AB120061

Cyclothiazide, AMPA receptor desensitisation inhibitor

Name: Cyclothiazide, AMPA receptor desensitisation抑制剂 (ab120061)| Abcam中文官网
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SKU: AB120061
Price: 1065 CNY
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(18 Publications)

MW 389.9 Da, Purity >98%. Positive allosteric modulator of AMPA receptors. Produces a fast inhibition of AMPA receptor desensitization and a much slower potentiation of the AMPA current. Also available in Kit: Ionotropic agonists (ab120323).

查看别名

AMPA 1, AMPA 2, AMPA 3, AMPA 4, AMPA-selective glutamate receptor 1, AMPA-selective glutamate receptor 2, AMPA-selective glutamate receptor 3, AMPA-selective glutamate receptor 4, GLUH1, GLUK3, GLUR4C, GRIA1_HUMAN, GRIA2_HUMAN, GRIA3_HUMAN, GRIA4_HUMAN, GluA 4, GluA1, GluA2, GluA3, GluR-1, GluR-2, GluR-3, GluR-4, GluR-A, GluR-B, GluR-C, GluR-D, GluR-K1, GluR-K2, GluR-K3, Glutamate ionotropic receptor AMPA type subunit 3, Glutamate receptor 1, Glutamate receptor 2, Glutamate receptor 3, Glutamate receptor 4, Glutamate receptor C, Glutamate receptor ionotrophic AMPA 3, Glutamate receptor ionotrophic AMPA 4, Glutamate receptor ionotropic, Glutamate receptor ionotropic AMPA 1, Glutamate receptor ionotropic AMPA 2, Glutamate receptor subunit 3, Glutamate receptor, ionotropic, AMPA 3, HBGR1, HBGR2, Ionotrophic Glutamate Receptor, Ionotropic Glutamate receptor 4, MGC133252, MRX94, OTTHUMP00000160643, OTTHUMP00000165781, OTTHUMP00000224241, OTTHUMP00000224242, OTTHUMP00000224243, dJ1171F9.1

2 Images

Cellular Activation - Cyclothiazide, AMPA receptor desensitisation inhibitor (AB120061)

CellAct

Unknown

Cellular Activation - Cyclothiazide, AMPA receptor desensitisation inhibitor (AB120061)

To determine the capability of VCN-LSO synapses to support repetitive activity in the developing circuit, we added cyclothiazide to the perfusate to prevent AMPAR desensitization and measured responses to 50 Hz pulse-train stimuli delivered to the ventral acoustic stria. A. Representative responses to 50 Hz pulse-trains in P2, P5, and P9 cells; responses to the first five pulses only are shown. Greater paired-pulse depression between pulse 1 and 2 is evident in the youngest cell than in the older cells.

Image from Case DT, et al. Plos One, 6(6), e20756. Fig S4,; doi: 10.1371/journal.pone.0020756

Chemical Structure - Cyclothiazide, AMPA receptor desensitisation inhibitor (AB120061)

Chemical Structure

Lab

Chemical Structure - Cyclothiazide, AMPA receptor desensitisation inhibitor (AB120061)

2D chemical structure image of ab120061, Cyclothiazide, AMPA receptor desensitisation inhibitor

关键信息

CAS 号

2259-96-3

纯度

>98%

形式

Solid

form

分子量

389.9 Da

分子式

C14H16ClN3O4S2

PubChem

2910

属性

Synthetic

溶解度

Soluble in ethanol to 25 mM

Soluble in DMSO to 100 mM

生化试剂名称

Cyclothiazide

生物学描述

Positive allosteric modulator of AMPA receptors. Produces a fast inhibition of AMPA receptor desensitization and a much slower potentiation of the AMPA current. Also available in Kit: Ionotropic agonists (ab120323).

经典 SMILES

C1C2CC(C1C=C2)C3NC4=CC(=C(C=C4S(=O)(=O)N3)S(=O)(=O)N)Cl

InChi

InChI=1S/C14H16ClN3O4S2/c15-10-5-11-13(6-12(10)23(16,19)20)24(21,22)18-14(17-11)9-4-7-1-2-8(9)3-7/h1-2,5-9,14,17-18H,3-4H2,(H2,16,19,20)

InChiKey

BOCUKUHCLICSIY-UHFFFAOYSA-N

IUPAC 名

3-(2-bicyclo[2.2.1]hept-5-enyl)-6-chloro-1,1-dioxo-3,4-dihydro-2H-1λ6,2,4-benzothiadiazine-7-sulfonamide

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性能和储存信息

运输条件

Ambient - Can Ship with Ice

储存信息

Store under desiccating conditions|The product can be stored for up to 12 months

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补充信息

This supplementary information is collated from multiple sources and compiled automatically.

Glutamate Receptor 1 also called AMPA receptor 1 is an ionotropic receptor that mediates fast synaptic transmission in the central nervous system. It is part of a larger family of glutamate receptors including subtypes GluA2 GluA3 and GluA4. The AMPA receptor structure typically forms a tetrameric complex mainly located in neuronal cells such as those in the hippocampus and cerebral cortex. The receptor has a mass of approximately 100 kDa. These receptors enable rapid excitatory signaling by allowing the flow of sodium (Na+) and calcium (Ca2+) ions into the cell upon binding glutamate.

Biological function summary

The AMPA receptors facilitate neuronal communication and plasticity by modulating synaptic strength. This modulation occurs through processes such as potentiation and desensitisation where the receptor's response to glutamate changes. Potentiated sulfonamides like cyclothiazide can influence AMPA receptor activity by preventing desensitization maintaining prolonged neurotransmission. Cyclothiazide itself binds within the AMPA structure altering the conformation to prevent the desensitised state which is key in sustaining synaptic efficacy. AMPA receptors also interact with auxiliary proteins like TARPs (Transmembrane AMPA Receptor Regulatory Proteins) that assist in their trafficking and channel properties.

Pathways

AMPA receptors play a significant role in the glutamatergic pathway integral for synaptic transmission and neuroplasticity. This pathway influences learning and memory processes. AMPA receptors also interact with the NMDA receptors in long-term potentiation (LTP) a process critical for memory formation and synaptic strength. Additionally they connect with proteins like CaMKII (Calcium/Calmodulin-dependent protein kinase II) during signal transduction processes inside neurons important for cellular responses following synaptic activation.

Abnormal AMPA receptor function associates with neurodegenerative conditions like Alzheimer’s disease and neurological disorders such as epilepsy. Dysregulation can lead to conditions characterized by excitotoxicity where excessive receptor activity causes neuronal damage. The abnormal interaction between AMPA receptors and proteins like the NMDA receptor may contribute to these conditions. Therapies targeting AMPA receptors aiming to modulate their activity present possible strategies for managing these diseases highlighting their importance on the AMPA receptors market.

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产品实验方案

Visit the General protocols
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文献 (18)

Recent publications for all applications. Explore the full list and refine your search

Frontiers in cellular neuroscience 12:513 PubMed30670950

2019

Electrophysiological Excitability and Parallel Fiber Synaptic Properties of Zebrin-Positive and -Negative Purkinje Cells in Lobule VIII of the Mouse Cerebellar Slice.

Applications

Unspecified application

Species

Unspecified reactive species

Viet T Nguyen-Minh,Khoa Tran-Anh,Yuanjun Luo,Izumi Sugihara

Biomedicine & pharmacotherapy = Biomedecine & phar 101:362-370 PubMed29499411

2018

GIRK1-mediated inwardly rectifying potassium current suppresses the epileptiform burst activities and the potential antiepileptic effect of ML297.

Applications

Unspecified application

Species

Unspecified reactive species

Yian Huang,Yuwen Zhang,Shuzhen Kong,Kai Zang,Shize Jiang,Li Wan,Lulan Chen,Guoxiang Wang,Min Jiang,Xin Wang,Jie Hu,Yun Wang

Frontiers in molecular neuroscience 10:402 PubMed29276473

2017

Ferric Chelate Reductase 1 Like Protein (FRRS1L) Associates with Dynein Vesicles and Regulates Glutamatergic Synaptic Transmission.

Applications

Unspecified application

Species

Unspecified reactive species

Wenyan Han,Huiqing Wang,Jun Li,Shizhong Zhang,Wei Lu

The European journal of neuroscience 46:2519-2533 PubMed28921719

2017

Inflammation alters AMPA-stimulated calcium responses in dorsal striatal D2 but not D1 spiny projection neurons.

Applications

Unspecified application

Species

Unspecified reactive species

Carissa D Winland,Nora Welsh,Alberto Sepulveda-Rodriguez,Stefano Vicini,Kathleen A Maguire-Zeiss

Scientific reports 7:44817 PubMed28322255

2017

Ca-permeable AMPA receptors in mouse olfactory bulb astrocytes.

Applications

Unspecified application

Species

Unspecified reactive species

Damian Droste,Gerald Seifert,Laura Seddar,Oliver Jädtke,Christian Steinhäuser,Christian Lohr

Philosophical transactions of the Royal Society of London. Series B, Biological sciences 369:20130602 PubMed25225096

2014

Heterogeneity in expression of functional ionotropic glutamate and GABA receptors in astrocytes across brain regions: insights from the thalamus.

Applications

Unspecified application

Species

Unspecified reactive species

Simon Höft,Stephanie Griemsmann,Gerald Seifert,Christian Steinhäuser

The Journal of neuroscience : the official journal of the Society for Neuroscience 34:11673-83 PubMed25164663

2014

Molecular mechanisms contributing to TARP regulation of channel conductance and polyamine block of calcium-permeable AMPA receptors.

Applications

Unspecified application

Species

Unspecified reactive species

David Soto,Ian D Coombs,Esther Gratacòs-Batlle,Mark Farrant,Stuart G Cull-Candy

The Journal of neuroscience : the official journal of the Society for Neuroscience 34:980-91 PubMed24431456

2014

Photoinactivation of glutamate receptors by genetically encoded unnatural amino acids.

Applications

Unspecified application

Species

Unspecified reactive species

Viktoria Klippenstein,Valentina Ghisi,Marcus Wietstruk,Andrew J R Plested

Biochimica et biophysica acta 1833:1820-31 PubMed23545413

2013

The type II cGMP dependent protein kinase regulates GluA1 levels at the plasma membrane of developing cerebellar granule cells.

Applications

Unspecified application

Species

Unspecified reactive species

Salvatore Incontro,Francisco Ciruela,Edward Ziff,Franz Hofmann,José Sánchez-Prieto,Magdalena Torres

Nature neuroscience 14:1430-8 PubMed21983683

2011

Bidirectional plasticity of calcium-permeable AMPA receptors in oligodendrocyte lineage cells.

Applications

Unspecified application

Species

Unspecified reactive species

Marzieh Zonouzi,Massimiliano Renzi,Mark Farrant,Stuart G Cull-Candy

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Cyclothiazide, AMPA receptor desensitisation inhibitor