Mabuterol hydrochloride - CAS 54240-36-7
Category: Inhibitor
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Molecular Formula:
C13H19Cl2F3N2O
Molecular Weight:
347.203
COA:
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Targets:
Adrenergic Receptor
Description:
Mabuterol hydrochloride is a salt form of Mabuterol, which is a selective β2 adrenoreceptor agonist.
Related CAS:
1353867-83-0 (labelled)
Synonyms:
1-(4-Amino-3-chloro-5-trifluoromethylphenyl)-2-tert-butylaminoethanol hydrochloride
MSDS:
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InChIKey:
MMCDXJOMPMIKGP-UHFFFAOYSA-N
InChI:
InChI=1S/C13H18ClF3N2O.ClH/c1-12(2,3)19-6-10(20)7-4-8(13(15,16)17)11(18)9(14)5-7;/h4-5,10,19-20H,6,18H2,1-3H3;1H
Canonical SMILES:
CC(C)(C)NCC(C1=CC(=C(C(=C1)Cl)N)C(F)(F)F)O.Cl
1.Toxicology of mabuterol.
Amemiya K, Kudoh M, Suzuki H, Saga K, Hosaka K. Arzneimittelforschung. 1984;34(11A):1680-4.
The acute, subacute and chronic toxicity of dl-1- (4-amino-3-chloro-5-trifluoromethyl-phenyl)-2-tert.-butyl-amino-ethanol hydrochloride (mabuterol), a new beta 2-selective adrenoceptor stimulant, was studied in mouse, rat, rabbit and dog. The acute oral LD50 was between 199.9 and 319.3 mg/kg in all four species used and did not differ significantly between the sexes. Intravenous LD50 was between 18.3 and 51.1 mg/kg (four species), i.p. between 60 and 78.3 mg/kg and s.c. between 113 and 125.7 mg/kg (mouse and rat only). In subacute and chronic studies in Wistar rats, mabuterol was dosed by gavage at 0, 10, 20, 40, 80 and 120 mg/kg for 1 month, and 0, 1, 2.5, 10 and 40 mg/kg for 3 (interim) and 6 months or in food at 0, 2.5, 10 and 40 mg/kg for 6 (interim) and 12 months. Beagle dogs were dosed by gelatine capsule with 0, 0.05, 0.5, 5 and 50 (25) mg/kg for 6 (interim) and 24 months. In rats, 1 and 2.5 mg/kg were well tolerated. At 10 mg/kg and above, irritability and hypersalivation were seen dependent on dose.
2.Pilot clinical trial with a new beta 2-sympathomimetic bronchodilator, mabuterol.
Ulmer WT, Scholz HJ, Baines A. Arzneimittelforschung. 1984;34(11A):1697-8.
An open pilot study was performed on 10 patients with chronic, reversible, obstructive lung disease and known good response to beta 2-bronchodilators. The effects of 40, 60 and 80 micrograms 1-(4-amino-3-chloro-5-trifluoromethyl-phenyl)-2-tert.-butylamino-ethanol hydrochloride (mabuterol) given orally and of 0.4 mg fenoterol (aerosol) were measured on airway resistance, thoracic gas volume, pulse rate and blood pressure. Side effects, ECG and laboratory values were recorded. Mabuterol was found to have a good, clinically useful, bronchodilating effect and to possess excellent tolerability at doses of 40-60 micrograms.
3.Single dose pharmacokinetics of mabuterol in man.
Guentert TW, Buskin JN, Galeazzi RL. Arzneimittelforschung. 1984;34(11A):1691-6.
The pharmacokinetics of 1-(4-amino-3-chloro-5-trifluoromethyl-phenyl)-2-tert.-butylamino-ethanol hydrochloride (mabuterol), a new bronchodilator in the series of phenyl-ethanolamine derivatives, was investigated in six healthy young male volunteers. Use of tritiated compound allowed characterization of the plasma concentration-time profile of unchanged drug after a single oral dose of 40 micrograms in the form of a drinking solution. Peak concentrations of 96-160 pg/ml were reached between 1.5 and 3.2 h and drug concentrations declined thereafter in a biphasic pattern. Elimination of unchanged drug was slow (t 1/2 beta 20-30 h) due to a low clearance (CL/F 3.0 ml/min/kg) and a large volume of distribution (V beta/F 5.8 l/kg). Absorption of the drug from the gastrointestinal tract was complete and availability of unchanged drug to the systemic circulation could be estimated (F greater than 0.91) using flow model concepts. At peak concentrations mabuterol accounted for only 46% of total radioactivity in plasma but no major conjugated or unconjugated metabolite has been identified.
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CAS 54240-36-7 Mabuterol hydrochloride

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