Metipranolol

Metipranolol is a nonselective and orally active β-adrenergic receptor antagonist. Metipranolol can be used for hypertension and glaucoma research[1][2].

Research Areas >> Cardiovascular Disease

Signaling Pathways >> GPCR/G Protein >> Adrenergic Receptor

β1 adrenoceptor:8.3 (pA2)

β2 adrenoceptor:8.4 (pA2)

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[2]. 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[3].

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[1].

[1]. Yogita Kanan, et al. Metipranolol promotes structure and function of retinal photoreceptors in the rd10 mouse model of human retinitis pigmentosa. J Neurochem. 2019 Jan;148(2):307-318.

[2]. M F Sugrue, et al. A study on the ocular and extraocular pharmacology of metipranolol. Graefes Arch Clin Exp Ophthalmol. 1985;222(3):123-7.

[3]. José Melena, et al. Metipranolol attenuates lipid peroxidation in rat brain: a comparative study with other antiglaucoma drugs. Graefes Arch Clin Exp Ophthalmol. 2003 Oct;241(10):827-33.

MOLECULAR FORMULA :

C17-H27-N-O4

MOLECULAR WEIGHT :

309.45

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :

LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :

Subcutaneous

SPECIES OBSERVED :

Rodent - mouse

DOSE/DURATION :

250 mg/kg

TOXIC EFFECTS :

Details of toxic effects not reported other than lethal dose value

REFERENCE :

CCCCAK Collection of Czechoslovak Chemical Communications. (Academic Press Inc. Ltd., 24-28 Oval Rd., London NW1 7DX, UK) V.1- 1929- Volume(issue)/page/year: 50,2289,1985

TYPE OF TEST :

LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :

Intravenous

SPECIES OBSERVED :

Rodent - mouse

DOSE/DURATION :

31 mg/kg

TOXIC EFFECTS :

Details of toxic effects not reported other than lethal dose value

REFERENCE :

ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 27,1022,1977