Bupranolol

Names

[ Name ]:
Bupranolol

[Synonym ]:
Ophtorenin
Bupranol

Biological Activity

[Description]:

Bupranolol is an orally active, competitive and non-selective β-adrenoceptor antagonist without intrinsic sympathomimetic activity[1].

[Related Catalog]:

Research Areas >> Cancer

Signaling Pathways >> GPCR/G Protein >> Adrenergic Receptor

Research Areas >> Inflammation/Immunology

[Target]

β-adrenoceptor

[In Vitro]

Bupranolol (1~3 μM) shifts isoprenaline-induced relaxation in the presence of 30 μM propranolol. Bupranolol acts as a competitive antagonist of isoprenaline-induced relaxation in the presence of 300 nM propranolol, with a pA2 value of 5.90. Bupranolol antagonizes β1- and β2-ARs with pA2 values of ≈9.0, and also antagonizes β3-AR with a pA2 value of 6.0[1].

[References]

[1]. Chino D, et al. Pharmacological identification of β-adrenoceptor subtypes mediating isoprenaline-induced relaxation of guinea pig colonic longitudinal smooth muscle. J Smooth Muscle Res. 2018;54(0):13-27.

[2]. Babu RJ, et al. Effect of cyclodextrins on the complexation and transdermal delivery of bupranolol through rat skin. Int J Pharm. 2004;271(1-2):155-165.

Chemical & Physical Properties

[ Density]:
1.098g/cm3

[ Boiling Point ]:
396.3ºC at 760mmHg

[ Molecular Formula ]:
C₁₄H₂₂ClNO₂

[ Molecular Weight ]:
271.78300

[ Flash Point ]:
193.5ºC

[ Exact Mass ]:
271.13400

[ PSA ]:
41.49000

[ LogP ]:
3.16710

[ Vapour Pressure ]:
5.44E-07mmHg at 25°C

[ Index of Refraction ]:
1.522

Toxicological Information

CHEMICAL IDENTIFICATION

RTECS NUMBER :: UA8430000

CHEMICAL NAME :: 2-Propanol, 1-(tert-butylamino)-3-(2-chloro-5-methylphenoxy)-

CAS REGISTRY NUMBER :: 14556-46-8

LAST UPDATED :: 199612

DATA ITEMS CITED :: 1

MOLECULAR FORMULA :: C14-H22-Cl-N-O2

MOLECULAR WEIGHT :: 271.82

WISWESSER LINE NOTATION :: 1X1&1&M1YQ1OR BG E1

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 45 mg/kg

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

REFERENCE :: ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 27,1022,1977

Safety Information

[ HS Code ]:
2922509090

Customs

[ HS Code ]: 2922509090

[ Summary ]:
2922509090. other amino-alcohol-phenols, amino-acid-phenols and other amino-compounds with oxygen function. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:30.0%