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Sibenadet hydrochloride

Cat. No. M28582
Sibenadet hydrochloride Structure
Synonym:

AR-C68397AA

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Biological Activity

Sibenadet hydrochloride (AR-C68397AA) is a dual D2 dopamine receptor, beta2-adrenoceptor agonist with bronchodilator activity. Investigation in animal models of key chronic obstructive pulmonary disease (COPD) symptoms has demonstrated that Sibenadet hydrochloride effectively inhibits sensory nerve activity, thereby reducing reflex cough, mucus production and tachypnoea.

Chemical Information
Molecular Weight 501.06
Formula C22H29ClN2O5S2
CAS Number 154189-24-9
Storage Please store the product under the recommended conditions in the Certificate of Analysis.
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] Jonathan P Bradley, et al. J Pharm Sci. Probing intermolecular hydrogen bonding in sibenadet hydrochloride polymorphs by high-resolution (1) H double-quantum solid-state NMR spectroscopy

[2] Stephen Connolly, et al. Bioorg Med Chem Lett. Design-driven LO: the discovery of new ultra long acting dibasic β2-adrenoceptor agonists

[3] S D Cosgrove, et al. J Pharm Sci. Understanding the polymorphic behavior of sibenadet hydrochloride through detailed studies integrating structural and dynamical assessment

[4] F C Hiller, et al. Respir Med. Long-term use of Viozan (sibenadet HCl) in patients with chronic obstructive pulmonary disease: results of a 1-year study

[5] P W Ind, et al. Respir Med. Early clinical investigation of Viozan (sibenadet HCl), a novel D2 dopamine receptor, beta2-adrenoceptor agonist for the treatment of chronic obstructive pulmonary disease symptoms

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