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Sigma-1 receptor antagonist 5

Cat. No. M42704
Sigma-1 receptor antagonist 5 Structure
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Biological Activity

Sigma-1 receptor antagonist 5 and histamine H3 (hH3R, Ki=7.7 nM, IC50=215 nM).

Chemical Information
Molecular Weight 397.51
Formula C26H27N3O
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Alba Vera-Zambrano et al. Pharmacol Res. Sigma-1 receptor modulation fine-tunes KV1.5 channels and impacts pulmonary vascular function

[2] Dan V Iosifescu et al. J Clin Psychiatry. Efficacy and Safety of AXS-05 (Dextromethorphan-Bupropion) in Patients With Major Depressive Disorder: A Phase 3 Randomized Clinical Trial (GEMINI)

[3] Herriot Tabuteau et al. Am J Psychiatry. Effect of AXS-05 (Dextromethorphan-Bupropion) in Major Depressive Disorder: A Randomized Double-Blind Controlled Trial

[4] Melissa A Tapia et al. Behav Brain Res. Sigma-1 receptor antagonist PD144418 suppresses food reinforced operant responding in rats

[5] Omar Vélez López et al. J Neuroimmune Pharmacol. Sigma-1 Receptor Antagonist (BD1047) Decreases Cathepsin B Secretion in HIV-Infected Macrophages Exposed to Cocaine

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