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Arotinolol

Cat. No. M30480
Arotinolol Structure
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Biological Activity

Arotinolol is a nonselective α/β-adrenergic receptor blocker and a vasodilating β-blocker. Arotinolol also shows potency for inhibiting the binding of the radioligand 125I-ICYP to 5HT1B-serotonergic receptor sites. Arotinolol is an antihypertensive agent for the treatment of a variety of cardiovascular pathologies as well as non-cardiovascular diseases.

Chemical Information
Molecular Weight 371.54
Formula C15H21N3O2S3
CAS Number 68377-92-4
Form Solid
Solubility (25°C) DMSO 125 mg/mL (ultrasonic)
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] Pingping Huang, et al. Front Cardiovasc Med. Effect of arotinolol on chronic heart failure: A systematic review and meta-analysis of randomized controlled trials

[2] Zheyuan Qian, et al. J Pharm Biomed Anal. Enantiospecific determination of arotinolol in rat plasma by LC-MS/MS: application to a stereoselective pharmacokinetic study

[3] Wugang Zhou, et al. PLoS One. Mechanisms of improved aortic stiffness by arotinolol in spontaneously hypertensive rats

[4] J Zhao, et al. Can J Physiol Pharmacol. Arotinolol is a weak partial agonist on beta 3-adrenergic receptors in brown adipocytes

[5] S Morimoto, et al. Clin Exp Pharmacol Physiol. Effects of arotinolol, an alpha- and beta-adrenoceptor antagonist, on renin release from rat kidney cortical slices

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