Bevantolol hydrochloride
(Synonyms: 贝凡洛尔盐酸盐) 目录号 : GC39546
A β1-AR antagonist
Cas No.:42864-78-8
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
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
1.Takita, M., Kigoshi, S., and Muramatsu, I.Selectivity of bevantolol hydrochloride towards ɑ and β-adrenoceptor subtypes in rat cerebral cortexJpn. J. Pharmacol.58(2)193-196(1992) 2.T., O., Kobayashi, T., Nishioka, K., et al.Ca2+-antagonistic action of bevantolol on hypothalamic neurons in vitro: Its comparison with those of other β-adrenoceptor antagonists, a local anesthetic and a Ca2+-antagonistBrain 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 ActivityGen. 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 ratsPharmacol. Biochem. Behav.45623-627(1993)
| Cas No. | 42864-78-8 | SDF | |
| 别名 | 贝凡洛尔盐酸盐 | ||
| Canonical SMILES | OC(CNCCC1=CC=C(C(OC)=C1)OC)COC2=CC=CC(C)=C2.[H]Cl | ||
| 分子式 | C20H28ClNO4 | 分子量 | 381.89 |
| 溶解度 | DMSO: 62.5 mg/mL (163.66 mM) | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.6186 mL | 13.0928 mL | 26.1856 mL |
| 5 mM | 0.5237 mL | 2.6186 mL | 5.2371 mL |
| 10 mM | 0.2619 mL | 1.3093 mL | 2.6186 mL |
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动物数量 | 只 |
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Bevantolol hydrochloride--preclinical pharmacologic profile
Angiology 1986 Mar;37(3 Pt 2):254-62.PMID:2871786DOI:10.1177/000331978603700319.
Bevantolol hydrochloride, a beta adrenoceptor antagonist, can be categorized using conventional schemes as being cardioselective, devoid of intrinsic sympathomimetic activity and having weak membrane-stabilizing and local anesthetic properties. The cardioselectivity of bevantolol was conferred by the incorporation of a 3,4-dimethoxyphenyl moiety into the terminal amino portion of the molecule. This portion of the molecule also appears to account for bevantolol's in vitro binding affinity at alpha-adrenoceptor sites; the in vivo significance of which remains unclear. In the various cardiovascular disease-state models, bevantolol's profile differed from that of propranolol, i.e., there was no initial pressor response in spontaneously hypertensive or renal hypertensive rats. In a myocardial ischemia model, bevantolol, unlike propranolol, increased contractile function in the ischemic myocardium. A ring hydroxylated urinary metabolite, which occurred only in trace amounts in human urine, had an interesting profile when studied in animals at pharmacologic doses. It ranked high in cardioselectivity (like bevantolol), but unlike bevantolol showed significant intrinsic beta sympathomimetic activity. The clinical significance of this metabolite, if any, remains to be established. Collectively the preclinical profile of bevantolol showed it to have an interesting profile for a beta adrenoceptor antagonist in a variety of pharmacologic test systems.
Selectivity of Bevantolol hydrochloride, a beta 1-adrenoceptor antagonist, in asthmatic patients
Pharmacotherapy 1984 Jul-Aug;4(4):205-10.PMID:6148733DOI:10.1002/j.1875-9114.1984.tb03359.x.
Bevantolol hydrochloride, a new beta-adrenoceptor antagonist, has been shown to be cardioselective in animals. To evaluate its selectivity in humans, a double-blind, crossover study was conducted in 8 asthmatics. Following a single oral dose of placebo, bevantolol 75 or 150 mg or propranolol hydrochloride 40 mg, forced expiratory volume in 1 second (FEV1), heart rate, blood pressure and skeletal muscle tremor were measured before and after 4 increasing intravenous doses of terbutaline sulfate to establish terbutaline dose-response curves. The FEV1 decreased after all active treatments. During terbutaline infusions there was an increase in FEV1 after both bevantolol doses and placebo. The terbutaline dose-response curve after bevantolol shifted to the right, however. After propranolol, there was no increase in FEV1 during terbutaline stimulation. Heart rate and skeletal muscle tremor showed a similar pattern during the experiment. In dosages that have previously been shown to produce at least the same degree of blockade of exercise-induced tachycardia, bevantolol has less influence on terbutaline-induced bronchodilation, heart rate increase and skeletal muscle tremor than did propranolol. Thus bevantolol has relative beta 1-adrenoceptor antagonist selectivity. Drawing upon the results of a previous study in the same patients, we believe bevantolol, atenolol and metoprolol have similar beta 1-selectivity.
Pharmacology of Bevantolol hydrochloride
Am J Cardiol 1986 Nov 26;58(12):3E-7E.PMID:2878599DOI:10.1016/0002-9149(86)90590-4.
Bevantolol is a cardioselective, beta-adrenoreceptor antagonist, devoid of intrinsic beta sympathomimetic activity and with weak membrane-stabilizing and local anesthetic properties. The 3,4-dimethoxyphenylethylamino moiety, substituted on the side chain amine function, confers cardioselectivity, which has been confirmed by a number of experiments. In vitro, bevantolol demonstrated greater antagonism of atrial than tracheal responses to isoproterenol. In vivo, bevantolol preferentially inhibited isoproterenol-induced tachycardias in conscious and anesthetized dogs, compared with the nonselective agent propranolol. Conversely, its effect on blood pressure after isoproterenol was minimal compared with propranolol, reflecting its muted effect on beta 2 peripheral receptors. A functional difference between bevantolol and propranolol was demonstrated in histamine-challenged guinea pigs. Bevantolol had little effect on the antiasthmatic effect of isoproterenol, whereas propranolol blocked it totally. Bevantolol's lack of intrinsic sympathomimetic activity was demonstrated in normal and reserpinized dogs, where it was devoid of intrinsic sympathomimetic activity at doses up to 10 mg/kg. Similarly, intravenous doses of 10 mg/kg had to be administered before direct myocardial depression occurred in the reserpinized animals. Metabolite 3, which is excreted in trace amounts in human urine, demonstrates intrinsic sympathomimetic activity when administered in pharmacologic doses to dogs; however, any clinical relevance remains to be established. Several laboratories have demonstrated that bevantolol interacts at alpha-adrenergic sites. These data require further investigation. The dose-related antihypertensive effect of bevantolol has been demonstrated in spontaneously hypertensive and 2 kidney, 1 clip renal hypertensive rats. Animal experiments also suggest that bevantolol may be useful in angina: It caused a favorable redistribution of blood flow in dogs in which the left circumflex artery had been stenosed.(ABSTRACT TRUNCATED AT 250 WORDS)
A proof-of-concept study with SOM3355 (Bevantolol hydrochloride) for reducing chorea in Huntington's disease
Br J Clin Pharmacol 2022 Dec 9.PMID:36494329DOI:10.1111/bcp.15635.
Aims: The study's aim is to investigate the efficacy and safety of SOM3355 (Bevantolol hydrochloride), a β1 -adrenoreceptor antagonist with recently identified vesicular monoamine transporter type 2 inhibitory properties, as a repositioned treatment to reduce chorea in Huntington's disease (HD). Methods: A randomized, placebo-controlled proof-of-concept study was performed in 32 HD patients allocated to 2 arms of 4 sequential 6-week periods each. Patients received placebo and SOM3355 at 100 and 200 mg twice daily in a crossover design. The primary endpoint was improvement by at least 2 points in the total maximal chorea score in any active drug period compared with the placebo period. Results: The primary endpoint was met in 57.1% of the patients. Improvements ≥3, ≥4, ≥5 and ≥6 points vs. placebo treatment were observed in 28.6, 25.0, 17.9 and 10.7% of the patients, respectively. A mixed-model analysis found a significant improvement in the total maximal chorea score of -1.14 (95% confidence interval, -2.11 to -0.16; P = .0224) with 200 mg twice daily SOM3355 treatment compared with placebo treatment. These results were paralleled by Clinical and Patient Global Impression of Change ratings (secondary endpoints). An elevation in plasma prolactin levels by 1.7-1.9-fold was recorded (P < .005), probably reflecting the effect on the dopamine pathway, consistent with vesicular monoamine transporter type 2 inhibition. The most frequent adverse events during SOM3355 administration were mild to moderate. Conclusion: Within the limits of this study, the results suggest that SOM3355 reduces chorea in patients with HD and is well-tolerated. Larger studies are necessary to confirm its therapeutic utility as an antichoreic drug. EudraCT number: 2018-000203-16 and ClinicalTrials.gov Identifier: NCT03575676.
Selectivity of Bevantolol hydrochloride towards alpha- and beta-adrenoceptor subtypes in rat cerebral cortex
Jpn J Pharmacol 1992 Feb;58(2):193-6.PMID:1354761DOI:10.1254/jjp.58.193.
Selectivity of Bevantolol hydrochloride (NC-1400) towards alpha- and beta-adrenoceptor subtypes of rat cerebral cortex was examined in binding experiments and compared with propranolol. Bevantolol biphasically displaced the 3H-dihydroalprenolol binding. The affinity of bevantolol to beta 1-adrenoceptor was equal to that of propranolol. Bevantolol displaced 3H-prazosin binding monophasically but not 3H-p-aminoclonidine binding. These results suggest that bevantolol is a beta 1-adrenoceptor antagonist with a relatively high affinity to alpha 1-adrenoceptor subtypes.