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https://www.readbyqxmd.com/read/30467466/the-varieties-of-the-psychedelic-experience-a-preliminary-study-of-the-association-between-the-reported-subjective-effects-and-the-binding-affinity-profiles-of-substituted-phenethylamines-and-tryptamines
#1
Federico Zamberlan, Camila Sanz, Rocío Martínez Vivot, Carla Pallavicini, Fire Erowid, Earth Erowid, Enzo Tagliazucchi
Classic psychedelics are substances of paramount cultural and neuroscientific importance. A distinctive feature of psychedelic drugs is the wide range of potential subjective effects they can elicit, known to be deeply influenced by the internal state of the user ("set") and the surroundings ("setting"). The observation of cross-tolerance and a series of empirical studies in humans and animal models support agonism at the serotonin (5-HT)2A receptor as a common mechanism for the action of psychedelics...
2018: Frontiers in Integrative Neuroscience
https://www.readbyqxmd.com/read/30451579/5-ht-2a-receptors-and-parkinson-s-disease-psychosis-a-pharmacological-discussion
#2
Philippe Huot
No abstract text is available yet for this article.
December 2018: Neurodegenerative Disease Management
https://www.readbyqxmd.com/read/30443669/5-ht-2a-blockade-for-dyskinesia-and-psychosis-in-parkinson-s-disease-is-there-a-limit-to-the-efficacy-of-this-approach-a-study-in-the-mptp-lesioned-marmoset-and-a-literature-mini-review
#3
Cynthia Kwan, Imane Frouni, Dominique Bédard, Stephen G Nuara, Jim C Gourdon, Adjia Hamadjida, Philippe Huot
Virtually every patient affected by Parkinson's disease (PD) eventually requires treatment with L-3,4-dihydroxyphenylalanine (L-DOPA), which leads to complications such as dyskinesia and psychosis. Whereas blockade of serotonin 2A (5-HT2A ) receptors appears to be an effective way to reduce both dyskinesia and psychosis, whether it has the potential to eliminate the two phenomena remains to be determined. In a previous study, we showed that highly selective 5-HT2A receptor blockade with EMD-281,014, at plasma levels comparable to those achieved in the clinic, reduced dyskinesia and psychosis-like behaviours (PLBs), in the 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP)-lesioned marmoset...
November 15, 2018: Experimental Brain Research. Experimentelle Hirnforschung. Expérimentation Cérébrale
https://www.readbyqxmd.com/read/30400993/5-htr-2a-and-5-htr-3a-but-not-5-htr-1a-antagonism-impairs-the-cross-modal-reactivation-of-deprived-visual-cortex-in-adulthood
#4
Nathalie Lombaert, Maroussia Hennes, Sara Gilissen, Giel Schevenels, Laetitia Aerts, Ria Vanlaer, Lieve Geenen, Ann Van Eeckhaut, Ilse Smolders, Julie Nys, Lutgarde Arckens
Visual cortical areas show enhanced tactile responses in blind individuals, resulting in improved behavioral performance. Induction of unilateral vision loss in adult mice, by monocular enucleation (ME), is a validated model for such cross-modal brain plasticity. A delayed whisker-driven take-over of the medial monocular zone of the visual cortex is preceded by so-called unimodal plasticity, involving the potentiation of the spared-eye inputs in the binocular cortical territory. Full reactivation of the sensory-deprived contralateral visual cortex is accomplished by 7 weeks post-injury...
November 6, 2018: Molecular Brain
https://www.readbyqxmd.com/read/30373886/the-5-ht-2a-receptor-5-ht-2a-r-regulates-impulsive-action-and-cocaine-cue-reactivity-in-male-sprague-dawley-rats
#5
Dennis J Sholler, Sonja J Stutz, Robert G Fox, Edward L Boone, Qin Wang, Kenner C Rice, F Gerard Moeller, Noelle C Anastasio, Kathryn A Cunningham
Impulsivity and the responsivity to cocaine-linked cues ("cue reactivity") promote relapse in cocaine use disorder (CUD). A time-dependent escalation of cue reactivity ("incubation") occurs during extended forced abstinence (FA) from cocaine self-administration. The investigational serotonin (5-HT) 5-HT2A receptor (5-HT2A R) antagonist/inverse agonist M100907 suppresses impulsive action (inability to withhold premature responses) and cocaine-seeking behavior. The recent approval of the 5-HT2A R antagonist/inverse agonist pimavanserin (NUPLAZID™) provides the opportunity to assess an FDA-approved medication in preclinical analyses of relapse vulnerability...
October 29, 2018: Journal of Pharmacology and Experimental Therapeutics
https://www.readbyqxmd.com/read/30367948/inhibitor-of-striatal-enriched-protein-tyrosine-phosphatase-8-trifluoromethyl-1-2-3-4-5-benzopentathiepin-6-amine-hydrochloride-tc-2153-produces-antidepressant-like-effect-and-decreases-functional-activity-and-protein-level-of-5-ht-2a-receptor-in-the-brain
#6
E A Kulikova, N V Khotskin, N B Illarionova, I E Sorokin, E Y Bazhenova, E M Kondaurova, K P Volcho, T M Khomenko, N F Salakhutdinov, E Ponimaskin, V S Naumenko, A V Kulikov
The serotoninergic 5-HT2A receptor is involved in the mechanism of depression and antidepressant drugs action. Earlier we showed that striatal-enriched protein tyrosine phosphatase (STEP) inhibitor - 8-(trifluoromethyl)-1,2,3,4,5-benzopentathiepin-6-amine hydrochloride (TC-2153) affects both the brain serotoninergic system and the brain-derived neurotropic factor that are known to be involved in the psychopathology of depression. In the present study we investigated the effects of chronic TC-2153 administration on behavior in the standard battery of tests as well as the effects of acute and chronic TC-2153 treatment on the brain 5-HT2A receptors in mice...
December 1, 2018: Neuroscience
https://www.readbyqxmd.com/read/30360947/involvement-of-5-ht-2a-receptor-hyperfunction-in-the-anxiety-like-behavior-induced-by-doxorubicin-and-cyclophosphamide-combination-treatment-in-rats
#7
Yuka Nakamura, Yoshihisa Kitamura, Yusuke Sumiyoshi, Nanami Naito, Shiho Kan, Soichiro Ushio, Ikuko Miyazaki, Masato Asanuma, Toshiaki Sendo
We examined whether combination treatment with doxorubicin and cyclophosphamide, a traditional chemotherapy for breast cancer, induced anxiety-like behavior in rats. Furthermore, we evaluated the role of the serotonin (5-HT)2A receptor subtype in the anxiety-like behavior induced by such chemotherapy. Rats were intraperitoneally injected with doxorubicin and cyclophosphamide once a week for 2 weeks. This caused the rats to display anxiety-like behavior during the light-dark test. In addition, we examined the rats' 5-HT2A receptor-mediated behavioral responses...
October 9, 2018: Journal of Pharmacological Sciences
https://www.readbyqxmd.com/read/30355630/5-ht-2a-receptor-induced-morphological-reorganization-of-pkc%C3%AE-expressing-interneurons-gates-inflammatory-mechanical-allodynia-in-rat
#8
Cristina Alba-Delgado, Sarah Mountadem, Noémie Mermet-Joret, Lénaïc Monconduit, Radhouane Dallel, Alain Artola, Myriam Antri
Mechanical allodynia, a widespread pain symptom which still lacks effective therapy, is associated with the activation of a dorsally-directed polysynaptic circuit within spinal (SDH) or medullary dorsal horn (MDH), whereby tactile inputs into deep SDH/MDH can gain access to superficial SDH/MDH, eliciting pain. Inner lamina II (IIi ) interneurons expressing the γ isoform of protein kinase C (PKCγ+ ) are key elements for allodynia circuits but how they operate is still unclear. Combining behavioral, ex vivo electrophysiological and morphological approaches in an adult rat model of facial inflammatory pain (Complete Freund's Adjuvant, CFA), we show that the mechanical allodynia observed 1h after CFA injection is associated with i) sensitization (using ERK1/2 phosphorylation as a marker) and ii) reduced dendritic arborizations and enhanced spine density-in exclusively PKCγ+ interneurons, but iii) depolarized resting membrane potential (RMP) in all lamina IIi PKCγ+ /PKCγ- interneurons...
October 24, 2018: Journal of Neuroscience: the Official Journal of the Society for Neuroscience
https://www.readbyqxmd.com/read/30336190/expression-of-pituitary-adenylate-cyclase-activating-peptide-calcitonin-gene-related-peptide-and-headache-targets-in-the-trigeminal-ganglia-of-rats-and-humans
#9
Simona Denise Frederiksen, Karin Warfvinge, Lena Ohlsson, Lars Edvinsson
Neurotransmitter and headache target localization in the trigeminal ganglia (TG) might increase the understanding of sites of action, and mechanisms related to headache therapy. The overall aim of the study was to investigate the presence of migraine targets in the TG with particular emphasis on pituitary adenylate cyclase-activating peptide (PACAP) and calcitonin gene-related peptide (CGRP), known to be involved in cranial pain processing, and selected headache targets. Rat- and human TG were processed for immunohistochemistry...
October 15, 2018: Neuroscience
https://www.readbyqxmd.com/read/30322874/involvement-of-5-ht-1a-and-5-ht-2a-receptors-but-not-%C3%AE-2-adrenoceptors-in-the-acute-electrophysiological-effects-of-cariprazine-in-the-rat-brain-in-vivo
#10
Anna Herman, Mostafa El Mansari, Nika Adham, Béla Kiss, Bence Farkas, Pierre Blier
Cariprazine, an orally active and potent dopamine D3 -preferring D3 /D2 receptor partial agonist, is approved to treat adults with schizophrenia (in the United States and Europe) and manic or mixed episodes associated with bipolar I disorder (in the United States). Cariprazine also displays partial agonism at serotonin [5-hydroxytryptamine (5-HT)] 5-HT1A receptors and antagonism at 5-HT2A and 5-HT2B receptors in vitro. The study objective was to determine whether cariprazine leads to functional alterations of monoamine systems in vivo via electrophysiological recordings from anesthetized rats...
December 2018: Molecular Pharmacology
https://www.readbyqxmd.com/read/30304725/antiallodynic-effects-of-intrathecal-areca-nut-for-spinal-nerve-ligated-and-chemotherapy-induced-neuropathic-pain-in-rats
#11
Hyung Gon Lee, Ji A Song, Dong Soo Han, Kyeong Wan Woo, Myung Ha Yoon
This study examined the effects of intrathecal areca nut on spinal nerve-ligated and chemotherapy-induced neuropathic pain (NP), and investigated the relevance of spinal 5-hydroxytryptamine (5-HT) and α2-adrenergic receptors to those effects. For drug administration, intrathecal catheters were inserted into the subarachnoid space of male Sprague-Dawley rats. NP was induced either by spinal nerve ligation (left spinal nerves L5 and L6) or by chemotherapeutic injection (intraperitoneal cisplatin, 2 mg/kg/day, once daily for 4 days)...
2018: Pharmacology
https://www.readbyqxmd.com/read/30298296/effect-of-the-selective-5-ht-2a-receptor-antagonist-emd-281-014-on-l-dopa-induced-abnormal-involuntary-movements-in-the-6-ohda-lesioned-rat
#12
Imane Frouni, Cynthia Kwan, Dominique Bédard, Sébastien Belliveau, Élodie Bourgeois-Cayer, Fleur Gaudette, Francis Beaudry, Adjia Hamadjida, Philippe Huot
L-3,4-Dihydroxyphenylalanine (L-DOPA) is the most effective therapy for motor symptoms of Parkinson's disease (PD); however, with repeated administration, as many as 94% of PD patients develop complications such as L-DOPA-induced dyskinesia. We previously demonstrated that EMD-281,014, a highly selective serotonin 2A (5-HT2A ) receptor antagonist, reduces the severity of dyskinesia in the parkinsonian marmoset, without interfering with L-DOPA anti-parkinsonian benefit. Here, we assessed the effects of EMD-281,014 on L-DOPA-induced abnormal involuntary movements (AIMs) in the 6-hydroxydopamine (6-OHDA)-lesioned rat...
October 8, 2018: Experimental Brain Research. Experimentelle Hirnforschung. Expérimentation Cérébrale
https://www.readbyqxmd.com/read/30278246/effect-of-5-ht-2a-receptor-antagonist-ketanserin-on-micturition-in-male-rats
#13
Xiaohu Wang, Nailong Cao, Jianshu Ni, Jiemin Si, Baojun Gu, Andersson Karl-Erik
OBJECTIVES: This study aimed to investigate the effects of ketanserin on micturition mediated via the 5-HT2A receptor in the motoneuron nucleus of the Lumbosacral cord, as reflected in high frequency oscillations (HFOs) of intravesical pressure and the external urethral sphincter electromyogram (EUS-EMG) in anesthetized male rats. METHODS:: Male Sprague-Dawley rats were used. Cystometry and EUS-EMG were performed in all rats under urethane anesthesia to examine the variations after successive intrathecal (i...
September 29, 2018: Neuroscience Letters
https://www.readbyqxmd.com/read/30261175/neurochemical-pharmacology-of-psychoactive-substituted-n-benzylphenethylamines-high-potency-agonists-at-5-ht-2a-receptors
#14
Amy J Eshleman, Katherine M Wolfrum, John F Reed, Sunyoung O Kim, Robert A Johnson, Aaron Janowsky
The use of new psychoactive substituted 2,5-dimethoxy-N-benzylphenethylamines is associated with abuse and toxicity in the United States and elsewhere and their pharmacology is not well known. This study compares the mechanisms of action of 2-(2,5-dimethoxy-4-methylphenyl)-N-(2-methoxybenzyl)ethanamine (25D-NBOMe), 2-(4-ethyl-2,5-dimethoxyphenyl)-N-(2-methoxybenzyl)ethanamine (25E-NBOMe), 2-(2,5-dimethoxyphenyl)-N-(2-methoxybenzyl)ethanamine (25H-NBOMe), 2-(((4-iodo-2,5-dimethoxyphenethyl)amino)methyl)phenol (25I-NBOH); and 2-(2,5-dimethoxy-4-nitrophenyl)-N-(2-methoxybenzyl)ethanamine) (25N-NBOMe) with hallucinogens and stimulants...
September 25, 2018: Biochemical Pharmacology
https://www.readbyqxmd.com/read/30240783/modality-selective-roles-of-pro-nociceptive-spinal-5-ht-2a-and-5-ht-3-receptors-in-normal-and-neuropathic-states
#15
Ryan Patel, Anthony H Dickenson
Descending brainstem control of spinal nociceptive processing permits a dynamic and adaptive modulation of ascending sensory information. Chronic pain states are frequently associated with enhanced descending excitatory drive mediated predominantly through serotonergic neurones in the rostral ventromedial medulla. In this study, we examine the roles of spinal 5-HT2A and 5-HT3 receptors in modulating ascending sensory output in normal and neuropathic states. In vivo electrophysiology was performed in anaesthetised spinal nerve ligated (SNL) and sham-operated rats to record from wide dynamic range neurones in the ventral posterolateral thalamus...
December 2018: Neuropharmacology
https://www.readbyqxmd.com/read/30225486/influence-of-the-substituent-on-the-phosphine-ligand-in-novel-rhenium-i-aldehydes-synthesis-computational-studies-and-first-insights-into-the-antiproliferative-activity
#16
Michelle Muñoz-Osses, Daniel Siegmund, Alejandra Gómez, Fernando Godoy, Angélica Fierro, Leonel Llanos, Daniel Aravena, Nils Metzler-Nolte
Cyrhetrenyl aldehyde derivatives [(η5-C5H4CHO)Re(CO)2PR3] with R = methyl (Me, 2a), phenyl (Ph, 2b), and cyclohexyl (Cy, 2c) were synthesized by a photochemical reaction from the starting material [(η5-C5H4CHO)Re(CO)3] (1) and the corresponding phosphines. The complexes were fully characterized by FT-IR, 1H, 13C and 31P NMR spectroscopy, elemental analysis and mass spectrometry. The molecular structures of 2a-c have also been determined. Electronic structure calculations by TD-DFT and electrochemical studies are in sound agreement with the effect of the substitution of one carbonyl group by a phosphine ligand...
September 18, 2018: Dalton Transactions: An International Journal of Inorganic Chemistry
https://www.readbyqxmd.com/read/30209534/role-of-mglu2-in-the-5-ht-2a-receptor-dependent-antipsychotic-activity-of-clozapine-in-mice
#17
Kelsey S Hideshima, Ashkhan Hojati, Justin M Saunders, Doan M On, Mario de la Fuente Revenga, Jong M Shin, Ana Sánchez-González, Cassandra M Dunn, Alexander B Pais, Anthony C Pais, Michael F Miles, Jennifer T Wolstenholme, Javier González-Maeso
BACKGROUND: Serotonin 5-HT2A and metabotropic glutamate 2 (mGlu2) are neurotransmitter G protein-coupled receptors (GPCRs) involved in the signaling mechanisms underlying psychosis and schizophrenia treatment. Previous findings in mGlu2 knockout (KO) mice suggested that mGlu2 is necessary for head-twitch behavior, a rodent phenotype characteristic of hallucinogenic 5-HT2A receptor agonists. However, the role of mGlu2 in the behavioral effects induced by antipsychotic drugs remains poorly understood...
September 12, 2018: Psychopharmacology
https://www.readbyqxmd.com/read/30140550/influence-of-patient-demographics-and-graft-types-on-acl-second-injury-rates-in-ipsilateral-versus-contralateral-knees-a-systematic-review-and-meta-analysis
#18
Zakariya Nawasreh, Gabrielle Adams, Olivia Pryzbylkowski, David Logerstedt
Background: There are inconsistencies in the reported rates of second anterior cruciate ligament (ACL) injuries per limb, patients' sex and graft types after primary ACL reconstruction (ACLR). There are also inconsistencies regarding the influence of these factors on the occurrence of second ACL injury after primary ACLR. Purpose: To determine the rate of second ACL injury, to either the ipsilateral graft or contralateral healthy ACL, as influenced by sex, age, and graft types and to determine the influence of sex, age, and graft types on the occurrence of second ACL injury after primary ACLR...
August 2018: International Journal of Sports Physical Therapy
https://www.readbyqxmd.com/read/30138970/-5-ht-2a-receptor-protein-kinase-c-pathway-in-mediating-long-term-facilitation-of-carotid-sinus-nerve-discharge-in-chronic-intermittent-hypoxia-rats
#19
Y C Luo, Y Q Zhang, K Hu, Z Zhang, M Q Xiong, W H Hu, M L Dong, M Shang
Objective: To explore the role of 5-HT(2A)R/PKC pathway in mediating long-term facilitation (LTF) of carotid sinus nerve (CSN) discharge in chronic intermittent hypoxia (CIH) rats. Methods: With number table, 24 adult SD rats were randomly divided into saline control group (group A, n =6), 5-HT(2A)R antagonist (ketanserin) group (group B, n =6), PKC inhibitor (PKC θ-pseudosubstrate) group (group C, n =6) and combined ketanserin with PKC θ-pseudosubstrate group (group D, n =6). All rats were placed into the animal chambers for CIH treatment, 8 h per day (from 9: 00 to 17: 00) for 4 consecutive weeks...
August 12, 2018: Chinese Journal of Tuberculosis and Respiratory Diseases
https://www.readbyqxmd.com/read/30131678/serotonergic-regulation-of-corticoamygdalar-neurons-in-the-mouse-prelimbic-cortex
#20
Daniel Avesar, Emily K Stephens, Allan T Gulledge
Neuromodulatory transmitters, such as serotonin (5-HT), selectively regulate the excitability of subpopulations of cortical projection neurons to gate cortical output to specific target regions. For instance, in the mouse prelimbic cortex, 5-HT selectively excites commissurally projecting (COM) intratelencephalic neurons via activation of 5-HT2A (2A) receptors, while simultaneously inhibiting, via 5-HT1A (1A) receptors, corticofugally projecting pyramidal neurons targeting the pons. Here we characterize the physiology, morphology, and serotonergic regulation of corticoamygdalar (CAm) projection neurons in the mouse prelimbic cortex...
2018: Frontiers in Neural Circuits
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