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Metipranolol

SKU: orb1218388

Description

Metipranolol is a β-adrenergic receptor antagonist that is given orally for the treatment of hypertension and also applied topically to the cornea for treating glaucoma.(In Vivo):At postnatal day 35 (P35), rd10 mice given daily subcutaneous injections of 40 mg/kg of Metipranolol has reduction in markers of nitrosative stress, fewer TUNEL-positive cells, increased outer nuclear layer thickness, and substantially more staining for rhodopsin. At P50, Metipranolol-treated rd10 mice has decreased 3-nitrotyrosine staining in the retina, increased immunostaining for cone arrestin, a marker for cone photoreceptors, and significantly higher scotopic and photopic b-wave amplitudes at the highest stimulus intensity. At P65, cone density is significantly higher in Metipranolol-treated versus vehicle-injected rd10 mice.

Research Area

Pharmacology & Drug Discovery

Images & Validation

Key Properties

CAS Number22664-55-7
MW309.4
Purity>98% (HPLC)
FormulaC17H27NO4
SMILESCC1=CC(=C(C(=C1OC(=O)C)C)C)OCC(CNC(C)C)O
TargetAdenosine Receptor
SolubilityDMSO:10 mM

Bioactivity

In Vivo
At postnatal day 35 (P35), rd10 mice given daily subcutaneous injections of 40 mg/kg of Metipranolol has reduction in markers of nitrosative stress, fewer TUNEL-positive cells, increased outer nuclear layer thickness, and substantially more staining for rhodopsin. At P50, Metipranolol-treated rd10 mice has decreased 3-nitrotyrosine staining in the retina, increased immunostaining for cone arrestin, a marker for cone photoreceptors, and significantly higher scotopic and photopic b-wave amplitudes at the highest stimulus intensity. At P65, cone density is significantly higher in Metipranolol-treated versus vehicle-injected rd10 mice.
In Vitro
In vitro β1- and β2-adrenoceptor antagonism is evaluated using the guinea pig atrium and the rat uterus, respectively. The respective pA2 values are 8.3 and 8.4. Metipranolol significantly reduces iron/ascorbate-induced lipid peroxidation in rat brain homogenates with an IC50 value of 6.9 μM. Metipranolol also concentration-dependently inhibits sodium nitroprusside-stimulated lipid peroxidation in rat brain homogenates, displaying an IC50 value of 25.1 μM.

Storage & Handling

StorageStorage temperature: -20°C. Stability: ≥ 2 years
Expiration Date12 months from date of receipt.
DisclaimerFor research use only

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Protocol Information

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