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https://www.readbyqxmd.com/read/28229459/differential-serotonergic-modulation-across-the-main-and-accessory-olfactory-bulbs
#1
Zhenbo Huang, Nicolas Thiebaud, Debra Ann Fadool
Mitral cells (MCs) contained in the main (MOB) and accessory (AOB) olfactory bulb have distinct intrinsic membrane properties but a comparison of the extent of neuromodulation across the two systems is not well explored. Herein, we investigated a widely-distributed CNS modulator, serotonin (5-HT), for its ability to modulate the biophysical properties of MCs across the MOB and AOB, using an in vitro, brain slice approach in postnatal 15-30 day mice. In the MOB, 5-HT elicited three types of responses in 93% of 180 cells tested...
February 22, 2017: Journal of Physiology
https://www.readbyqxmd.com/read/28224459/effect-of-hallucinogens-on-unconditioned-behavior
#2
Adam L Halberstadt, Mark A Geyer
Because of the ethical and regulatory hurdles associated with human studies, much of what is known about the psychopharmacology of hallucinogens has been derived from animal models. However, developing reliable animal models has proven to be a challenging task due to the complexity and variability of hallucinogen effects in humans. This chapter focuses on three animal models that are frequently used to test the effects of hallucinogens on unconditioned behavior: head twitch response (HTR), prepulse inhibition of startle (PPI), and exploratory behavior...
February 22, 2017: Current Topics in Behavioral Neurosciences
https://www.readbyqxmd.com/read/28222297/hallucinogenic-drugs-a-new-study-answers-old-questions-about-lsd
#3
Adam L Halberstadt
LSD induces profound psychedelic effects, including changes in the meaning of percepts. The subjective effects of LSD are fully blocked by a 5-HT2A receptor antagonist. LSD may alter meaningfulness by increasing activity in cortical regions responsible for processing personal attribution.
February 20, 2017: Current Biology: CB
https://www.readbyqxmd.com/read/28221369/chemistry-based-molecular-signature-underlying-the-atypia-of-clozapine
#4
T Cardozo, E Shmelkov, K Felsovalyi, J Swetnam, T Butler, D Malaspina, S V Shmelkov
The central nervous system is functionally organized as a dynamic network of interacting neural circuits that underlies observable behaviors. At higher resolution, these behaviors, or phenotypes, are defined by the activity of a specific set of biomolecules within those circuits. Identification of molecules that govern psychiatric phenotypes is a major challenge. The only organic molecular entities objectively associated with psychiatric phenotypes in humans are drugs that induce psychiatric phenotypes and drugs used for treatment of specific psychiatric conditions...
February 21, 2017: Translational Psychiatry
https://www.readbyqxmd.com/read/28216047/serotonin-2a-homodimers-are-needed-for-signalling-via-both-phospholipase-a2-and-phospholipase-c-in-transfected-cho-cells
#5
Alba Iglesias, Marta Cimadevila, María Isabel Cadavid, María Isabel Loza, José Brea
Different ligands differentially activate phospholipase A2 (PLA2) and phospholipase C (PLC) signalling pathways that are coupled to the serotonin 2A (5-HT2A) receptor, a class-A G-protein coupled receptor (GPCR). The serotonin 5-HT2A receptor has been shown to be expressed as a homodimer displaying some ligands negative cooperativity between protomers in the PLA2 signalling pathway. We hypothesized that the homodimeric complex is the minimum functional unit required for activation of the PLA2 and PLC pathways by the serotonin 5-HT2A receptor...
February 17, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28212021/discovery-and-development-of-1-2-bromophenyl-sulfonyl-5-methoxy-3-4-methyl-1-piperazinyl-methyl-1h-indole-dimesylate-monohydrate-suvn-502-a-novel-potent-selective-and-orally-active-serotonin-6-5-ht6-receptor-antagonist-for-potential-treatment-of-alzheimer-s
#6
Ramakrishna Nirogi, Anil Shinde, Rama Sastry Kambhampati, Abdul Rasheed Mohammed, Sangram Keshari Saraf, Rajesh Kumar Badange, Thrinath Reddy Bandyala, Venugopalarao Bhatta, Kumar Bojja, Veena Reballi, Ramkumar Subramanian, Vijay Benade, Raghava Choudary Palacharla, Gopinadh Bhyrapuneni, Pradeep Jayarajan, Vinod Goyal, Venkat Jasti
Optimization of a novel series of 3-(piperazinylmethyl) indole derivatives as 5-hydroxytryptamine-6 receptor (5-HT6R) antagonists resulted in identification of 1-[(2-bromophenyl)sulfonyl]-5-methoxy-3-[(4-methyl-1-piperazinyl)methyl]-1H-indole dimesylate monohydrate (5al, SUVN-502) as a clinical candidate for potential treatment of cognitive disorders. It has high affinity at human 5-HT6R (Ki = 2.04 nM) and selectivity over 100 target sites which include receptors, enzymes, peptides, growth factors, ion channels, steroids, immunological factors, second messengers, and prostaglandins...
February 17, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28202410/atypical-antipsychotic-clozapine-reversed-deficit-on-prepulse-inhibition-of-the-acoustic-startle-reflex-produced-by-microinjection-of-doi-into-the-inferior-colliculus-in-rats
#7
Rodolpho Pereira de Oliveira, Karen Yuriko Nagaishi, Regina Cláudia Barbosa Silva
Dysfunctions of the serotonergic system have been suggested to be important in the neurobiology of schizophrenia. Patients with schizophrenia exhibit deficits in an operational measure of sensorimotor gating: prepulse inhibition (PPI) of startle. PPI is the normal reduction in the startle response caused by a low intensity non-startling stimulus (prepulse) which is presented shortly before the startle stimulus (pulse). The hallucinogen 2,5-dimethoxy-4-iodoamphetamine (DOI), a 5-hydroxytryptamine(HT)2 receptor agonist disrupted PPI in rats...
February 12, 2017: Behavioural Brain Research
https://www.readbyqxmd.com/read/28185964/experimental-occlusal-disharmony-a-promoting-factor-for-anxiety-in-rats-under-chronic-psychological-stress
#8
Xuan Tang, Jian Li, Ting Jiang, Shu-Hui Han, Dong-Yuan Yao
BACKGROUND AND PURPOSE: Clinically, patients under chronic psychological stress (PS) appear to be more susceptible to occlusal disharmony (OD) compared with those without PS. OD was proved to introduce anxiety-like stress. Therefore, the purpose of the study was to investigate whether OD would affect psychological stress-induced anxiety and its underlying mechanisms. METHODS: Chronic PS was induced by a communication box, and OD was produced by bonding a 0.3mm-thick crown on the right maxillary first molar of male Sprague-Dawley rats...
February 7, 2017: Progress in Neuro-psychopharmacology & Biological Psychiatry
https://www.readbyqxmd.com/read/28182676/the-swimming-test-is-effective-for-evaluating-spasticity-after-contusive-spinal-cord-injury
#9
Youngjae Ryu, Toru Ogata, Motoshi Nagao, Taku Kitamura, Kazuhito Morioka, Yoshinori Ichihara, Toru Doi, Yasuhiro Sawada, Masami Akai, Ryohei Nishimura, Naoki Fujita
Spasticity is a frequent chronic complication in individuals with spinal cord injury (SCI). However, the severity of spasticity varies in patients with SCI. Therefore, an evaluation method is needed to determine the severity of spasticity. We used a contusive SCI model that is suitable for clinical translation. In this study, we examined the feasibility of the swimming test and an EMG for evaluating spasticity in a contusive SCI rat model. Sprague-Dawley rats received an injury at the 8th thoracic vertebra...
2017: PloS One
https://www.readbyqxmd.com/read/28177082/5-ht2a-agonists-a-novel-therapy-for-functional-neurological-disorders
#10
Alexander Bryson, Olivia Carter, Trevor Norman, Richard Kanaan
No abstract text is available yet for this article.
February 8, 2017: International Journal of Neuropsychopharmacology
https://www.readbyqxmd.com/read/28176400/effect-of-a-hallucinogenic-serotonin-5-ht2a-receptor-agonist-on-visually-guided-hippocampal-dependent-spatial-cognition-in-c57bl-6j-mice
#11
Gongliang Zhang, David Cinalli, Robert W Stackman
By acting on serotonin 5-HT2A receptors (5-HT2A Rs), serotonergic psychedelic drugs induce perceptual and visual hallucinations by increasing neuronal excitability and altering visual-evoked neuronal responses. The present study was designed to examine whether the perceptual alterations induced by a serotonergic psychedelic drug would affect the integrity of hippocampal-dependent, visually guided spatial cognition. phenylalkylamine hallucinogen TCB-2 is a selective agonist of 5-HT2A Rs. Mice received TCB-2 (1...
February 8, 2017: Hippocampus
https://www.readbyqxmd.com/read/28161375/receptor-stimulated-transamidation-induces-activation-of-rac1-and-cdc42-and-the-regulation-of-dendritic-spines
#12
Zhen Mi, Tuda Si, Khushboo Kapadia, Qian Li, Nancy A Muma
Regulation of dendritic spines is an important component of synaptic function and plasticity whereas dendritic spine dysregulation is related to several psychiatric and neurological diseases. In the present study, we tested the hypothesis that serotonin (5-HT)2A/2C receptor-induced Rho family transamidation and activation regulates dendritic spine morphology and that activation of multiple types of receptors can induce transglutaminase (TGase)-catalyzed transamidation of small G proteins. We previously reported a novel 5-HT2A receptor downstream effector, TGase-catalyzed serotonylation of the small G protein Rac1 in A1A1v cells, a rat embryonic cortical cell line...
February 1, 2017: Neuropharmacology
https://www.readbyqxmd.com/read/28160177/influence-of-nonylphenol-and-octylphenol-exposure-on-5-ht-5-ht-transporter-and-5-ht2a-receptor
#13
Chunhong Liu, Yuting Lai, Junyan Ouyang, Tongwang Yang, Youting Guo, Jie Yang, Shaowen Huang
Nonylphenol (NP) and octylphenol (OP) are priority environmental contaminants that have a potential role as endocrine disruptors. They can be biomagnified in the food chain and pose an estrogenic health risk to human health. A 28-day oral toxicity study was performed to observe the impact of single and combined exposure to NP and OP on 5-HT transporter (SERT) as well as 5-HT2A receptor. Results showed that the 5-HT levels in rat plasma increased with exposure to middle-dose and high-dose NP, to high-dose OP, and to low, middle, and high doses of combined NP and OP (P < 0...
February 3, 2017: Environmental Science and Pollution Research International
https://www.readbyqxmd.com/read/28154892/differential-effects-of-antipsychotic-and-propsychotic-drugs-on-prepulse-inhibition-and-locomotor-activity-in-roman-high-rha-and-low-avoidance-rla-rats
#14
Ignasi Oliveras, Ana Sánchez-González, Daniel Sampedro-Viana, Maria Antonietta Piludu, Cristóbal Río-Alamos, Osvaldo Giorgi, Maria G Corda, Susana Aznar, Javier González-Maeso, Cristina Gerbolés, Gloria Blázquez, Toni Cañete, Adolf Tobeña, Alberto Fernández-Teruel
RATIONALE: Animal models with predictive and construct validity are necessary for developing novel and efficient therapeutics for psychiatric disorders. OBJECTIVES: We have carried out a pharmacological characterization of the Roman high- (RHA-I) and low-avoidance (RLA-I) rat strains with different acutely administered propsychotic (DOI, MK-801) and antipsychotic drugs (haloperidol, clozapine), as well as apomorphine, on prepulse inhibition (PPI) of startle and locomotor activity (activity cages)...
March 2017: Psychopharmacology
https://www.readbyqxmd.com/read/28133368/obesity-5-ht2a-in-glp1-mediated-weight-loss
#15
Alan Morris
No abstract text is available yet for this article.
January 30, 2017: Nature Reviews. Endocrinology
https://www.readbyqxmd.com/read/28127501/hippocampal-serotonin-2a-receptor-immunoreactive-neurons-density-increases-after-testosterone-therapy-in-the-gonadectomized-male-mice
#16
Emsehgol Nikmahzar, Mehrdad Jahanshahi, Amir Ghaemi, Gholam Reza Naseri, Ali Reza Moharreri, Ahmad Ali Lotfinia
The change of steroid levels may also exert different modulatory effects on the number and class of serotonin receptors present in the plasma membrane. The effects of chronic treatment of testosterone for anxiety were examined and expression of 5-HT2A serotonergic receptor, neuron, astrocyte, and dark neuron density in the hippocampus of gonadectomized male mice was determined. Thirty-six adult male NMRI mice were randomly divided into six groups: intact-no testosterone treatment (No T), gonadectomy (GDX)-No T, GDX-Vehicle, GDX-6...
December 2016: Anatomy & Cell Biology
https://www.readbyqxmd.com/read/28125323/increased-levels-of-5ht2a-receptor-mrna-expression-in-peripheral-blood-mononuclear-cells-of-patients-with-major-depression-correlations-with-severity-and-duration-of-illness
#17
Meysam Amidfar, Yong-Ku Kim, Lejla Colic, Mohammad Arbabi, Gholamhossein Mobaraki, Gholamreza Hassanzadeh, Martin Walter
BACKGROUND: Neuroimaging, immunologic, and pharmacologic studies have emphasized the role of 5-HT2A and 5-HT3A serotonin receptors in the pathophysiology of major depression. AIM: The aim of this study was to measure the relative expression of 5-HT2A and 5-HT3A receptor mRNA in peripheral blood mononuclear cells (PBMCs) of patients with major depressive disorder (MDD). METHOD: 5-HT2A and 5-HT3A receptor mRNA expressions were examined in PBMCs of 25 medication-naïve-patients with MDD, 25 medication-free MDD patients, and 25 healthy controls...
January 26, 2017: Nordic Journal of Psychiatry
https://www.readbyqxmd.com/read/28106398/synthesis-of-lysergol-and-its-analogues-to-assess-serotonin-receptor-activity
#18
Haosen Yuan, Zhixian Guo, Tuoping Luo
An efficient synthesis of ergot alkaloid lysergol and its analogues is described, providing compounds for functional evaluation at the human 5-HT1A, 5-HT2A, 5-HT2B, or 5-HT2C receptors. Key features of the synthesis include the development of a tandem reaction to construct the multifunctionalized piperidine skeleton and use of a rhodium-catalyzed [3 + 2] annulation in the late-stage indole formation.
January 20, 2017: Organic Letters
https://www.readbyqxmd.com/read/28101325/role-of-psilocybin-in-the-treatment-of-depression
#19
Ananya Mahapatra, Rishi Gupta
Psilocybin is a naturally occurring alkaloid, pharmacologically similar to the classic hallucinogen lysergic acid diethylamide (LSD). Although primarily used as a recreational drug or an entheogen in particular cultural settings, recent population based studies have shown that it does not lead to serious physical or mental health problems or dependent use. In view of recent work demonstrating psilocybin's potential to increase subjective sense of wellbeing and because of its novel mechanism of 5-HT2A serotonin receptor agonism, it is being explored for possible therapeutic utility in mood and anxiety disorders...
January 2017: Therapeutic Advances in Psychopharmacology
https://www.readbyqxmd.com/read/28101155/the-5-ht2a-receptor-potassium-chloride-cotransporter-2-signaling-pathway-in-a-rat-incision-pain-model
#20
Rong Dong, Buwei Yu, Lijiao Chen, Weifeng Yu
Postoperative pain is a critical problem in clinical pain administration. Due to the unclear formation mechanism of postoperative pain, the treatment of postoperative pain is still in the symptomatic treatment stage and lacking satisfactory analgesic effect. Postoperative pain can be simulated by using a rat incision pain model. We observed changes in pain-related behavior of rats affected by the 5-hydroxytryptamine 2A receptor (5-HT2AR) agonist, TCB-2, and antagonist, ketanserin, through intrathecal delivery...
December 2016: Experimental and Therapeutic Medicine
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