A β1-AR antagonist
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Bevantolol (hydrochloride)

Item No. 29792

Technical Information
Formal Name
1-[[2-(3,4-dimethoxyphenyl)ethyl]amino]-3-(3-methylphenoxy)-2-propanol, monohydrochloride
CAS Number
42864-78-8
Synonyms
  • CI-755
  • DL-Bevantolol
  • NC-1400
Molecular Formula
C20H27NO4 • HCl
Formula Weight
Purity
≥98%
Formulation
A crystalline solid
DMF: 30 mg/mlDMSO: 30 mg/mlDMSO:PBS (pH 7.2) (1:1): 0.50 mg/ml
SMILES
CC1=CC=CC(OCC(O)CNCCC2=CC(OC)=C(OC)C=C2)=C1.Cl
InChi Code
InChI=1S/C20H27NO4.ClH/c1-15-5-4-6-18(11-15)25-14-17(22)13-21-10-9-16-7-8-19(23-2)20(12-16)24-3;/h4-8,11-12,17,21-22H,9-10,13-14H2,1-3H3;1H
InChi Key
FJTKCFSPYUMXJB-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    Bevantolol is an antagonist of the β1-adrenergic receptor (β1-AR; Ki = 14.79 nM in rat cortical membranes).1 It is selective for β1- over β2-ARs (Ki = 588.84 nM), as well as α2-ARs up to 100 μM, but is an antagonist of α1-ARs (Ki = 125.89 nM). Bevantolol inhibits low voltage-activated calcium currents (LVA-ICa) in dissociated rat ventro-medial hypothalamic neurons (IC50 = 40 μM).2 It inhibits norepinephrine-induced contraction of isolated rabbit thoracic aorta (pA2 = 4.77), isoprenaline-induced inotropic effects in isolated guinea pig right atria (pA2 = 7.74), and isoprenaline-induced relaxation of isolated guinea pig trachea (pA2 = 6.69).3 Bevantolol (250 mg/kg per day) prevents immobilization stress-induced increases in systolic blood pressure in a rat model of stress-induced hypertension.4

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Takita, M., Kigoshi, S., and Muramatsu, I. Selectivity of bevantolol hydrochloride towards ɑ and β-adrenoceptor subtypes in rat cerebral cortex. Jpn. J. Pharmacol. 58(2), 193-196 (1992).

    2. T., O., Kobayashi, T., Nishioka, K., et alCa2+-antagonistic action of bevantolol on hypothalamic neurons in vitro: Its comparison with those of other β-adrenoceptor antagonists, a local anesthetic and a Ca2+-antagonist. Brain Res. 706(2), 289-292 (1996).

    3. Takayanagi, I., Kizawa, Y., Iwasaki, S., et al(+/-)-1-[[2-(3,4-dimethoxphenyl)ethyl]amino]-3-(3-methylphenoxy)-2-propanol hydrochloride (bevantolol, NC-1400) as a β1-selective adrenoceptor blocker With ɑ1-adrenoceptor Blocking Activity. Gen. Pharmacol. 18(1), 87-90 (1987).

    4. Takita, M., Kigoshi, S., and Muramatsu, I. Effects of bevantolol HCl on immobilization stress-induced hypertension and central β-adrenoceptors in rats. Pharmacol. Biochem. Behav. 45, 623-627 (1993).