Pronethalol hydrochloride

Names

[ CAS No. ]:
51-02-5

[ Name ]:
Pronethalol hydrochloride

[Synonym ]:
PRONETHALOL HYDROCHLORIDE
Pronetalol hydrochloride
Nethalide hydrochloride
DL-Pronethalol hydrochloride
Pronethalol.HCl
Naphthylisoproterenol hydrochloride
Alderlin hydrochloride

Biological Activity

[Description]:

Pronethalol ((±)-Pronethalo) is a non-selective β-adrenergic antagonist. Pronethalol is a potent inhibitor of Sox2 expression. Pronethalol protects against and to reverse Digitalis-induced ventricular arrhythmias, and limits the cerebral arteriovenous malformation (AVMs)[1][2].

[Related Catalog]:

Research Areas >> Cardiovascular Disease

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

Research Areas >> Neurological Disease

[In Vitro]

Pronethalol (2, 10, 20 μM) represses EGFP expression in a dose- and time-dependent manner in ReNcell VM cells. Pronethalol (10 μM; 2 days) reduces Sox2 expression to less than 10% after 2 days of treatment[2].

[In Vivo]

Pronethalol (0.15 mg/g; daily; for 14 days) stabilizes endothelial differentiation, lumen formation and improves cerebral arteriovenous malformation (AVMs) in Mgp–/– mice[2].

[References]

[1]. Aroesty JM, et al. The effects of a beta-adrenergic blocking agent, pronethalol, on digitalis-induced ventricular arrhythmias. Am Heart J. 1966 Apr;71(4):503-508.

[2]. Jiayi Yao, et al. Elevated endothelial Sox2 causes lumen disruption and cerebral arteriovenous malformations. J Clin Invest. 2019 Jun 24;129(8):3121-3133.

Chemical & Physical Properties

[ Density]:
1.074g/cm3

[ Boiling Point ]:
322.4ºC at 760mmHg

[ Molecular Formula ]:
C₁₅H₂₀ClNO

[ Molecular Weight ]:
265.77800

[ Flash Point ]:
84.3ºC

[ Exact Mass ]:
265.12300

[ PSA ]:
32.26000

[ LogP ]:
4.06410

[ Index of Refraction ]:
1.596

Toxicological Information

CHEMICAL IDENTIFICATION

RTECS NUMBER :: QJ9275000

CHEMICAL NAME :: Naphthalenemethanol, alpha-((isopropylamino)methyl)-, hydrochloride

CAS REGISTRY NUMBER :: 51-02-5

LAST UPDATED :: 199512

DATA ITEMS CITED :: 7

MOLECULAR FORMULA :: C15-H19-N-O.Cl-H

MOLECULAR WEIGHT :: 265.81

WISWESSER LINE NOTATION :: L66J CYQ1MY1&1 &GH

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 :: 425 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: 18,48,1968

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 102 mg/kg

TOXIC EFFECTS :: Behavioral - somnolence (general depressed activity) Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - respiratory stimulation

REFERENCE :: IJPPAZ Indian Journal of Physiology and Pharmacology. (All India Institute of Medical Sciences, Dept. of Physiology, Ansari Nagar, New Delhi 110 029, India) V.1- 1957- Volume(issue)/page/year: 17,235,1973

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 35 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: 18,48,1968 ** TUMORIGENIC DATA **

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 10 gm/kg/25W-C

TOXIC EFFECTS :: Tumorigenic - equivocal tumorigenic agent by RTECS criteria Endocrine - tumors

REFERENCE :: NATUAS Nature. (Nature Subscription Dept., POB 1018, Manasguan, NJ 08736) V.1- 1869- Volume(issue)/page/year: 207,594,1965 *** REVIEWS *** IARC Cancer Review:Animal Limited Evidence IMEMDT IARC Monographs on the Evaluation of Carcinogenic Risk of Chemicals to Man. (WHO Publications Centre USA, 49 Sheridan Ave., Albany, NY 12210) V.1- 1972- Volume(issue)/page/year: 13,227,1977 IARC Cancer Review:Human No Adequate Data IMEMDT IARC Monographs on the Evaluation of Carcinogenic Risk of Chemicals to Man. (WHO Publications Centre USA, 49 Sheridan Ave., Albany, NY 12210) V.1- 1972- Volume(issue)/page/year: 13,227,1977 IARC Cancer Review:Group 3 IMSUDL IARC Monographs, Supplement. (WHO Publications Centre USA, 49 Sheridan Ave., Albany, NY 12210) No.1- 1979- Volume(issue)/page/year: 7,56,1987

Safety Information

[ 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%