Zinterol hydrochloride

Modify Date: 2024-01-05 12:41:40

Zinterol hydrochloride Structure
Zinterol hydrochloride structure
Common Name Zinterol hydrochloride
CAS Number 38241-28-0 Molecular Weight 414.94700
Density N/A Boiling Point 574.3ºC at 760 mmHg
Molecular Formula C19H27ClN2O4S Melting Point N/A
MSDS USA Flash Point 301.1ºC
Symbol GHS07
GHS07
Signal Word Warning

 Use of Zinterol hydrochloride


Zinterol hydrochloride (MJ 9184 hydrochloride) is a potent and selective β2-adrenoceptor agonist[1]. Zinterol hydrochloride increases ICa in a concentration-dependent manner with an EC50 of 2.2 nM[2]. Zinterol hydrochloride induces ventricular arrhythmias in conscious heart failure rabbits[3].

 Names

Name Zinterol hydrochloride
Synonym More Synonyms

 Zinterol hydrochloride Biological Activity

Description Zinterol hydrochloride (MJ 9184 hydrochloride) is a potent and selective β2-adrenoceptor agonist[1]. Zinterol hydrochloride increases ICa in a concentration-dependent manner with an EC50 of 2.2 nM[2]. Zinterol hydrochloride induces ventricular arrhythmias in conscious heart failure rabbits[3].
Related Catalog
Target

β2-adrenoceptor[1]

In Vivo Zinterol (2.5 μg/kg i.v. bolus over 5 s) leads to ventricular arrhythmias including premature ventricular complexes (PVCs) and runs of ventricular tachycardia (VT) in heart failure (HF) rabbits. Zinterol at a lower dose (1 μg/kg i.v, n=4) does not induce ventricular arrhythmias in HF rabbits[3]. Animal Model: In New Zealand White HF rabbits of either sex[3] Dosage: 1.0 or 2.5 μg/kg Administration: Intravenous bolus administration; over 5 seconds Result: 2.5 μg/kg did not significantly alter heart rate or mean arterial blood pressure in either control or HF rabbits. 2.5 μg/kg led to ventricular arrhythmias including premature ventricular complexes (PVCs) and runs of VT (up to 13 beats long) in 4 of 6 HF rabbits (vs 0 of 5 controls, p<0.01). 1 μg/kg did not induce ventricular arrhythmias in HF rabbits.
References

[1]. Gwee MC, et al. Pharmacological actions of a new -adrenoceptor agonist, MJ-9184-1, in anaesthetized cats. Br J Pharmacol. 1972 Nov;46(3):375-85.

[2]. Skeberdis VA, et al. Beta-2 adrenergic activation of L-type Ca2+ current in cardiac myocytes. J Pharmacol Exp Ther. 1997 Nov;283(2):452-61.

[3]. Desantiago J, et al. Arrhythmogenic effects of beta2-adrenergic stimulation in the failing heart are attributable to enhanced sarcoplasmic reticulum Ca load. Circ Res. 2008 Jun 6;102(11):1389-97.

 Chemical & Physical Properties

Boiling Point 574.3ºC at 760 mmHg
Molecular Formula C19H27ClN2O4S
Molecular Weight 414.94700
Flash Point 301.1ºC
Exact Mass 414.13800
PSA 107.04000
LogP 4.75470

 Toxicological Information

CHEMICAL IDENTIFICATION

RTECS NUMBER :
PB0512953
CHEMICAL NAME :
Methanesulfonanilide, 5'-(2-((alpha,alpha-dimethylphenethyl)amino)-1-hydrox yethyl)-2'- hydroxy-, monohydrochloride
CAS REGISTRY NUMBER :
38241-28-0
LAST UPDATED :
199007
DATA ITEMS CITED :
1
MOLECULAR FORMULA :
C19-H26-N2-O4-S.Cl-H
MOLECULAR WEIGHT :
414.99

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Mammal - species unspecified
DOSE/DURATION :
1 gm/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
JMCMAR Journal of Medicinal Chemistry. (American Chemical Soc., Distribution Office Dept. 223, POB POB 57136, West End Stn., Washington, DC 20037) V.6- 1963- Volume(issue)/page/year: 19,626,1976

 Safety Information

Symbol GHS07
GHS07
Signal Word Warning
Hazard Statements H319
Precautionary Statements P305 + P351 + P338
Hazard Codes Xi
RIDADR NONH for all modes of transport

 Articles24

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The beta3-adrenoceptor agonist 4-[[(Hexylamino)carbonyl]amino]-N-[4-[2-[[(2S)-2-hydroxy-3-(4-hydroxyphenoxy)propyl]amino]ethyl]-phenyl]-benzenesulfonamide (L755507) and antagonist (S)-N-[4-[2-[[3-[3-(acetamidomethyl)phenoxy]-2-hydroxypropyl]amino]-ethyl]phenyl]benzenesulfonamide (L748337) activate different signaling pathways in Chinese hamster ovary-K1 cells stably expressing the human beta3-adrenoceptor.

Mol. Pharmacol. 74(5) , 1417-28, (2008)

This study identifies signaling pathways activated by the beta(2)-/beta(3)-adrenoceptor (AR) agonist zinterol, the selective beta(3)-AR agonist L755507, and the selective beta(3)-AR antagonist L748337...

Multiple signalling pathways involved in beta2-adrenoceptor-mediated glucose uptake in rat skeletal muscle cells.

Br. J. Pharmacol. 147(4) , 446-54, (2006)

1. Beta-adrenoceptor (AR) agonists increase 2-deoxy-[3H]-D-glucose uptake (GU) via beta2-AR in rat L6 cells. The beta-AR agonists, zinterol (beta2-AR) and (-)-isoprenaline, increased cAMP accumulation...

Rapid turnover of glycogen in memory formation.

Neurochem. Res. 37(11) , 2456-63, (2012)

The influence of noradrenaline acting at α(2)-AR and β(2)-ARs on the turnover of glycogen after learning has been investigated. The role of glycogen turnover in memory formation was examined using wea...

 Synonyms

N-[2-hydroxy-5-[1-hydroxy-2-[(2-methyl-1-phenylpropan-2-yl)amino]ethyl]phenyl]methanesulfonamide,hydrochloride
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