CAS 63659-19-8|Betaxolol hydrochloride

Introduction：Basic information about CAS 63659-19-8|Betaxolol hydrochloride, including its chemical name, molecular formula, synonyms, physicochemical properties, and safety information, etc.

Table of Contents

1. Names
2. Betaxolol hydrochloride BiologicalActivity
3. Chemical & Physical Properties
4. Toxicological Information
CHEMICAL IDENTIFICATION
HEALTH HAZARD DATA
ACUTE TOXICITY DATA
5. Safety Information
6. Customs
7. Articles25
8. Synonyms

Common Name	Betaxolol hydrochloride
CAS Number	63659-19-8	Molecular Weight	343.889
Density	/	Boiling Point	448ºC at 760 mmHg
Molecular Formula	C₁₈H₃₀ClNO₃	Melting Point	/
MSDS	ChineseUSA	Flash Point	224.7ºC
Symbol	GHS07	Signal Word	Warning

Names

Name	betaxolol hydrochloride
Synonym	More Synonyms

Betaxolol hydrochloride BiologicalActivity

Description	Betaxolol Hydrochloride is a selective beta1 adrenergic receptor blocker used in the treatment of hypertension and glaucoma.Target: Beta1 Adrenergic ReceptorBetaxolol is a cardioselective beta-adrenergic receptor blocking agent. Betaxolol (5 mg/kg via i.p. injection) was administered at 24 and then 44 h following the final chronic cocaine administration. Animals treated with betaxolol during cocaine withdrawal exhibited a significant attenuation of anxiety-like behavior characterized by increased time spent in the open arms and increased entries into the open arms compared to animals treated with only saline during cocaine withdrawal. Betaxolol did not produce anxiolytic-like effects in control animals treated chronically with saline [1]. Betaxolol produces less systemic beta 2- and possibly beta 1-adrenergic receptor blockade than either timolol or levobunolol. Betaxolol may be relatively safer to use in patients with reactive airway disease than either timolol or levobunolol [2].
Related Catalog	Signaling Pathways >>GPCR/G Protein >>Adrenergic ReceptorResearch Areas >>Cardiovascular Disease
References	[1]. Rudoy, C.A. and E.J. Van Bockstaele, Betaxolol, a selective beta(1)-adrenergic receptor antagonist, diminishes anxiety-like behavior during early withdrawal from chronic cocaine administration in rats. Prog Neuropsychopharmacol Biol Psychiatry, 2007. 31(5 [2]. Lesar, T.S., Comparison of ophthalmic beta-blocking agents. Clin Pharm, 1987. 6(6): p. 451-63.

Description

Betaxolol Hydrochloride is a selective beta1 adrenergic receptor blocker used in the treatment of hypertension and glaucoma.Target: Beta1 Adrenergic ReceptorBetaxolol is a cardioselective beta-adrenergic receptor blocking agent. Betaxolol (5 mg/kg via i.p. injection) was administered at 24 and then 44 h following the final chronic cocaine administration. Animals treated with betaxolol during cocaine withdrawal exhibited a significant attenuation of anxiety-like behavior characterized by increased time spent in the open arms and increased entries into the open arms compared to animals treated with only saline during cocaine withdrawal. Betaxolol did not produce anxiolytic-like effects in control animals treated chronically with saline [1]. Betaxolol produces less systemic beta 2- and possibly beta 1-adrenergic receptor blockade than either timolol or levobunolol. Betaxolol may be relatively safer to use in patients with reactive airway disease than either timolol or levobunolol [2].

Related Catalog

Signaling Pathways >>GPCR/G Protein >>Adrenergic ReceptorResearch Areas >>Cardiovascular Disease

References

[1]. Rudoy, C.A. and E.J. Van Bockstaele, Betaxolol, a selective beta(1)-adrenergic receptor antagonist, diminishes anxiety-like behavior during early withdrawal from chronic cocaine administration in rats. Prog Neuropsychopharmacol Biol Psychiatry, 2007. 31(5

[2]. Lesar, T.S., Comparison of ophthalmic beta-blocking agents. Clin Pharm, 1987. 6(6): p. 451-63.

Chemical & Physical Properties

Boiling Point	448ºC at 760 mmHg
Molecular Formula	C₁₈H₃₀ClNO₃
Molecular Weight	343.889
Flash Point	224.7ºC
Exact Mass	343.191437
PSA	50.72000
LogP	3.58630
InChIKey	CHDPSNLJFOQTRK-UHFFFAOYSA-N
SMILES	CC(C)NCC(O)COc1ccc(CCOCC2CC2)cc1.Cl
Storage condition	Store at RT
Water Solubility	H2O: 36 mg/mL, soluble

Toxicological Information

CHEMICAL IDENTIFICATION

RTECS NUMBER :: UA9823000

CHEMICAL NAME :: 2-Propanol, 1-(4-(2-(cyclopropylmethoxy)ethyl)phenoxy)-3-((1-meth ylethyl)amino)-, hydrochloride

CAS REGISTRY NUMBER :: 63659-19-8

LAST UPDATED :: 199612

DATA ITEMS CITED :: 19

MOLECULAR FORMULA :: C18-H29-N-O3.Cl-H

MOLECULAR WEIGHT :: 343.94

WISWESSER LINE NOTATION :: L3TJ A1O2R DO1YQ1MY1&1 &GH

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 998 mg/kg

TOXIC EFFECTS :: Behavioral - tremor Behavioral - ataxia Nutritional and Gross Metabolic - body temperature decrease

REFERENCE :: YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972- Volume(issue)/page/year: 18(Suppl 7),S1621,1990

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 389 mg/kg

TOXIC EFFECTS :: Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - dyspnea Skin and Appendages - hair

REFERENCE :: YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972- Volume(issue)/page/year: 18(Suppl 7),S1621,1990

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 27400 ug/kg

TOXIC EFFECTS :: Sense Organs and Special Senses (Eye) - effect, not otherwise specified Behavioral - tremor Behavioral - convulsions or effect on seizure threshold

REFERENCE :: YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972- Volume(issue)/page/year: 18(Suppl 7),S1621,1990

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 48 mg/kg

TOXIC EFFECTS :: Behavioral - tremor Behavioral - convulsions or effect on seizure threshold Behavioral - changes in motor activity (specific assay)

REFERENCE :: LMSED6 L.E.R.S. Monograph Series. Laboratories d'Etudes et de Recherches Synthelabo Monograph Series. (Raven Press, 1185 Ave. of the Americas, New York, NY 10036) V.1- 1983- Volume(issue)/page/year: 1,43,1983

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 332 mg/kg

TOXIC EFFECTS :: Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - dyspnea Skin and Appendages - hair

REFERENCE :: YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972- Volume(issue)/page/year: 18(Suppl 7),S1621,1990

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 37 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: USXXAM United States Patent Document. (U.S. Patent Office, Box 9, Washington, DC 20231) Volume(issue)/page/year: #4252984

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: 30 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: IYKEDH Iyakuhin Kenkyu. Study of Medical Supplies. (Nippon Koteisho Kyokai, 12-15, 2-chome, Shibuya, Shibuya-ku, Tokyo 150, Japan) V.1- 1970- Volume(issue)/page/year: 25,815,1994 ** OTHER MULTIPLE DOSE TOXICITY DATA **

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 72800 mg/kg/26W-I

TOXIC EFFECTS :: Liver - changes in liver weight Endocrine - changes in spleen weight Related to Chronic Data - death

REFERENCE :: LMSED6 L.E.R.S. Monograph Series. Laboratories d'Etudes et de Recherches Synthelabo Monograph Series. (Raven Press, 1185 Ave. of the Americas, New York, NY 10036) V.1- 1983- Volume(issue)/page/year: 1,43,1983

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 7840 mg/kg/4W-I

TOXIC EFFECTS :: Gastrointestinal - changes in structure or function of salivary glands

REFERENCE :: LMSED6 L.E.R.S. Monograph Series. Laboratories d'Etudes et de Recherches Synthelabo Monograph Series. (Raven Press, 1185 Ave. of the Americas, New York, NY 10036) V.1- 1983- Volume(issue)/page/year: 1,43,1983

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: 7300 mg/kg/1Y-I

TOXIC EFFECTS :: Kidney, Ureter, Bladder - other changes in urine composition

REFERENCE :: YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972- Volume(issue)/page/year: 18(Suppl 7),S1689,1990

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: 7280 mg/kg/52W-I

TOXIC EFFECTS :: Sense Organs and Special Senses (Eye) - effect, not otherwise specified

REFERENCE :: LMSED6 L.E.R.S. Monograph Series. Laboratories d'Etudes et de Recherches Synthelabo Monograph Series. (Raven Press, 1185 Ave. of the Americas, New York, NY 10036) V.1- 1983- Volume(issue)/page/year: 1,43,1983

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: 168 mg/kg/4W-I

TOXIC EFFECTS :: Cardiac - pulse rate

REFERENCE :: LMSED6 L.E.R.S. Monograph Series. Laboratories d'Etudes et de Recherches Synthelabo Monograph Series. (Raven Press, 1185 Ave. of the Americas, New York, NY 10036) V.1- 1983- Volume(issue)/page/year: 1,43,1983 ** REPRODUCTIVE DATA **

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 30464 mg/kg

SEX/DURATION :: multigeneration

TOXIC EFFECTS :: Reproductive - Fertility - post-implantation mortality (e.g. dead and/or resorbed implants per total number of implants) Reproductive - Fertility - litter size (e.g. # fetuses per litter; measured before birth) Reproductive - Effects on Embryo or Fetus - fetotoxicity (except death, e.g., stunted fetus)

REFERENCE :: YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972- Volume(issue)/page/year: 18(Suppl 7),S1703,1990

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 30464 mg/kg

SEX/DURATION :: multigeneration

TOXIC EFFECTS :: Reproductive - Effects on Embryo or Fetus - fetal death Reproductive - Effects on Newborn - growth statistics (e.g.%, reduced weight gain) Reproductive - Effects on Newborn - delayed effects

REFERENCE :: YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972- Volume(issue)/page/year: 18(Suppl 7),S1703,1990

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 5200 mg/kg

SEX/DURATION :: female 17-21 day(s) after conception lactating female 21 day(s) post-birth

TOXIC EFFECTS :: Reproductive - Effects on Newborn - stillbirth Reproductive - Effects on Newborn - viability index (e.g., # alive at day 4 per # born alive) Reproductive - Effects on Newborn - physical

REFERENCE :: YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972- Volume(issue)/page/year: 18(Suppl 7),S1753,1990

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 5200 mg/kg

SEX/DURATION :: female 17-21 day(s) after conception lactating female 21 day(s) post-birth

TOXIC EFFECTS :: Reproductive - Effects on Newborn - viability index (e.g., # alive at day 4 per # born alive) Reproductive - Effects on Newborn - physical Reproductive - Effects on Newborn - delayed effects

REFERENCE :: YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972- Volume(issue)/page/year: 18(Suppl 7),S1753,1990

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Subcutaneous

DOSE :: 50 mg/kg

SEX/DURATION :: female 7-16 day(s) after conception

TOXIC EFFECTS :: Reproductive - Effects on Newborn - other neonatal measures or effects Reproductive - Effects on Newborn - biochemical and metabolic

REFERENCE :: AIPBE4 Archives Internationalos de Physiologie, de Biochimie et de Biophysique. (Vaillant-Carmanne, s.a., Zeven Puttenstraat 20, 3690 Zutendaal, Belgium) V.99- 1991- Volume(issue)/page/year: 100,355,1992

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 468 mg/kg

SEX/DURATION :: female 6-18 day(s) after conception

TOXIC EFFECTS :: Reproductive - Fertility - post-implantation mortality (e.g. dead and/or resorbed implants per total number of implants)

REFERENCE :: LMSED6 L.E.R.S. Monograph Series. Laboratories d'Etudes et de Recherches Synthelabo Monograph Series. (Raven Press, 1185 Ave. of the Americas, New York, NY 10036) V.1- 1983- Volume(issue)/page/year: 1,43,1983

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 468 mg/kg

SEX/DURATION :: female 6-18 day(s) after conception

TOXIC EFFECTS :: Reproductive - Fertility - pre-implantation mortality (e.g. reduction in number of implants per female; total number of implants per corpora lutea) Reproductive - Fertility - post-implantation mortality (e.g. dead and/or resorbed implants per total number of implants)

REFERENCE :: YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972- Volume(issue)/page/year: 18(Suppl 7),S1741,1990

Safety Information

Symbol	GHS07
Signal Word	Warning
Hazard Statements	H302
Precautionary Statements	P301 + P312 + P330
Personal Protective Equipment	dust mask type N95 (US);Eyeshields;Gloves
Hazard Codes	Xn:Harmful;
Risk Phrases	R22
RIDADR	NONH for all modes of transport
WGK Germany	3
RTECS	UA9823000
HS Code	2922199090

Customs

HS Code	2922199090
Summary	2922199090. other amino-alcohols, other than those containing more than one kind of oxygen function, their ethers and esters; salts thereof. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:30.0%

Articles25

Development and validation of stability-indicating TLC-densitometric method for determination of betaxolol with LC-ESI/MS analysis of degradation product.

Acta Pol. Pharm. 70(4) , 643-52, (2013)

The purpose of this work was to develop a sensitive stability indicating TLC-densitometric method for the determination of betaxolol (Bx) in pharmaceutical preparations and to study the stability of B...

Comparison of the Progression Rates of the Superior, Inferior, and Both Hemifield Defects in Normal-Tension Glaucoma Patients

Am. J. Ophthalmol. 154(6) , 958-968.e1, (2012)

Purpose To investigate the progression rates of superior and inferior hemifield defects and each hemifield in bihemifield defects in normal-tension glaucoma patients and to compare the progression rat...

Microcalorimetric and spectrographic studies on the interaction of DNA with betaxolol.

Int. J. Pharm. 386(1-2) , 165-71, (2010)

The interaction of calf thymus deoxyribonucleic acid (ct-DNA) with betaxolol (BET) in aqueous buffer solution (pH 7.40) has been investigated using isothermal titration calorimetry (ITC), ultraviolet ...

Synonyms

(±)-1-(p-(2-(Cyclopropylmethoxy)ethyl)phenoxy)-3-(isopropylamino)-2-propanol Hydrochloride

Betaxolol

(+/-)-1-{p-[2-(cyclopropylmethoxy) ethyl] phenoxy}-3-isopropylamino-2-propanol

Betaxololum

2-Propanol, 1-[4-[2-(cyclopropylmethoxy)ethyl]phenoxy]-3-[(1-methylethyl)amino]-, hydrochloride (1:1)

EINECS 264-384-3

1-{4-[2-(cyclopropylmethoxy)ethyl]phenoxy}-3-(propan-2-ylamino)propan-2-ol hydrochloride (1:1)

Betaxolol (TN)

Betoptic

Betazolol

1-{4-[2-(cyclopropylmethoxy)ethyl]phenoxy}-3-[(1-methylethyl)amino]propan-2-ol hydrochloride

MFCD00242959

1-{4-[2-(Cyclopropylmethoxy)ethyl]phenoxy}-3-[(1-methylethyl)amino]propan-2-olhydrochlorid

1-[4-[2-(cyclopropylmethoxy)ethyl]phenoxy]-3-(propan-2-ylamino)propan-2-ol,hydrochloride

1-[4-[2-(cyclopropylmethoxy)ethyl]phenoxy]-3-[(1-methylethyl)amino]-2-propanol

1-{4-[2-(Cyclopropylmethoxy)ethyl]phenoxy}-3-(isopropylamino)-2-propanol hydrochloride (1:1)

Betaxolol [INN:BAN]

Betaxolol hydrochloride

Kerlone

1-{4-[2-(cyclopropylméthoxy)éthyl]phénoxy}-3-[(1-méthyléthyl)amino]propan-2-ol chlorhydrate

1-[4-[2-(cyclopropylmethoxy)ethyl]phenoxy]-3-(propan-2-ylamino)propan-2-ol

1-{4-[2-(Cyclopropylmethoxy)-ethyl]-phenoxy}-3-isopropylamino-propan-2-ol

1-{4-[2-(Cyclopropylmethoxy)ethyl]phenoxy}-3-(isopropylamino)propan-2-ol hydrochloride (1:1)

Betaxololum [INN-Latin]

2-propanol, 1-[4-[2-(cyclopropylmethoxy)ethyl]phenoxy]-3-[(1-methylethyl)amino]-, hydrochloride

UNII:6X97D2XT0O

Betaxolol HCl

Betaxolol (hydrochloride)

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