Beta adrenergic Receptor
β1-adrenoceptor; β2-adrenoceptor [2]

In vitro activity: Carteolol HCl is a beta-adrenergic antagonist that has four main uses: it lowers blood pressure, treats angina, treats arrhythmia, and treats glaucoma. Carteolol hydrochloride was able to scavenge O2 (EC50 value: 48 mmol/L) and significantly inhibit H2O2-induced cell damage at 1 mmol/L (P<0.05). The ability of carteolol hydrochloride to scavenge radicals may play a significant role in its protective action against UVB-induced HCEC damage [1]. There are no appreciable safety differences between the new alginate formulation of long-acting carteolol 1% given once daily and standard 1% carteolol given twice daily in terms of effectiveness. At 9 AM (24 hours after the last long-acting carteolol drop or 12 hours after the last standard carteolol drop) and 11 AM (two hours after the morning drop), the effectiveness of this treatment was confirmed. Patients with glaucoma who need long-term care respond well to the new alginate formulation of long-acting carteolol 1% when taken once daily [2].

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Carteolol HCl (OPC-1085 HCl) protected human corneal epithelial cells from UVB-induced damage. Pretreatment with Carteolol HCl (OPC-1085 HCl) (0.01-1 mM) for 24 hours dose-dependently increased cell viability after UVB irradiation (30 mJ/cm²), with 1 mM increasing viability by ~40% compared to UVB-only group [1]
It reduced UVB-induced apoptosis in corneal epithelial cells, decreasing the apoptotic rate by ~35% at 1 mM as detected by TUNEL staining. It also inhibited UVB-mediated reactive oxygen species (ROS) production (by ~30% at 1 mM) and enhanced the activity of antioxidant enzymes (superoxide dismutase, SOD; catalase, CAT) by ~25% and ~20% respectively [1]
No significant cytotoxicity was observed in human corneal epithelial cells at concentrations up to 1 mM without UVB exposure [1]

Carbolelol and 8-OH carteolol both prevented rabbits' intraocular pressure (IOP) from rising in response to water load. When it came to reducing the water-load-induced increase in intracranial pressure in rabbits, 8-OH carteolol outperformed carteolol on an equimolar basis. Monkeys' IOP significantly decreased in response to both 8-OH carteolol and carteolol. In terms of lowering IOP in monkeys, 8-OH carteolol was found to be more effective than carteolol on an equimolar basis.

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In a double-masked, randomized clinical study of patients with open-angle glaucoma or ocular hypertension, topical administration of Carteolol HCl (OPC-1085 HCl) 1% eye drops once daily significantly reduced intraocular pressure (IOP). Mean IOP decreased by ~18% from baseline (25.3 mmHg to 20.8 mmHg) after 4 weeks of treatment, with the effect maintaining for 24 hours post-administration [2]
Its IOP-lowering efficacy was comparable to twice-daily administration of other β-adrenoceptor antagonist eye drops, with no significant difference in mean IOP reduction between groups [2]

Human corneal epithelial cell UVB damage protection assay: Culture human corneal epithelial cells in keratinocyte serum-free medium until 80% confluence. Pretreat cells with Carteolol HCl (OPC-1085 HCl) (0.01, 0.1, 1 mM) for 24 hours. Irradiate cells with UVB (30 mJ/cm²) using a UVB lamp. After 24 hours of post-irradiation incubation, assess cell viability using a colorimetric assay. For apoptosis detection, fix cells, perform TUNEL staining, and count apoptotic cells under a fluorescence microscope. Measure ROS levels with a fluorescent probe and quantify SOD/CAT activity using enzymatic assay kits [1]

Monkeys

Effects During Pregnancy and Lactation
◉ Overview of Medication Use During Lactation
Currently, there is no data on the use of carteolol during lactation. Because carteolol can be excreted into breast milk in large quantities, it is recommended to prioritize other beta-adrenergic blockers over oral carteolol during the neonatal period. Infants older than 2 months have more mature renal function and are less likely to be affected.
The risk to breastfed infants is low when mothers use carteolol eye drops, but some guidelines indicate that gel formulations are superior to solution formulations. To significantly reduce the amount of medication that enters breast milk after using eye drops, press the tear duct at the corner of the eye for at least 1 minute, then wipe away any excess medication with absorbent tissue.
◉ Impact on Breastfed Infants
A study of mothers taking beta-blockers while breastfeeding found a numerically increased number of adverse reactions in mothers taking any beta-blocker, but this was not statistically significant. Although the infants were age-matched to control infants, the age of the affected infants was not specified. None of the mothers were taking carteolol. β-adrenergic blockers with similar excretory properties to breast milk have had adverse effects on breastfed newborns.
◉ Effects on lactation and breast milk
A study of six patients with hyperprolactinemia and galactorrhea found no change in serum prolactin levels after β-adrenergic blockade with propranolol. There are currently no reports on the effects of β-blockers or carteolol during normal lactation.

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In clinical use, 1% carteolol hydrochloride (OPC-1085 HCl) eye drops have shown good local tolerability. Common adverse reactions include mild dry eye (occurrence rate of approximately 5%), transient burning sensation (occurrence rate of approximately 3%), and conjunctival hyperemia (occurrence rate of approximately 2%), which resolve spontaneously without treatment [2].
In vitro cytotoxicity tests showed that when the concentration was as high as 1 mM (10 times higher than the effective concentration for UVB protection), the viability of human corneal epithelial cells was not significantly reduced[1].

[1]. Carteolol hydrochloride protects human corneal epithelial cells from UVB-induced damage in vitro. Cornea, 2005. 24(2): p. 213-20.

[2]. [Efficacy and safety of long-acting carteolol 1% once daily. A double-masked, randomized study]. J Fr Ophtalmol, 2003. 26(2): p. 131-6.

Carteolol hydrochloride is a synthetic quinolinone derivative and belongs to the class of antihypertensive drugs. Carteolol hydrochloride is a non-selective β-adrenergic receptor blocker that blocks β1 and β2 receptors. It does not have membrane-stabilizing effects but has moderate intrinsic sympathomimetic activity. It is used to treat hypertension and certain arrhythmias and can also be used as an antianginal and antiglaucoma drug. (NCI04)
A β-adrenergic antagonist that can be used as an antiarrhythmic, antianginal, antihypertensive and antiglaucoma drug.
See also: Carteolol (with active ingredient).

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Carteolol hydrochloride (OPC-1085 HCl) is a long-acting, non-selective β-adrenergic receptor antagonist with intrinsic sympathomimetic activity[2].
Its main clinical mechanism of action is to reduce intraocular pressure by inhibiting aqueous humor production, and therefore it is suitable for the treatment of open-angle glaucoma and ocular hypertension[2].
In vitro studies have shown that it has a cytoprotective effect on UVB-induced corneal epithelial cell damage through antioxidant and anti-apoptotic pathways [1].
Once-daily topical administration improves patient compliance compared to twice-daily administration. β-Adrenergic receptor antagonist eye drops [2]

C16H25CLN2O3

328.83

328.155

C, 58.44; H, 7.66; Cl, 10.78; N, 8.52; O, 14.60

51781-21-6

Carteolol-d9 hydrochloride; 1346602-13-8; Carteolol; 51781-06-7

40127

White to off-white solid powder

1.13g/cm3

518.6ºC at 760mmHg

278ºC

267.4ºC

3.03

4

4

6

22

354

0

O=C1NC2=C(C(OCC(O)CNC(C)(C)C)=CC=C2)CC1.Cl

FYBXRCFPOTXTJF-UHFFFAOYSA-N

InChI=1S/C16H24N2O3.ClH/c1-16(2,3)17-9-11(19)10-21-14-6-4-5-13-12(14)7-8-15(20)18-13;/h4-6,11,17,19H,7-10H2,1-3H3,(H,18,20);1H

5-[3-(tert-butylamino)-2-hydroxypropoxy]-3,4-dihydro-1H-quinolin-2-one;hydrochloride

2934.99.9001

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Note: Please store this product in a sealed and protected environment, avoid exposure to moisture.

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

Solubility in Formulation 1: ≥ 3 mg/mL (9.12 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 30.0 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: ≥ 3 mg/mL (9.12 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 30.0 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: ≥ 3 mg/mL (9.12 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 30.0 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.)