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Carteolol

Names

[ CAS No. ]:
51781-06-7

[ Name ]:
Carteolol

[Synonym ]:
Carteololum
Carteolol [INN:BAN]
Carteololum [INN-Latin]
5-[3-(tert-Butylamino)-2-hydroxypropoxy]-3,4-dihydro-1H-quinolin-2-one
CARTEOLOL
Ocupress
Carteolol HCl
Carteolol Monohydrochloride
Carteolol (INN)
5-(3-tert-butylamino-2-hydroxy-propoxy)-3,4-dihydro-1H-quinolin-2-one
5-[3-(1,1-dimethylethyl)amino-2-hydroxypropoxy]-3,4-dihydro-2(1H)-quinolinone

Biological Activity

[Description]:

Carteolol is a non-selective β-adrenoceptor antagonist. Carteolol induces apoptosis via a caspase activated and mitochondrial-dependent pathway. Carteolol can be used for glaucoma research[1].

[Related Catalog]:

Signaling Pathways >> Apoptosis >> Bcl-2 Family
Signaling Pathways >> Apoptosis >> Caspase
Signaling Pathways >> GPCR/G Protein >> Adrenergic Receptor
Research Areas >> Neurological Disease

[In Vitro]

Carteolol (0-2%; 0-28 hours; HCECs) has cytotoxicity and decreases cell viability in a dose- and time-dependent manner[1]. Carteolol (0.25%; 4-12 hours; HCECs) induces apoptosis and necroptotic protein expression in HCECs[1]. Cell Viability Assay[1] Cell Line: HCECs Concentration: 0.00390625-2% Incubation Time: 0, 2, 4, 8, 16, 20,24 and 28 hours Result: Decreased cell viability with the concentrations above 0.0015625% in a dose- and time-dependent manner. Western Blot Analysis[1] Cell Line: HCECs Concentration: 0.25% Incubation Time: 4, 8 and 12 hours Result: Dampened expression of the anti-apoptotic protein Bcl-2 and Bcl-xL, enhanced expression of the pro-apoptotic proteins Bax and Bad, and mitochondrial-released pro-apoptotic proteins Cyt.c and AIF. Cell Cycle Analysis[1] Cell Line: HCECs Concentration: 0.25% Incubation Time: 4, 8 and 12 hours Result: Increased the number of G1 phase of the cell cycle, whereas decreased S phase.

[References]

[1]. Su W, et, al. Dose- and Time-Dependent Cytotoxicity of Carteolol in Corneal Endothelial Cells and the Underlying Mechanisms. Front Pharmacol. 2020 Mar 6;11:202.

Chemical & Physical Properties

[ Density]:
1.13 g/cm3

[ Boiling Point ]:
518.6ºC at 760 mmHg

[ Molecular Formula ]:
C16H24N2O3

[ Molecular Weight ]:
292.37300

[ Flash Point ]:
267.4ºC

[ Exact Mass ]:
292.17900

[ PSA ]:
70.59000

[ LogP ]:
2.22800

[ Index of Refraction ]:
1.5800 (estimate)

Toxicological Information

CHEMICAL IDENTIFICATION

RTECS NUMBER :
VC8281000
CHEMICAL NAME :
2(1H)-Quinolinone, 5-(3-((1,1-dimethylethyl)amino)-2-hydroxypropoxy)-3,4 -dihydro-
CAS REGISTRY NUMBER :
51781-06-7
LAST UPDATED :
199112
DATA ITEMS CITED :
4
MOLECULAR FORMULA :
C16-H24-N2-O3
MOLECULAR WEIGHT :
292.42
WISWESSER LINE NOTATION :
T66 BMVT&J GO1YQ1MX1&1&1

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
810 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
JJTOEX Japanese Journal of Toxicology. (Yakugyo Jihosha, Hokushin Bldg., 2-36 Jinbo-cho, Kanda, Chiyoda-ku, Tokyo, 101, Japan) V.1- 1988- Volume(issue)/page/year: 4,121,1991
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Mammal - dog
DOSE/DURATION :
830 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 19,323,1980
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - rabbit
DOSE/DURATION :
740 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 19,323,1980
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Rodent - rabbit
DOSE/DURATION :
112 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 19,323,1980

Safety Information

[ HS Code ]:
2933790090

Synthetic Route

Click to get detail synthetic route

Customs

[ HS Code ]: 2933790090

[ Summary ]:
2933790090. other lactams. VAT:17.0%. Tax rebate rate:9.0%. . MFN tariff:9.0%. General tariff:20.0%

Related Compounds

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