Betaxolol HCl

Synonyms: SL 75212 HCl

Betaxolol (SL 75212) is a β1 adrenergic receptor blocker with IC50 of 6 μM.

Betaxolol HCl Chemical Structure

Betaxolol HCl Chemical Structure

CAS No. 63659-19-8

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Biological Activity

Description Betaxolol (SL 75212) is a β1 adrenergic receptor blocker with IC50 of 6 μM.
Targets
β1-adrenergic receptor [1]
6 μM
In vitro
In vitro Betaxolol is able to protect retinal neurones. [2] Betaxolol attenuates the NMDA-induced influx of 45Ca2+ while β-adrenoreceptor agonists are ineffective. [3] The glutamate-induced release of LDH is almost completely prevented when betaxolol (10 μM) is included. [4] Betaxolol (100 μM) is very effective in preventing the hypoxia-induced release of LDH from cortical cultures. [5]
Cell Research Cell lines Dissociated rat cortical cells
Concentrations 100 μM
Incubation Time 4 hours
Method Dissociated cortical cells from 16–18-day-old fetal rats are grown, in 35 mm dishes, in DMEM supplemented with L-glutamine (4 mM), glucose (6 g/L), penicillin (100 U/mL), streptomycin (100 μg/mL) and 10% hormonal supplemented medium consisting of transferrin (1 mg/mL), insulin (250 μg/mL) putrescine (600 μM), sodium selenite (0.3 μM), progesterone (0.2 μM) and estradiol (0.1 pM) for 7 days in an atmosphere of 5% CO2/95% O2 at 37 °C. The cultures are then transferred to a culture medium which lacks the hormonal supplemented medium. L-glutamate is added to the medium and incubated for a further 4 hours under normoxic conditions. Betaxolol are added to the cultures at the same time as L-glutamate. In other experiments the cultures are subjected to anoxic conditions, 95% N2/5% CO2, for 5 hours at 37 °C. Betaxolol is added prior to anoxia. Reoxygenation is then achieved by replacing the cells in normoxic conditions (95% O2/5% CO2) for 3 hours. Cellular injury is assessed by measuring lactate dehydrogenase (LDH) release into the cell culture supernatant after hypoxia/reoxygenation or glutamate exposure. LDH activity is assayed spectrophotometrically by following NADH metabolism for 2 minutes at 340 nm.
In Vivo
In vivo When Betaxolol is injected i.p. into the rats before ischaemia and on the days of reperfusion the changes to the calretinin and ChAT immunoreactivities are reduced and the reduction of the b-wave is prevented. Inclusion of betaxolol partially prevents the changes caused by NMDA and lack of oxygen/glucose. [5]
Animal Research Animal Models Rat wiht ischaemia
Dosages 2.5 mg/kg
Administration Administered via i.p.

Chemical Information & Solubility

Molecular Weight 343.89 Formula

C18H29NO3.HCl

CAS No. 63659-19-8 SDF Download Betaxolol HCl SDF
Smiles CC(C)NCC(COC1=CC=C(C=C1)CCOCC2CC2)O.Cl
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 69 mg/mL ( (200.64 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : 69 mg/mL

Ethanol : 69 mg/mL


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In vivo
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