Rat uterus and guinea pig atrium were used to measure in vitro β1- and β2-adrenoceptor antagonistic interactions, respectively. The pA2 levels are 8.3 and 8.4 correspondingly[2]. With an IC50 value of 6.9 μM, metyrolol considerably decreases the lipid peroxidation in rat brain homogenate produced by iron and ascorbic acid. In rat brain homogenate, metyrolol also showed a concentration-dependent inhibition of sodium nitroprusside-stimulated lipid peroxidation, with an IC50 value of 25.1 μM [3].

Postnatal day 35 (P35) rd10 mice subcutaneously injected with 40 mg/kg metyrolol daily showed decreased markers of nitrosative stress, a decrease in TUNEL-positive cells, an increase in the thickness of the outer nuclear layer, and rhodopsin staining. rising. In the retina of rd10 mice treated with metyranol, 3-nitrotyrosine staining decreased at P50 and increased immunostaining for cone inhibitory protein, a marker of cone photoreceptors, at the highest stimulation intensity. Under scotopic and photopic conditions, the amplitude of the b-wave increased significantly. Compared to rd10 mice injected with vehicle, metyrolol-treated mice exhibited a significantly higher cone density at P65 [1].

Effects During Pregnancy and Lactation
◉ Overview of Use During Lactation
Based on its physicochemical properties and ocular route of administration, metenolol eye drops are not expected to have any adverse effects on breastfed infants. Some guidelines indicate that the gel formulation is preferred over the solution formulation. To significantly reduce the amount of medication that enters breast milk after instillation, press your finger against the tear duct near the corner of your eye for at least 1 minute, then blot away any excess medication with absorbent paper. ◉ Effects on Breastfed Infants
As of the revision date, no published information was found regarding metenolol. A study of breastfeeding mothers taking beta-blockers found a numerically increased number of adverse events, but this was not statistically significant. Although the infants' ages were matched to those in the control group, the ages of the affected infants were not specified. None of the mothers were taking metenolol.
◉ Effects on Lactation and Breast Milk
As of the revision date, no published information was found regarding the effects of beta-blockers or metenolol during normal lactation. A study of six patients with hyperprolactinemia and galactorrhea found no change in serum prolactin levels after beta-adrenergic blockade with propranolol.

[1]. 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]. A study on the ocular and extraocular pharmacology of metipranolol. Graefes Arch Clin Exp Ophthalmol. 1985;222(3):123-7.

[3]. 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.

Metipranolol is a 3-(propyl-2-ylamino)propane-1,2-diol, in which the hydrogen atom on the primary hydroxyl group is replaced by 4-acetoxy-2,3,5-trimethylphenoxy. It is a non-selective beta-blocker used to lower intraocular pressure and treat open-angle glaucoma. It has the effects of a beta-adrenergic antagonist, antiarrhythmia agent, antihypertensive agent, and antiglaucoma agent. It is a propanolamine compound, belonging to the acetate, aromatic ether, and secondary amino compounds. It is a beta-adrenergic antagonist, effective against both β1 and β2 receptors. It is used as an antiarrhythmia agent, antihypertensive agent, and antiglaucoma agent. Metipranolol is a beta-adrenergic blocker. The mechanism of action of metipranolol is as a beta-adrenergic receptor antagonist. It is a beta-adrenergic receptor antagonist, effective against both β1 and β2 receptors. It is used as an antiarrhythmic, antihypertensive, and antiglaucoma drug. Indications: It is indicated for the treatment of elevated intraocular pressure, including ocular hypertension and open-angle glaucoma. Mechanism of Action: Although metenolol is known to bind to β1 and β2 adrenergic receptors, its mechanism of action is unclear. It has no significant intrinsic sympathomimetic activity, only weak local anesthetic (membrane stabilization) and myocardial depressant effects. Ophthalmic β-adrenergic blockers appear to reduce aqueous humor production, as confirmed by tonometry and fluorometry. A slight increase in aqueous humor outflow may be one of its mechanisms of action. Pharmacodynamics: Metenolol is a β1 and β2 (non-selective) adrenergic receptor blocker with no significant intrinsic sympathomimetic activity, direct myocardial depressant effect, or local anesthetic (membrane stabilizing) effect. Metenolol is indicated for the treatment of elevated intraocular pressure in patients with ocular hypertension or open-angle glaucoma. When applied topically to the eye, metenolol can lower elevated intraocular pressure as well as normal intraocular pressure, regardless of whether glaucoma is present. Elevated intraocular pressure is a major risk factor in the pathogenesis of glaucomatous visual field defects and optic nerve damage. Unlike cholinergic drugs known to cause pupillary constriction, metenolol lowers intraocular pressure with little effect on pupil size or accommodation.

C17H27NO4

309.40058

309.194

22664-55-7

31477

White to off-white solid powder

1.068g/cm3

458.7ºC at 760mmHg

105-107 °C
105 - 107 °C

231.2ºC

3.29E-09mmHg at 25°C

1.512

2.665

2

5

8

22

348

0

BQIPXWYNLPYNHW-UHFFFAOYSA-N

InChI=1S/C17H27NO4/c1-10(2)18-8-15(20)9-21-16-7-11(3)17(22-14(6)19)13(5)12(16)4/h7,10,15,18,20H,8-9H2,1-6H3

[4-[2-hydroxy-3-(propan-2-ylamino)propoxy]-2,3,6-trimethylphenyl] acetate

2934.99.9001

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Note: This product requires protection from light (avoid light exposure) during transportation and storage.

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

DMSO : ~250 mg/mL (~808.02 mM)

Solubility in Formulation 1: ≥ 2.08 mg/mL (6.72 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution.

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Solubility in Formulation 2: ≥ 2.08 mg/mL (6.72 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.

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Solubility in Formulation 3: ≥ 2.08 mg/mL (6.72 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.

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 (Please use freshly prepared in vivo formulations for optimal results.)