Abcam, ab120061, Cyclothiazide, AMPA receptor desensitisation inhibitor

Size: 10mg / 50mg
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).
Key facts
CAS number:2259-96-3,
Purity:>98%,
Form:SolidSee storage information,
Molecular weight:389.9 Da,
Molecular formula:C14H16ClN3O4S2,
PubChem:2910,
Nature:Synthetic,
Solubility:Soluble in ethanol to 25 mMSoluble in DMSO to 100 mM,
Biochemical name:Cyclothiazide,
Biological description: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).,
Canonical 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 Name:3-(2-bicyclo[2.2.1]hept-5-enyl)-6-chloro-1,1-dioxo-3,4-dihydro-2H-1λ6,2,4-benzothiadiazine-7-sulfonamide

Properties and Storage Information:
Shipped at conditions-Ambient - Can Ship with Ice, Appropriate short-term storage conditions-+4°C, Appropriate long-term storage conditions-+4°C, Storage information-Store under desiccating conditions, The product can be stored for up to 12 months

Supplementary Information:
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.