Atagabalin hydrochloride
Atagabalin hydrochloride (PD 0200390 hydrochloride) is a Voltage-gated Calcium channel α2δ subunit binder with an IC50 of 22 nM. Atagabalin hydrochloride regulates neurotransmitter release by inhibiting calcium influx at high neuronal firing rates. Atagabalin hydrochloride can be used in research related to sleep disorders.
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- CAS. Nr.: 223445-67-8
- Formel: C10H20ClNO2
- Molecular Weight:221.72
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
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Chemical Information
- Protokoll
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
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Biologische Aktivität
Beschreibung
IC50 & Target
[3]|
Calcium Channel |
In Vitro
Atagabalin hydrochloride potently binds to the VGCC α2δ subunit with an IC50 of 22 nM[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS. Nr. 223445-67-8
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Molecular Weight 221.72
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Formel C10H20ClNO2
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SMILES
OC(CC1(C[C@@H]([C@H](C1)C)C)CN)=O.Cl
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Synonyms
PD 0200390 hydrochloride
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Protokoll
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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Ca2+ Staining Technique
Ca2+ staining is an experimental technique that utilizes specific fluorescent probes (such as Fluo-4 AM, Fura-2, etc.) to qualitatively or quantitatively detect dynamic changes in intracellular Ca2+ concentrations; this is achieved by monitoring the changes in fluorescent signals generated when these probes bind to free intracellular calcium ions. The underlying principle relies primarily on the presence of chelating groups within the probe's molecular structure that possess high affinity for calcium ions.
Reinheit & Dokumentation
Verweise
[1]. Kjellsson MC, et al. Modeling sleep data for a new drug in development using markov mixed-effects models. Pharmaceutical research. 2011 Oct;28(10):2610-27. [Content Brief]
[2]. Corrigan B, et al. Effect of renal impairment on the pharmacokinetics of PD 0200390, a novel ligand for the voltage-gated calcium channel alpha-2-delta subunit. British journal of clinical pharmacology. 2009 Aug;68(2):174-80. [Content Brief]
[3]. Chen Y, et al. Review of Voltage-gated Calcium Channel α2δ Subunit Ligands for the Treatment of Chronic Neuropathic Pain and Insight into Structure-activity Relationship (SAR) by Pharmacophore Modeling. Current medicinal chemistry. 2022 Aug 15;29(30):5097-5112. [Content Brief]
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Atagabalin hydrochloride Related Classifications
HY-14856B Related Classifications
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Keywords
- Atagabalin
- 223445-67-8
- PD 0200390
- PD0200390
- PD-0200390
- Calcium Channel
- renal excretion
- neurotransmitter release
- calcium channel α2δ subunit
- insomnia
- sleep disturbance
- slow-wave sleep
- rapid eye movement sleep
- pharmacophore modeling
- voltage-gated calcium channel alpha-2-delta subunits
- calcium influx
- Inhibitor
- inhibitor
- inhibit