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Carteolol hydrochloride

CAS No.
51781-21-6
Chemical Name:
Carteolol hydrochloride
Synonyms
endak;oc1085;Teoptic;Tenalet;Cartrol;Carteol;Cartelo;mikelan;opc1085;Cartelol
CBNumber:
CB6335371
Molecular Formula:
C16H25ClN2O3
Molecular Weight:
328.83
MDL Number:
MFCD00941499
MOL File:
51781-21-6.mol
Last updated:2024-03-08 11:25:09

Carteolol hydrochloride Properties

Melting point 278°C
storage temp. Refrigerator
solubility Soluble in water, sparingly soluble in methanol, slightly soluble in ethanol 96 per cent, practically insoluble in methylene chloride.
color White to Off-White
Merck 14,1866
FDA UNII 4797W6I0T4

SAFETY

Risk and Safety Statements

Symbol(GHS)  GHS hazard pictograms
GHS07
Signal word  Warning
Hazard statements  H302
Precautionary statements  P301+P312+P330
RTECS  VC8282000
HS Code  2933790002
Toxicity LD50 in male mice, rats (mg/kg): 810, 1380 orally; 54.5, 158 i.v.; 380, 400 i.p. (Lang)
NFPA 704
0
2 0

Carteolol hydrochloride price More Price(30)

Manufacturer Product number Product description CAS number Packaging Price Updated Buy
Sigma-Aldrich Y0000193 Carteolol for system suitability European Pharmacopoeia (EP) Reference Standard 51781-21-6 y0000193 $150 2024-03-01 Buy
Sigma-Aldrich BP567 Carteolol hydrochloride British Pharmacopoeia (BP) Reference Standard 51781-21-6 100MG $208 2024-03-01 Buy
Sigma-Aldrich 1096757 Carteolol for system suitability 51781-21-6 200mg $416 2024-03-01 Buy
Cayman Chemical 23758 Carteolol (hydrochloride) ≥98% 51781-21-6 25mg $68 2024-03-01 Buy
Cayman Chemical 23758 Carteolol (hydrochloride) ≥98% 51781-21-6 50mg $121 2024-03-01 Buy
Product number Packaging Price Buy
Y0000193 y0000193 $150 Buy
BP567 100MG $208 Buy
1096757 200mg $416 Buy
23758 25mg $68 Buy
23758 50mg $121 Buy

Carteolol hydrochloride Chemical Properties,Uses,Production

Chemical Properties

Crystalline Solid

Uses

β-Adrenergic blocker. Antihypertensive; antianginal; antiarrhythmic; antiglaucoma.

brand name

Cartrol (Abbott); Ocupress (Novartis).

Biological Activity

beta-adrenergic antagonist are an important class of drugs for the treatment of various heart diseases, such as high blood pressure, insufficiency of blood flow to the heart muscle, irregular heart beat, thickened heart muscle, and decreased ability of the heart to empty or fill normally. β-blockers can also be used to treat migraine headache and increased eye pressure (glaucoma). carteolol is a nonselective beta-adrenoceptor antagonist.

Pharmacology

Carteolol hydrochloride is a powerful beta-adrenergic receptor antagonist characterized by a long-term pharmacological action, the lack of beta receptor selectivity, an intrinsic sympathomimetic activity (ISA), and a slight local anaesthetic activity (approximately 1/10 of that of propranolol). This drug has a dose-dependent hypotensive effect and does not engender the onset of tachyphylaxis. The pharmacological action consists in the decreased formation of aqueous humor, probably by acting at the level of the ciliary body presenting a wealth of ?2 receptors. The intrinsic sympathomimetic activity of carteolol is responsible for the low incidence of side effects and, thus, for maintaining the heart rate, pulse rate, and arterial blood pressure within the normal physiological range.

Pharmacokinetics

The instillation of carteolol hydrochloride is followed by the rapid absorption by the ocular tissues. Following the instillation of 10μl of 14C-carteolol ophthalmic solution 20 mg/ml into rabbit eyes, the highest platelet and tissue concentrations were obtained between 30 minutes to 2 hours. The study shows that, following topical application, carteolol spreads rapidly into the ocular tissues, passing the corneal barrier. The highest concentrations of 14C-carteolol were found in the following ocular tissues: cornea, iris, anterior sclera, ciliary body conjunctiva, and extraocular muscle. Slightly lower concentrations were found in the retina, choroid, posterior sclera, optic nerve, and aqueous humor. The concentration was especially low in the lens, vitreous body, and plasma. In the various tissues of the contralateral eye, very low radioactivity levels were measured. After the instillation of one drop of carteolol ophthalmic solution 20 mg/ml in healthy volunteers, the plasma concentrations were negligible (1-2 ng/ml). Approximately 16% of the dose is excreted in the urine as an unchanged compound during the first 24 hours after the instillation of a single drop of carteolol hydrochloride 20 mg/ml. The urinary elimination half-life following topical application is about 5 hours.

Clinical Use

The chemical name for carteolol hydrochloride (carteolol) is (±)-5-[3-[(1,1-dimethyl ethyl) amino]-2-hydroxypropoxy]-3,4-dihydro-2(1H)-quinolinone monohydrochloride. Carteolol Hydrochloride (carteolol) Ophthalmic Solution USP, 1% is a nonselective beta-adrenoceptor blocking agent for ophthalmic use. Each mL of sterile solution contains Active: carteolol hydrochloride (carteolol) 10 mg (1%). This drug is used to treat open-angle glaucoma and other causes of high pressure inside the eye. Carteolol hydrochloride ophthalmic may interact with oral carteolol, digoxin, reserpine, insulin or oral diabetes medications, other beta-blockers, calcium channel blockers, or medicines to treat psychiatric disorders.

in vitro

previous findings demonstrate that carteolol, unlike xamoterol, is a nonconventional partial agonist, which causes agonistic effects via interaction with the low-affinity propranolol-resistant site of β1-adrenoceptors and antagonistic actions by the high-affinity site of the same receptors [1].

in vivo

both 8-oh carteolol and carteolol suppressed the water-load induced intraocular pressure (iop) rise in rabbits. 8-oh carteolol was more effective in suppressing water-load induced iop rise in rabbits compared with carteolol on equimolar basis. both 8-oh carteololand carteolol caused a significant decrease in iop in monkeys. 8-oh carteolol was estimated to be more potent than carteolol in lowering iop on equimolar basis in monkeys [2].

References

[1] maura floreani, guglielmina froldi, luigi quintieri, katia varani, pier andrea borea, maria teresa dorigo and paola dorigo. in vitro evidence that carteolol is a nonconventional partial agonist of guinea pig cardiac β1-adrenoceptors: a comparison with xamoterol. jpet 315:1386–1395, 2005
[2] sugiyama k, enya t, kitazawa y. ocular hypotensive effect of 8-hydroxycarteolol, a metabolite of carteolol. int ophthalmol. 1989 jan;13(1-2):85-9.
[3] trinquand c, romanet jp, nordmann jp, allaire c; groupe d'étude. efficacy and safety of long-acting carteolol 1% once daily. a double-masked, randomized study. j fr ophtalmol. 2003 feb;26(2):131-6.

Carteolol hydrochloride Preparation Products And Raw materials

Raw materials

Preparation Products

Global( 175)Suppliers
Supplier Tel Email Country ProdList Advantage
Zibo Hangyu Biotechnology Development Co., Ltd
+86-0533-2185556 +8617865335152 Mandy@hangyubiotech.com China 11001 58
Beijing Cooperate Pharmaceutical Co.,Ltd
010-60279497 sales01@cooperate-pharm.com CHINA 1811 55
Henan Tianfu Chemical Co.,Ltd.
+86-0371-55170693 +86-19937530512 info@tianfuchem.com China 21700 55
Nanjing ChemLin Chemical Industry Co., Ltd.
025-83697070 product@chemlin.com.cn CHINA 3012 60
Hubei XinRunde Chemical Co., Ltd.
+8615102730682 bruce@xrdchem.cn CHINA 566 55
career henan chemical co
+86-0371-86658258 sales@coreychem.com China 29914 58
BOC Sciences
+1-631-485-4226 inquiry@bocsci.com United States 19553 58
Chongqing Chemdad Co., Ltd
+86-023-61398051 +8613650506873 sales@chemdad.com China 39916 58
Zhengzhou Alfa Chemical Co.,Ltd
+8618530059196 sale04@alfachem.cn China 12333 58
TargetMol Chemicals Inc.
+1-781-999-5354 +1-00000000000 marketing@targetmol.com United States 19892 58

View Lastest Price from Carteolol hydrochloride manufacturers

Image Update time Product Price Min. Order Purity Supply Ability Manufacturer
Carteolol hydrochloride pictures 2024-01-02 Carteolol hydrochloride
51781-21-6
US $80.00-800.00 / KG 1KG 0.99 20 tons Zibo Hangyu Biotechnology Development Co., Ltd
Carteolol hydrochloride USP/EP/BP pictures 2021-08-12 Carteolol hydrochloride USP/EP/BP
51781-21-6
US $1.10 / g 1g 99.9% 100 Tons min Dideu Industries Group Limited
Carteolol hydrochloride pictures 2021-07-13 Carteolol hydrochloride
51781-21-6
US $15.00-10.00 / KG 1KG 99%+ HPLC Monthly supply of 1 ton Zhuozhou Wenxi import and Export Co., Ltd

Carteolol hydrochloride Spectrum

5-[3-[(1,1-Dimethylethyl)amino]-2-hydroxypropoxy]-3,4-dihydro-2(1H)-quinolinone Hydrochloride 5-[3-[(tert-butyl)amino]-2-hydroxypropoxy]-3,4-dihydro-2-quinolone monohydrochloride Arteoptic Caltidren Carteol Cartrol dl-Carteolol hydrochloride NSC 300906 Optipress Tenalet Teoptic Cartelo Cartelol Carteolol T Orukalol Carteolol Hydrochloride (200 mg) Ocupress 2(1H)-Quinolinone,5-[3-[(1,1-diMethylethyl)aMino]-2-hydroxypropoxy]-3,4-dihydro-, hydrochloride(1:1) 5-[3-[(1,1-dimethylethyl)amino]-2-hydroxypropoxy]-3,4-dihydro-2(1H)-quinolinone,hydrochloride (1:1) Carteolol monohydrochloride 5-(2-hydroxy-3-tert-butylamino)propoxy-3,4-dihydrocarbostyrilhydrochloride 5-(3-((1,1-dimethylethyl)amino)-2-hydroxypropoxy)-3,4-dihydro-2(1h)-quinolin 5-(3-tert-butylamino-2-hydroxy)propoxy-3,4-dihydrocarbostyrilhydrochloride 5-(3-tert-butylamino-2-hydroxy-propoxy)-3,4-dihydro-2(1h)-chinolinon-hydroch abbott-43326 carbonolol carteololhydrochloride endak endakmite mikelan oc1085 opc1085 2(1H)-QUINOLINONE, 5-[3-[(1,1-DIMETHYLETHYL)AMINO]-2-HYDROXYPROPOXY]-3,4-DIHYDRO-, MONOHYDROCHLORIDE carteolol HCl CARTEOLOL (HYDROCHLORIDE);NSC 300906;OPC 1085 Carteolol for system suitability CRS OPC-1085 hydrochloride 5-[(2RS)-3-[(1,1-Dimethylethyl)amino]-2-hydroxypropoxy]- 3,4-dihydroquinolin-2(1H)-one hydrochloride Carteolol hydrochloride USP/EP/BP Carteolol HCl (OPC-1085 HCl) 2(1H)-QUINOLINONE, 5-[3-[(1,1-DIMETHYLETHYL)AMINO]-2-HYDROXYPROPOXY]-3,4-DIHYDRO-, MONOHYDROCHLORIDE 51781-21-6 Carteolol Hydrochloride (1096757) Carteolol Hydrochloride CAS NO.51781-21-6 51781-21-6 C16H25ClN2O3 C16H24N2O3HCl 32883 CARTROL Intermediates & Fine Chemicals Pharmaceuticals API