Endogenous Serotonin 5-HT2A and 5-HT2C Receptors Associate in the Medial Prefrontal Cortex.

Abstract:

:The 5-HT2A receptor (5-HT2AR) and 5-HT2CR are localized to the same neurons within the medial prefrontal cortex (mPFC), which regulates executive function, decision-making, and reward-guided learning and memory processes. The 5-HT2AR and 5-HT2CR coimmunoprecipitate in the mPFC of male Sprague-Dawley rats, while in vitro studies demonstrate the presence of a physical interaction between the 5-HT2AR and 5-HT2CR. The purpose of this study was to identify mPFC subregions in which the 5-HT2AR and 5-HT2CR physically interact ex vivo in the male Sprague-Dawley rat. We established the expression patterns of 5-HT2AR and 5-HT2CR in layers I-VI of the anterior cingulate cortex (ACC), prelimbic (PL), and infralimbic (IL) subregions using double-label fluorescence immunohistochemistry in male rats. We then employed the proximity ligation assay (PLA) to test the hypothesis that the 5-HT2AR and 5-HT2CR form a close, physical association within these mPFC subregions. Our results demonstrate subregion- and layer-specific expression of the 5-HT2AR and 5-HT2CR proteins using immunofluorescence and single recognition PLA, and a spatially close (within 40 nm) interaction between the 5-HT2AR and 5-HT2CR that occurs along a dorsal-ventral gradient in the rat mPFC.

journal_name

ACS Chem Neurosci

authors

Price AE,Sholler DJ,Stutz SJ,Anastasio NC,Cunningham KA

doi

10.1021/acschemneuro.8b00669

subject

Has Abstract

pub_date

2019-07-17 00:00:00

pages

3241-3248

issue

7

issn

1948-7193

journal_volume

10

pub_type

杂志文章
  • Thermodynamic description of Beta amyloid formation using physicochemical scales and fractal bioinformatic scales.

    abstract::Protein function depends on both protein structure and amino acid (aa) sequence. Here we show that modular features of both structure and function can be quantified economically from the aa sequences alone for the small (40,42 aa) plaque-forming (aggregative) amyloid beta fragments. Some edge and center features of th...

    journal_title:ACS chemical neuroscience

    pub_type: 杂志文章

    doi:10.1021/cn5001793

    authors: Phillips JC

    更新日期:2015-05-20 00:00:00

  • EF-hands in Neuronal Calcium Sensor Downstream Regulatory Element Antagonist Modulator Demonstrate Submillimolar Affinity for Li+: A New Prospect for Li+ Therapy.

    abstract::Lithium has been used for the treatment of mood disorders for decades though the molecular mechanism of its therapeutic action and intracellular targets remain furtive. We report that neurotropic agent Li+ binds to the neuronal calcium sensor, Downstream Regulatory Element Antagonist Modulator (DREAM), with an equilib...

    journal_title:ACS chemical neuroscience

    pub_type: 杂志文章

    doi:10.1021/acschemneuro.0c00399

    authors: Azam S,Bhattarai N,Riveron A,Rodriguez S,Chapagain PP,Miksovska J

    更新日期:2020-09-02 00:00:00

  • Increased Brain Exposure of an Alpha-Synuclein Fibrillization Modulator by Utilization of an Activated Ester Prodrug Strategy.

    abstract::Previous work in our laboratories has identified a series of peptidomimetic 2-pyridone molecules as modulators of alpha-synuclein (α-syn) fibrillization in vitro. As a first step toward developing molecules from this scaffold as positron emission tomography imaging agents, we were interested in evaluating their blood-...

    journal_title:ACS chemical neuroscience

    pub_type: 杂志文章

    doi:10.1021/acschemneuro.8b00236

    authors: Cairns AG,Vazquez-Romero A,Mahdi Moein M,Ådén J,Elmore CS,Takano A,Arakawa R,Varrone A,Almqvist F,Schou M

    更新日期:2018-11-21 00:00:00

  • PDE-7 Inhibitor BRL-50481 Reduces Neurodegeneration and Long-Term Memory Deficits in Mice Following Sevoflurane Exposure.

    abstract::Sevoflurane, one of the most commonly used anesthetic agents, has been demonstrated to induce widespread neurodegeneration in the developing brain. We aimed to evaluate the protective effects of a PDE-7 inhibitor (BRL-50481) against the neurotoxic effects of sevoflurane on the developing nervous system. Spatial learni...

    journal_title:ACS chemical neuroscience

    pub_type: 杂志文章

    doi:10.1021/acschemneuro.0c00106

    authors: Chen Y,Li S,Zhong X,Kang Z,Chen R

    更新日期:2020-05-06 00:00:00

  • The molecular basis of memory. Part 2: chemistry of the tripartite mechanism.

    abstract::We propose a tripartite mechanism to describe the processing of cognitive information (cog-info), comprising the (1) neuron, (2) surrounding neural extracellular matrix (nECM), and (3) numerous "trace" metals distributed therein. The neuron is encased in a polyanionic nECM lattice doped with metals (>10), wherein it p...

    journal_title:ACS chemical neuroscience

    pub_type: 杂志文章,评审

    doi:10.1021/cn300237r

    authors: Marx G,Gilon C

    更新日期:2013-06-19 00:00:00

  • Antidepressive Effect of Arctiin by Attenuating Neuroinflammation via HMGB1/TLR4- and TNF-α/TNFR1-Mediated NF-κB Activation.

    abstract::Inflammation is a potential factor in the pathophysiology of depression. A traditional Chinese herbal medicine, arctiin, and its aglycone, arctigenin, are the major bioactive components in Fructus arctii and exhibit neuroprotective and anti-inflammatory activities. Arctigenin has been reported to have antidepressant-l...

    journal_title:ACS chemical neuroscience

    pub_type: 杂志文章

    doi:10.1021/acschemneuro.0c00120

    authors: Xu X,Zeng XY,Cui YX,Li YB,Cheng JH,Zhao XD,Xu GH,Ma J,Piao HN,Jin X,Piao LX

    更新日期:2020-08-05 00:00:00

  • (3-Cyano-5-fluorophenyl)biaryl negative allosteric modulators of mGlu(5): Discovery of a new tool compound with activity in the OSS mouse model of addiction.

    abstract::Glutamate is the major excitatory transmitter in the mammalian CNS, exerting its effects through both ionotropic and metabotropic glutamate receptors. The metabotropic glutamate receptors (mGlus) belong to family C of the G-protein-coupled receptors (GPCRs). The eight mGlus identified to date are classified into three...

    journal_title:ACS chemical neuroscience

    pub_type: 杂志文章

    doi:10.1021/cn100099n

    authors: Lindsley CW,Bates BS,Menon UN,Jadhav SB,Kane AS,Jones CK,Rodriguez AL,Conn PJ,Olsen CM,Winder DG,Emmitte KA

    更新日期:2011-08-17 00:00:00

  • Maternal Exposure to Di-(2-ethylhexyl) Phthalate Impairs Hippocampal Synaptic Plasticity in Male Offspring: Involvement of Damage to Dendritic Spine Development.

    abstract::Exposure to di-(2-ethylhexyl) phthalate (DEHP), a widely used kind of plasticizer, can result in neurodevelopment impairments and learning and memory disorders. We studied the effects and possible mechanisms of maternal DEHP treatment on hippocampal synaptic plasticity in offspring. Pregnant Wistar rats were randomly ...

    journal_title:ACS chemical neuroscience

    pub_type: 杂志文章

    doi:10.1021/acschemneuro.0c00612

    authors: Dong J,Fu H,Fu Y,You M,Li X,Wang C,Leng K,Wang Y,Chen J

    更新日期:2021-01-20 00:00:00

  • Effects of Baicalein on Cortical Proinflammatory Cytokines and the Intestinal Microbiome in Senescence Accelerated Mouse Prone 8.

    abstract::Baicalein, a flavonoid derived from the roots of Scutellariae baicalensis Georgi, has shown health benefits for an array of human diseases including dementia. The senescence-accelerated mouse prone 8 (SAMP8) strain is extensively used as a senile dementia model. To further investigate the effects of baicalein in SAMP8...

    journal_title:ACS chemical neuroscience

    pub_type: 杂志文章

    doi:10.1021/acschemneuro.8b00074

    authors: Gao L,Li J,Zhou Y,Huang X,Qin X,Du G

    更新日期:2018-07-18 00:00:00

  • A Multifunctional Chemical Agent as an Attenuator of Amyloid Burden and Neuroinflammation in Alzheimer's Disease.

    abstract::Alzheimer's disease (AD) is the most common neurodegenerative disease, and its main hallmark is the deposition of amyloid beta (Aβ) peptides. However, several clinical trials focusing on Aβ-targeting agents have failed recently, and thus new therapeutic leads are focusing on alternate targets such as tau protein patho...

    journal_title:ACS chemical neuroscience

    pub_type: 杂志文章

    doi:10.1021/acschemneuro.0c00114

    authors: Cho HJ,Sharma AK,Zhang Y,Gross ML,Mirica LM

    更新日期:2020-05-20 00:00:00

  • Tau-derived-hexapeptide 306VQIVYK311 aggregation inhibitors: nitrocatechol moiety as a pharmacophore in drug design.

    abstract::The nitrocatechol derivatives tolcapone (1) and entacapone (2), used as adjunctive therapy in the treatment of Parkinson's disease, were investigated for their potential to inhibit the tau-derived-hexapeptide 306VQIVYK311. They were compared to small molecules that contain similar pharmacophores including the catechol...

    journal_title:ACS chemical neuroscience

    pub_type: 杂志文章

    doi:10.1021/cn400151a

    authors: Mohamed T,Hoang T,Jelokhani-Niaraki M,Rao PP

    更新日期:2013-12-18 00:00:00

  • An azobenzene photoswitch sheds light on turn nucleation in amyloid-β self-assembly.

    abstract::Amyloid-β (Aβ) self-assembly into cross-β amyloid fibrils is implicated in a causative role in Alzheimer's disease pathology. Uncertainties persist regarding the mechanisms of amyloid self-assembly and the role of metastable prefibrillar aggregates. Aβ fibrils feature a sheet-turn-sheet motif in the constituent β-stra...

    journal_title:ACS chemical neuroscience

    pub_type: 杂志文章

    doi:10.1021/cn2001188

    authors: Doran TM,Anderson EA,Latchney SE,Opanashuk LA,Nilsson BL

    更新日期:2012-03-21 00:00:00

  • Oligomer Diversity during the Aggregation of the Repeat Region of Tau.

    abstract::The molecular mechanism of protein aggregation is of both fundamental and clinical importance as amyloid aggregates are linked to a number of neurodegenerative disorders. Such protein aggregates include macroscopic insoluble fibrils as well as small soluble oligomeric species. Time-dependent resolution of these specie...

    journal_title:ACS chemical neuroscience

    pub_type: 杂志文章

    doi:10.1021/acschemneuro.8b00250

    authors: Kjaergaard M,Dear AJ,Kundel F,Qamar S,Meisl G,Knowles TPJ,Klenerman D

    更新日期:2018-12-19 00:00:00

  • Neuromicrobiology: How Microbes Influence the Brain.

    abstract::We review here recent discoveries in the exciting new field of neuromicrobiology. This field encompasses the interactions between the microbiome and the central nervous system. The microbiome has a tremendous impact on human health. In particular, the gut microbiota may play a key role in many essential processes in h...

    journal_title:ACS chemical neuroscience

    pub_type: 杂志文章,评审

    doi:10.1021/acschemneuro.7b00373

    authors: de la Fuente-Nunez C,Meneguetti BT,Franco OL,Lu TK

    更新日期:2018-02-21 00:00:00

  • Identification of Metabotropic Glutamate Receptor Subtype 5 Potentiators Using Virtual High-Throughput Screening.

    abstract::Selective potentiators of glutamate response at metabotropic glutamate receptor subtype 5 (mGluR5) have exciting potential for the development of novel treatment strategies for schizophrenia. A total of 1,382 compounds with positive allosteric modulation (PAM) of the mGluR5 glutamate response were identified through h...

    journal_title:ACS chemical neuroscience

    pub_type: 杂志文章

    doi:10.1021/cn9000389

    authors: Mueller R,Rodriguez AL,Dawson ES,Butkiewicz M,Nguyen TT,Oleszkiewicz S,Bleckmann A,Weaver CD,Lindsley CW,Conn PJ,Meiler J

    更新日期:2010-04-21 00:00:00

  • Quantitative proteomics analysis of CaMKII phosphorylation and the CaMKII interactome in the mouse forebrain.

    abstract::Ca(2+)/calmodulin-dependent protein kinase IIα (CaMKIIα) autophosphorylation at Thr286 and Thr305/Thr306 regulates kinase activity and modulates subcellular targeting and is critical for normal synaptic plasticity and learning and memory. Here, a mass spectrometry-based approach was used to identify Ca(2+)-dependent a...

    journal_title:ACS chemical neuroscience

    pub_type: 杂志文章

    doi:10.1021/cn500337u

    authors: Baucum AJ 2nd,Shonesy BC,Rose KL,Colbran RJ

    更新日期:2015-04-15 00:00:00

  • Mitochondrial GSH Systems in CA1 Pyramidal Cells and Astrocytes React Differently during Oxygen-Glucose Deprivation and Reperfusion.

    abstract::Pyramidal cells and astrocytes have differential susceptibility to oxygen-glucose deprivation and reperfusion (OGD-RP). It is known that excessive reactive oxygen species (ROS) in mitochondria initiates cell death, while glutathione (GSH) is one of the major defenses against ROS. Although it is known that astrocytes c...

    journal_title:ACS chemical neuroscience

    pub_type: 杂志文章

    doi:10.1021/acschemneuro.7b00369

    authors: Yin B,Barrionuevo G,Weber SG

    更新日期:2018-04-18 00:00:00

  • D-serine uptake and release in PC-12 cells measured by chiral microchip electrophoresis-mass spectrometry.

    abstract::Previous work has established that D-serine (D-Ser) plays important roles in certain neurological processes. Study on its uptake/storage and release by neuronal cells is highly significant for elucidating relevant mechanisms. In this work, PC-12 cells were incubated with racemic Ser (100 μM each enantiomer). After inc...

    journal_title:ACS chemical neuroscience

    pub_type: 杂志文章

    doi:10.1021/cn5003122

    authors: Li X,McCullum C,Zhao S,Hu H,Liu YM

    更新日期:2015-04-15 00:00:00

  • The implications of angiotensin-converting enzymes and their modulators in neurodegenerative disorders: current and future perspectives.

    abstract::Angiotensin converting enzyme (ACE) is a dipeptidyl peptidase transmembrane bound enzyme. Generally, ACE inhibitors are used for the cardiovascular disorders. ACE inhibitors are primary agents for the management of hypertension, so these cannot be avoided for further use. The present Review focuses on the implications...

    journal_title:ACS chemical neuroscience

    pub_type: 杂志文章,评审

    doi:10.1021/cn500363g

    authors: Kaur P,Muthuraman A,Kaur M

    更新日期:2015-04-15 00:00:00

  • Activation of Dopamine D3 Receptor Subtypes Inhibits the Neurogenic Systemic Vasodilation Induced by Stimulation of the Perivascular CGRPergic Discharge.

    abstract::The sensory nervous system controls cardiovascular homeostasis via capsaicin-sensitive neurons that release calcitonin gene-related peptide (CGRP), which subsequently activates CGRP receptors. How this perivascular CGRPergic discharge is modulated, nevertheless, remains unclear. In pithed rats, systemic vasodilation i...

    journal_title:ACS chemical neuroscience

    pub_type: 杂志文章

    doi:10.1021/acschemneuro.9b00277

    authors: Manrique-Maldonado G,Altamirano-Espinoza AH,Rivera-Mancilla E,Hernández-Abreu O,Villalón CM

    更新日期:2019-08-21 00:00:00

  • Novel Tadalafil Derivatives Ameliorates Scopolamine-Induced Cognitive Impairment in Mice via Inhibition of Acetylcholinesterase (AChE) and Phosphodiesterase 5 (PDE5).

    abstract::On the basis of the drug-repositioning and redeveloping strategy, first-generation dual-target inhibitors of acetylcholinesterase (AChE) and phosphodiesterase 5 (PDE5) have been recently reported as a potentially novel therapeutic method for the treatment of Alzheimer's disease (AD), and the lead compound 2 has proven...

    journal_title:ACS chemical neuroscience

    pub_type: 杂志文章

    doi:10.1021/acschemneuro.8b00014

    authors: Ni W,Wang H,Li X,Zheng X,Wang M,Zhang J,Gong Q,Ling D,Mao F,Zhang H,Li J

    更新日期:2018-07-18 00:00:00

  • Behavioral and Biochemical Implications of Dendrimeric Rivastigmine in Memory-Deficit and Alzheimer's Induced Rodents.

    abstract::Exploration of dendrimers for effective drug delivery is giving promising results. The present study was designed and performed to explore the dendrimeric (polyamidoamine-lactoferrin; PAMAM-Lf) formulations for the effective rivastigmine (RIV) delivery against the Alzheimer's induced animal model using lactoferrin as ...

    journal_title:ACS chemical neuroscience

    pub_type: 杂志文章

    doi:10.1021/acschemneuro.9b00286

    authors: Gothwal A,Singh H,Jain SK,Dutta A,Borah A,Gupta U

    更新日期:2019-08-21 00:00:00

  • Hydrogels in spinal cord injury repair strategies.

    abstract::Nowadays there are at present no efficient therapies for spinal cord injury (SCI), and new approaches have to be proposed. Recently, a new regenerative medicine strategy has been suggested using smart biomaterials able to carry and deliver cells and/or drugs in the damaged spinal cord. Among the wide field of emerging...

    journal_title:ACS chemical neuroscience

    pub_type: 杂志文章,评审

    doi:10.1021/cn200030w

    authors: Perale G,Rossi F,Sundstrom E,Bacchiega S,Masi M,Forloni G,Veglianese P

    更新日期:2011-07-20 00:00:00

  • Development of Clickable Photoaffinity Ligands for Metabotropic Glutamate Receptor 2 Based on Two Positive Allosteric Modulator Chemotypes.

    abstract::The metabotropic glutamate receptor 2 (mGlu2) is a transmembrane-spanning class C G protein-coupled receptor that is an attractive therapeutic target for multiple psychiatric and neurological disorders. A key challenge has been deciphering the contribution of mGlu2 relative to other closely related mGlu receptors in m...

    journal_title:ACS chemical neuroscience

    pub_type: 杂志文章

    doi:10.1021/acschemneuro.0c00009

    authors: Hellyer SD,Aggarwal S,Chen ANY,Leach K,Lapinsky DJ,Gregory KJ

    更新日期:2020-06-03 00:00:00

  • Benzothiophene Selective Estrogen Receptor Modulators Provide Neuroprotection by a novel GPR30-dependent Mechanism.

    abstract::The clinical benzothiophene SERM (BT-SERM), raloxifene, was compared with estrogens in protection of primary rat neurons against oxygen-glucose deprivation (OGD). Structure-activity relationships for neuroprotection were determined for a family of BT-SERMs displaying a spectrum of ERα and ERβ binding affinity and agon...

    journal_title:ACS chemical neuroscience

    pub_type: 杂志文章

    doi:10.1021/cn100106a

    authors: Abdelhamid R,Luo J,Vandevrede L,Kundu I,Michalsen B,Litosh VA,Schiefer IT,Gherezghiher T,Yao P,Qin Z,Thatcher GR

    更新日期:2011-05-18 00:00:00

  • Bromoalkaloids protect primary cortical neurons from induced oxidative stress.

    abstract::Bromoalkaloids are secondary metabolites with a demonstrated high activity in several therapeutic areas. In this research, we probe the neuroprotective and antioxidant activities of hymenialdisine and hymenin. Both structures were tested in an oxidative stress cellular model, consisting of cortical neurons that are in...

    journal_title:ACS chemical neuroscience

    pub_type: 杂志文章

    doi:10.1021/cn500258c

    authors: Leirós M,Alonso E,Rateb ME,Houssen WE,Ebel R,Jaspars M,Alfonso A,Botana LM

    更新日期:2015-02-18 00:00:00

  • Alzheimer's Amyloid-β Sequesters Caspase-3 in Vitro via Its C-Terminal Tail.

    abstract::Amyloid-β (Aβ), the main constituent in senile plaques found in the brain of patients with Alzheimer's disease (AD), is considered as a causative factor in AD pathogenesis. The clinical examination of the brains of patients with AD has demonstrated that caspase-3 colocalizes with senile plaques. Cellular studies have ...

    journal_title:ACS chemical neuroscience

    pub_type: 杂志文章

    doi:10.1021/acschemneuro.6b00049

    authors: Chang YJ,Linh NH,Shih YH,Yu HM,Li MS,Chen YR

    更新日期:2016-08-17 00:00:00

  • A Small Molecule Mimetic of the Humanin Peptide as a Candidate for Modulating NMDA-Induced Neurotoxicity.

    abstract::Humanin (HN), a 24-amino acid bioactive peptide, has been shown to increase cell survival of neurons after exposure to Aβ and NMDA-induced toxicity and thus could be beneficial in the treatment of Alzheimer's disease (AD). The neuroprotection by HN is reported to be primarily through its agonist binding properties to ...

    journal_title:ACS chemical neuroscience

    pub_type: 杂志文章

    doi:10.1021/acschemneuro.7b00350

    authors: Alam MP,Bilousova T,Spilman P,Vadivel K,Bai D,Elias CJ,Evseenko D,John V

    更新日期:2018-03-21 00:00:00

  • Deciphering the Mechanism of the Anti-Hypertensive Effect of Isorhynchophylline by Targeting Neurotransmitters Metabolism of Hypothalamus in Spontaneously Hypertensive Rats.

    abstract::Essential hypertension is a major risk factor for cardiovascular disease that can lead eventually to structural and functional alterations in the brain. Accumulating evidence has suggested that the increased activities in renin-angiotensin system and sympathetic nerve participated in the pathogenesis of hypertension t...

    journal_title:ACS chemical neuroscience

    pub_type: 杂志文章

    doi:10.1021/acschemneuro.9b00699

    authors: Li Y,Yu R,Zhang D,Yang W,Hou Q,Li Y,Jiang H

    更新日期:2020-06-03 00:00:00

  • Synthesis and pharmacology of halogenated δ-opioid-selective [d-Ala(2)]deltorphin II peptide analogues.

    abstract::Deltorphins are naturally occurring peptides produced by the skin of the giant monkey frog (Phyllomedusa bicolor). They are δ-opioid receptor-selective agonists. Herein, we report the design and synthesis of a peptide, Tyr-d-Ala-(pI)Phe-Glu-Ile-Ile-Gly-NH2 3 (GATE3-8), based on the [d-Ala(2)]deltorphin II template, wh...

    journal_title:ACS chemical neuroscience

    pub_type: 杂志文章

    doi:10.1021/acschemneuro.5b00060

    authors: Pescatore R,Marrone GF,Sedberry S,Vinton D,Finkelstein N,Katlowitz YE,Pasternak GW,Wilson KR,Majumdar S

    更新日期:2015-06-17 00:00:00