الصفحة الرئيسية>>Signaling Pathways>> GPCR/G protein>> Adrenergic Receptor>>(S)-(-)-Atenolol

(S)-(-)-Atenolol

رقم الكتالوجGC12463

(S)-(-)-Atenolol is a potent β-adrenergic receptor blocker. (S)-(-)-Atenolol is the S(-) enantiomer of Atenolol, while the R(+) enantiomer of Atenolol has almost no β-receptor blocker activity.

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(S)-(-)-Atenolol التركيب الكيميائي

Cas No.: 93379-54-5

الحجم السعر المخزون الكميّة
1mg
54٫00
متوفر
5mg
130٫00
متوفر
10mg
190٫00
متوفر
25mg
322٫00
متوفر
50mg
472٫00
متوفر
100mg
688٫00
متوفر

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Sample solution is provided at 25 µL, 10mM.

Description of (S)-(-)-Atenolol

(S)-(-)-Atenolol is a potent β-adrenergic receptor blocker[1]. (S)-(-)-Atenolol is the S(-) enantiomer of Atenolol, while the R(+) enantiomer of Atenolol has almost no β-receptor blocker activity[2, 3]. (S)-(-)-Atenolol is mainly used to treat hypertension and heart-related chest pain[4].

In vitro, (S)-(-)-Atenolol (0-350μM) treated vascular smooth muscle A7r5 cells for 24h inhibited cell viability in a dose-dependent manner and reduced the levels of calmodulin and annexin A6 in the cells[5]. (S)-(-)-Atenolol (200, 400, 600μM) treated MCF7 cells for 72h significantly inhibited cell migration and reduced the percentage of wound healing (WH) of the cells[6].

In vivo, (S)-(-)-Atenolol (90mg/kg/day) was orally administered to spontaneously hypertensive rats for 8 weeks and was less effective in reducing carotid systolic blood pressure than Carvedilol (30mg/kg/day) or Nebivolol (30mg/kg/day)[7].

References:
[1] Mehvar R, Brocks D R. Stereospecific pharmacokinetics and pharmacodynamics of beta-adrenergic blockers in humans[J]. 2001.
[2] Seebauer C T, Graus M S, Huang L, et al. Non–beta blocker enantiomers of propranolol and atenolol inhibit vasculogenesis in infantile hemangioma[J]. The Journal of Clinical Investigation, 2022, 132(3). 
[3] Stoschitzky K, Egginger G, Zernig G, et al. Stereoselective features of (R)‐and (S)‐atenolol: Clinical pharmacological, pharmacokinetic, and radioligand binding studies[J]. Chirality, 1993, 5(1): 15-19.
[4] Heel R C, Brogden R N, Speight T M, et al. Atenolol: a review of its pharmacological properties and therapeutic efficacy in angina pectoris and hypertension[J]. Drugs, 1979, 17: 425-460.
[5] Sui J, Zhang J, Tan T L, et al. Comparative proteomics analysis of vascular smooth muscle cells incubated with S-and R-enantiomers of atenolol using iTRAQ-coupled two-dimensional LC-MS/MS[J]. Molecular & Cellular Proteomics, 2008, 7(6): 1007-1018.
[6] İşeri Ö D, Sahin F I, Terzi Y K, et al. beta-Adrenoreceptor antagonists reduce cancer cell proliferation, invasion, and migration[J]. Pharmaceutical biology, 2014, 52(11): 1374-1381.
[7] Del Mauro J S, Prince P D, Allo M A, et al. Effects of third-generation β-blockers, atenolol or amlodipine on blood pressure variability and target organ damage in spontaneously hypertensive rats[J]. Journal of Hypertension, 2020, 38(3): 536-545.

Protocol of (S)-(-)-Atenolol

Cell experiment [1]:

Cell lines

A7r5 cells

Preparation Method

After reaching 80% confluence the cells were incubated with 0-350μM (R)-(+)-Atenolol and (S)-(-)-Atenolol for 24h, in the absence of serum. The viability was examined by the MTT assay.

Reaction Conditions

0-350μM; 24h

Applications

The two enantiomers of Atenolol was toxic to the cells with a drastic decrease in cell viability for any concentration higher than 50μM. The (R)-(+)-Atenolol was somewhat less toxic than the (S)-(-)-Atenolol.

Animal experiment [2]:

Animal models

Spontaneously hypertensive rats (SHR)

Preparation Method

SHR rats received Carvedilol 30mg/kg, Nebivolol 30mg/kg, (S)-(-)-Atenolol 90mg/kg, Amlodipine 10mg/kg or vehicle by oral gavage once a day for 8 weeks. WKY rats administered with vehicle were used as normotensive control group.

Dosage form

90mg/kg/day for 8 weeks; p.o.

Applications

Chronic treatment with Carvedilol or Nebivolol attenuates carotid BP and short-term BPV, and reduces target organ damage in SHR to a greater extent than (S)-(-)-Atenolol.

References:
[1]Sui J, Zhang J, Tan T L, et al. Comparative proteomics analysis of vascular smooth muscle cells incubated with S-and R-enantiomers of atenolol using iTRAQ-coupled two-dimensional LC-MS/MS[J]. Molecular & Cellular Proteomics, 2008, 7(6): 1007-1018.
[2]Del Mauro J S, Prince P D, Allo M A, et al. Effects of third-generation ?-blockers, atenolol or amlodipine on blood pressure variability and target organ damage in spontaneously hypertensive rats[J]. Journal of Hypertension, 2020, 38(3): 536-545.

Chemical Properties of (S)-(-)-Atenolol

Cas No. 93379-54-5 SDF
Chemical Name (S)-2-(4-(2-hydroxy-3-(isopropylamino)propoxy)phenyl)acetamide
Canonical SMILES O[C@H](COC1=CC=C(CC(N)=O)C=C1)CNC(C)C
Formula C14H22N2O3 M.Wt 266.34
الذوبان Soluble to 25 mM in sterile water Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table of (S)-(-)-Atenolol

Prepare stock solution
1 mg 5 mg 10 mg
1 mM 3.7546 mL 18.773 mL 37.546 mL
5 mM 0.7509 mL 3.7546 mL 7.5092 mL
10 mM 0.3755 mL 1.8773 mL 3.7546 mL
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