not straightforward: 123 I emits photons at a principal energy emission spectrum of 143.1-179.9 keV. However, it also emits at a secondary energy spectrum (15-45 keV) that overlaps with the one of 125 I and the resulting cross-talk of emissions impedes the accurate quantification of 125 I...
April 30, 2018: NeuroImage
https://www.readbyqxmd.com/read/29722587/the-preclinical-discovery-and-development-of-cariprazine-for-the-treatment-of-schizophrenia
#10
Anna Wesołowska, Anna Partyka, Magdalena Jastrzębska-Więsek, Marcin Kołaczkowski
Cariprazine is approved in the United States and Europe for the treatment of manic or mixed episodes associated with bipolar I disorder and for the treatment of schizophrenia in adult patients. It is typically administered orally once a day (a dose range 1.5 - 6 mg/day), does require titration, and may be given with or without food. It has a half-life of 2 - 4 days with an active metabolite that has a terminal half-life of 2 - 3 weeks. Areas covered: This review article focuses on the preclinical discovery of cariprazine providing details regarding its pharmacological, behavioral, and neurochemical mechanisms and its contribution to clinical therapeutic benefits...
May 3, 2018: Expert Opinion on Drug Discovery
https://www.readbyqxmd.com/read/29720711/in-vitro-and-in-vivo-characterization-of-pcc0104005-a-novel-modulator-of-serotonin-dopamine-activity-as-an-atypical-antipsychotic-drug
#11
Yanan Xu, Xiaoyin Zhu, Hongbo Wang, Shanyue Sun, Xin Yue, Jingwei Tian
PCC0104005 is a novel drug candidate for treating schizophrenia that displays high affinity for serotonin, dopamine, and noradrenaline receptors, including partial agonism at dopamine D2 , D3 , D4 , serotonin 5-HT1A , and 5-HT2A receptors and antagonism at 5-HT2B , 5-HT6 , and 5-HT7 receptors. PCC0104005 blocks MK-801-induced hyperactivity in rats, consistent with the reduction in dopamine D2 receptor stimulation and increased dopamine release in the medial prefrontal cortex. PCC0104005 inhibits 5-HTP-induced head twitches in rats, due to its moderate affinity for human 5-HT2A receptors (Ki = 5...
May 2, 2018: Scientific Reports
https://www.readbyqxmd.com/read/29717980/5-ht2a-receptor-in-mpfc-influences-context-guided-reconsolidation-of-object-memory-in-perirhinal-cortex
#12
Juan Facundo Morici, Magdalena Miranda, Francisco Tomás Gallo, Belén Zanoni, Pedro Bekinschtein, Noelia V Weisstaub
Context-dependent memories may guide adaptive behavior relaying in previous experience while updating stored information through reconsolidation. Retrieval can be triggered by partial and shared cues. When the cue is presented, the most relevant memory should be updated. In a contextual version of the object recognition task, we examined the effect of medial PFC (mPFC) serotonin 2a receptor (5-HT2aR) blockade during retrieval in reconsolidation of competing objects memories. We found that mPFC 5-HT2aR controls retrieval and reconsolidation of object memories in the perirhinal cortex (PRH), but not in the dorsal hippocampus in rats...
May 2, 2018: ELife
https://www.readbyqxmd.com/read/29703645/psilocybin-modulates-functional-connectivity-of-the-amygdala-during-emotional-face-discrimination
#13
O Grimm, R Kraehenmann, K H Preller, E Seifritz, F X Vollenweider
Recent studies suggest that the antidepressant effects of the psychedelic 5-HT2A receptor agonist psilocybin are mediated through its modulatory properties on prefrontal and limbic brain regions including the amygdala. To further investigate the effects of psilocybin on emotion processing networks, we studied for the first-time psilocybin's acute effects on amygdala seed-to-voxel connectivity in an event-related face discrimination task in 18 healthy volunteers who received psilocybin and placebo in a double-blind balanced cross-over design...
April 24, 2018: European Neuropsychopharmacology: the Journal of the European College of Neuropsychopharmacology
https://www.readbyqxmd.com/read/29700292/enhancement-of-5-ht-2a-receptor-function-and-blockade-of-kv1-5-by-mk801-and-ketamine-implications-for-pcp-derivative-induced-disease-models
#14
Haiyue Lin, Jae Gon Kim, Sang Woong Park, Hyun Ju Noh, Jeong Min Kim, Chang Yong Yoon, Nam-Sik Woo, Bokyung Kim, Sung Il Cho, Bok Hee Choi, Dong Jun Sung, Young Min Bae
MK801 and ketamine, which are phencyclidine (PCP) derivative N-methyl-d-aspartate receptor (NMDAr) blockers, reportedly enhance the function of 5-hydroxytryptamine (HT)-2A receptors (5-HT2A Rs). Both are believed to directly affect the pathogenesis of schizophrenia, as well as hypertension. 5-HT2A R signaling involves the inhibition of Kv conductance. This study investigated the interaction of these drugs with Kv1.5, which plays important roles in 5-HT2A R signaling and in regulating the excitability of the cardiovascular and nervous system, and the potential role of this interaction in the enhancement of the 5-HT2A R-mediated response...
April 27, 2018: Experimental & Molecular Medicine
https://www.readbyqxmd.com/read/29695693/-functional-responses-to-the-chronic-activation-of-5-ht1a-receptors-in-mice-with-genetic-predisposition-to-catalepsy
#15
A S Tsybko, T V Ilchibaeva, D V Bazovkina, V S Naumenko
The effects of chronic 5-HT1A receptor activation on the behavior, functional activity of 5-HT1A receptors, and expression of key genes of the brain 5-HT system were studied in mice of the catalepsy-prone CBA strain and the catalepsy-resistant C57BL/6 strain. Chronic treatment with 8-Hydroxy-2-(di-n-propyl-amino)tetralin (8-OH-DPAT) (1.0 mg/kg i.p., 14 days) led to a significant decrease in the hypothermic response to acute administration of 8-OH-DPAT in CBA and C57BL/6 mice, which indicates the desensiti-zation of 5-HT1A receptors in both strains...
March 2018: Molekuliarnaia Biologiia
https://www.readbyqxmd.com/read/29679900/structural-insights-into-serotonin-receptor-ligands-polypharmacology
#16
Sabina Podlewska, Rafał Kafel, Enza Lacivita, Grzegorz Satała, Albert J Kooistra, Márton Vass, Chris de Graaf, Marcello Leopoldo, Andrzej J Bojarski, Stefan Mordalski
Identifying desired interactions with a target receptor is often the first step when designing new active compounds. However, attention should also be focused on contacts with other proteins that result in either selective or polypharmacological compounds. Here, the search for the structural determinants of selectivity between selected serotonin receptor subtypes was carried out. Special attention was focused on 5-HT7 R and the cross-interactions between its ligands and the 5-HT1A R, 5-HT1B R, 5-HT2A R, 5-HT2B R, and 5-HT6 R subtypes...
April 6, 2018: European Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/29677538/improvement-effects-of-a-mixed-extract-of-flowers-of-pueraria-thomsonii-benth-and-peels-of-citrus-unshiu-markovich-on-postmenopausal-symptoms-of-ovariectomized-mice
#17
Na-Ra Han, Sun-Young Nam, Sungwei Hong, Hee-Yun Kim, Phil-Dong Moon, Hyeong-Jin Kim, Hosong Cho, Boyoung Lee, Hyung-Min Kim, Hyun-Ja Jeong
BACKGROUND: Menopausal hot flushes occur frequently in postmenopausal women. In the present study, we investigated a regulatory effect of a mixed extract of flowers of Pueraria thomsonii Benth. and peels of Citrus unshiu Markovich (PCE17), an extract of flowers of Pueraria thomsonii Benth. (PE), an extract of peels of Citrus unshiu Markovich (CE), a mixture of tectorigenin 7-O-xylosylglucoside, tectoridin, and tectorigenin (Tec, the active compounds of PE), and hesperidin (Hes, an active compound of CE) on menopausal hot flushes...
April 17, 2018: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/29660654/assessment-of-the-possible-roles-of-sb-269970-versus-ketanserin-on-carbon-tetrachloride-induced-liver-fibrosis-in-rats-oxidative-stress-tgf-%C3%AE-1-induced-hscs-activation-pathway
#18
Marwa Ahmed Amin Atallah, Samah M Elaidy, Mona K Tawfik
BACKGROUND: In liver fibrosis, a major morbid and mortal disease, oxidative stress motivation of hepatic stellate cells (HSCs)-into myofibroblasts terminated in collagen deposition remain the key pathophysiological deal. Serotonin (5-HT) through its HSCs-expressed receptors, especially 5-HT2A and 7, shows crucial events in fibrogenesis of chronic liver diseases. Molecular hepatic oxidative stress-fibrotic roles of 5-HT2A and 7 receptors antagonists (ketanserin and SB-269970 respectively) are still a challenging issue...
November 28, 2017: Pharmacological Reports: PR
https://www.readbyqxmd.com/read/29658099/identification-of-serotoninergic-system-components-in-stallion-sperm
#19
F Jiménez-Trejo, I Coronado-Mares, M Boeta, I González-Santoyo, R Vigueras-Villaseñor, C Arriaga-Canon, L Herrera-Montalvo, M Tapia-Rodríguez
Assisted reproductive techniques have been used on several domestic animals to preserve desirable traits in strains of high genetic and commercial value; however in equines its efficiency rate is relatively low. To increase the conception ratio in stallions, some research groups have used pharmacological treatments which promote sperm hyperactivation in order to increase male's fertility rates. In this way, our previous work suggests that serotonin (5-HT) could be a good pharmacological candidate that facilitates conception rate in domestic horses...
April 16, 2018: Histology and Histopathology
https://www.readbyqxmd.com/read/29649585/effects-of-different-serotonin-receptor-subtype-antagonists-on-the-development-of-cardiac-allograft-vasculopathy-in-murine-aortic-allografts
#20
Annika Gocht, Jörg H W Distler, Bernd Spriewald, Martina Ramsperger-Gleixner, Michael Weyand, Stephan M Ensminger, Christian Heim
BACKGROUND: Cardiac allograft vasculopathy (CAV) is the main obstacle for long-term survival after heart transplantation. Alloimmune mediated chronic vascular rejection results in several mechanisms like platelet activation, immigration of inflammatory cells through the endothelial layer and proliferation and migration of smooth muscle cells (SMCs). Serotonin (5-HT) promotes these processes via activation of 5-HT2 receptors. We hypothesized that inhibiting 5-HT2 receptors ameliorates the development of CAV...
April 9, 2018: Transplant Immunology
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