acebutolol

Modify Date: 2024-01-02 14:20:32

acebutolol Structure
acebutolol structure
Common Name acebutolol
CAS Number 37517-30-9 Molecular Weight 336.426
Density 1.1±0.1 g/cm3 Boiling Point 564.1±50.0 °C at 760 mmHg
Molecular Formula C18H28N2O4 Melting Point 119-123ºC
MSDS N/A Flash Point 295.0±30.1 °C

 Use of acebutolol


Acebutolol is an orally active β1 adrenergic receptor (β1AR) antagonist. Acebutolol is used for hypertension, angina pectoris and cardiac arrhythmias research[1][2][3].

 Names

Name acebutolol
Synonym More Synonyms

 acebutolol Biological Activity

Description Acebutolol is an orally active β1 adrenergic receptor (β1AR) antagonist. Acebutolol is used for hypertension, angina pectoris and cardiac arrhythmias research[1][2][3].
Related Catalog
Target

β1 adrenoceptor

In Vivo Acebutolol is a beta blocker for the treatment of hypertension and arrhythmias. Acebutolol following single intravenous administration (10 mg/kg) to rat results in the plasma clearance of 61.9 mL/min/kg, the volume of distribution of 9.6 L/kg, and an elimination half-life of 1.8 hours. Acebutolol following single intravenous administration (50 mg/kg) to rat results in the plasma clearance of 46.5 mL/min/kg, the volume of distribution of 9.5 L/kg, and an elimination half-life of 2.3 hours[1]. Acebutolol (30 mg/kg) decreases cardiac output by 65% and 31% after 1 min and 10 min measurements, respectively, in Sprague-Dawley rats. Acebutolol (30 mg/kg) significantly reduces regional blood flow (RBF) in most organs either after 1 min or 10 min measurements when compare with the baseline values in Sprague-Dawley rats[3].
References

[1]. Piquette-Miller, M. and F. Jamali, Pharmacokinetics and multiple peaking of acebutolol enantiomers in rats. Biopharm Drug Dispos, 1997. 18(6): p. 543-56.

[2]. Bristow MR, et al. Treatment of chronic heart failure with β-adrenergic receptor antagonists: a convergence of receptor pharmacology and clinical cardiology. Circ Res. 2011 Oct 28;109(10):1176-94.

[3]. Mostafavi, S., R. Lewanczuk, and R. Foster, Influence of acebutolol and metoprolol on cardiac output and regional blood flow in rats. Biopharm Drug Dispos, 2000. 21(4): p. 121-8.

 Chemical & Physical Properties

Density 1.1±0.1 g/cm3
Boiling Point 564.1±50.0 °C at 760 mmHg
Melting Point 119-123ºC
Molecular Formula C18H28N2O4
Molecular Weight 336.426
Flash Point 295.0±30.1 °C
Exact Mass 336.204895
PSA 87.66000
LogP 1.95
Vapour Pressure 0.0±1.6 mmHg at 25°C
Index of Refraction 1.543
Water Solubility 259 mg/L

 Toxicological Information

CHEMICAL IDENTIFICATION

RTECS NUMBER :
EJ3500500
CHEMICAL NAME :
Butanamide, N-(3-acetyl-4-(2-hydroxy-3-((1-methylethyl)amino)prop oxy)phenyl)-, (+-)-
CAS REGISTRY NUMBER :
37517-30-9
LAST UPDATED :
199612
DATA ITEMS CITED :
8
MOLECULAR FORMULA :
C18-H28-N2-O4
MOLECULAR WEIGHT :
336.48
WISWESSER LINE NOTATION :
3VMR CV1 DO1YQ1MY1&1

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Human - woman
DOSE/DURATION :
152 mg/kg
TOXIC EFFECTS :
Cardiac - change in conduction velocity Vascular - BP lowering not characterized in autonomic section
REFERENCE :
JTCTDW Journal of Toxicology, Clinical Toxicology. (Marcel Dekker, 270 Madison Ave., New York, NY 10016) V.19- 1982- Volume(issue)/page/year: 20,69,1983
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Human - man
DOSE/DURATION :
137 mg/kg/24D-I
TOXIC EFFECTS :
Gastrointestinal - nausea or vomiting Kidney, Ureter, Bladder - other changes in urine composition Biochemical - Enzyme inhibition, induction, or change in blood or tissue levels - transaminases
REFERENCE :
AIMEAS Annals of Internal Medicine. (American College of Physicians, 4200 Pine St., Philadelphia, PA 19104) V.1- 1927- Volume(issue)/page/year: 111,533,1989
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Human - woman
DOSE/DURATION :
109 mg/kg/22D-I
TOXIC EFFECTS :
Gastrointestinal - nausea or vomiting Kidney, Ureter, Bladder - other changes in urine composition Biochemical - Enzyme inhibition, induction, or change in blood or tissue levels - transaminases
REFERENCE :
AIMEAS Annals of Internal Medicine. (American College of Physicians, 4200 Pine St., Philadelphia, PA 19104) V.1- 1927- Volume(issue)/page/year: 111,533,1989
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Subcutaneous
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
125 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
CKFRAY Ceskoslovenska Farmacie. (PNS-Ustredni Expedice a Dovoz Tisku, Kafkova 19, 160 00 Prague 6, Czechoslovakia) V.1- 1952- Volume(issue)/page/year: 42,82,1993
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
75200 ug/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
NPMDAD Nouvelle Presse Medicale. (Paris, France) V.1-11, 1972-82. Volume(issue)/page/year: 7,3258,1978
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Mammal - dog
DOSE/DURATION :
4 mg/kg
TOXIC EFFECTS :
Cardiac - change in rate Vascular - BP lowering not characterized in autonomic section Kidney, Ureter, Bladder - changes in blood vessels or in circulation of kidney
REFERENCE :
MASODV Masui to Sosei. Anesthesia and Resuscitation. (Hiroshima Masui Igakkai, Hiroshima Daigaku Igakubu Masuigaku Kyoshitsu, 1-2-3 Kasumi, Minami-ku, Hiroshima, Hiroshima, Japan) V.6- 1970- Volume(issue)/page/year: 16,13,1980 ** REPRODUCTIVE DATA **
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
DOSE :
120 mg/kg
SEX/DURATION :
female 34-39 week(s) after conception
TOXIC EFFECTS :
Reproductive - Specific Developmental Abnormalities - cardiovascular (circulatory) system Reproductive - Specific Developmental Abnormalities - respiratory system
REFERENCE :
DPTHDL Developmental Pharmacology and Therapeutics. (S. Karger Pub., Inc., 79 Fifth Ave., New York, NY 10003) V.1- 1980- Volume(issue)/page/year: 4(Suppl 1),109,1982
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Unreported
DOSE :
1080 mg/kg
SEX/DURATION :
female 1-39 week(s) after conception
TOXIC EFFECTS :
Reproductive - Specific Developmental Abnormalities - cardiovascular (circulatory) system Reproductive - Effects on Newborn - growth statistics (e.g.%, reduced weight gain) Reproductive - Effects on Newborn - biochemical and metabolic
REFERENCE :
BMJOAE British Medical Journal. (British Medical Assoc., BMA House, Tavistock Sq., London WC1H 9JR, UK) V.1- 1857- Volume(issue)/page/year: 283,1077,1981

 Safety Information

HS Code 2924299090

 Customs

HS Code 2924299090
Summary 2924299090. other cyclic amides (including cyclic carbamates) and their derivatives; salts thereof. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:30.0%

 Synonyms

3'-Acetyl-4'-[2-hydroxy-3-(isopropylamino)propoxy]butyranilide
Butanamide, N-(3-acetyl-4-(2-hydroxy-3-((1-methylethyl)amino)propoxy)phenyl)-, (±)-
アセブトロール
EINECS 253-539-0
Butanamide, N-[3-acetyl-4-[2-hydroxy-3-[(1-methylethyl)amino]propoxy]phenyl]-
N-{3-acetyl-4-[2-hydroxy-3-(propan-2-ylamino)propoxy]phenyl}butanamide
N-{3-Acetyl-4-[2-hydroxy-3-(isopropylamino)propoxy]phenyl}butanamide
acebutolol
N-(3-Acetyl-4-(2-hydroxy-3-(isopropylamino)propoxy)phenyl)butyramide
IL 17803A
MFCD00599435
Acecor