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Amosulalol

Names

[ CAS No. ]:
85320-68-9

[ Name ]:
Amosulalol

[Synonym ]:
Amosulalolum [Latin]
5-[1-hydroxy-2-[2-(2-methoxyphenoxyl)ethylamino]ethyl]-2-methylbenzenesulfonamide
(+-)-5-(1-Hydroxy-2-((2-(o-methoxyphenoxy)ethyl)amino)ethyl)-o-toluenesulfonamide
Amosulalolum
Lowgan
Amosulalol
(+/-)-5-[1-hydroxy-2-[[2-(2-methoxyphenoxy)ethyl]amino]ethyl]-2-methylbenzenesulfonamide
Amosulalol [INN]

Biological Activity

[Description]:

Amosulalol (YM 09538) is an orally active and dual inhibitor of α1/β1-Adrenergic Receptor. Amosulalol exhibits antihypertensive activity via α1-Adrenergic Receptor inhibition. Amosulalol decreases reflexogenic increases in heart rate and plasma renin activity (PRA) via β1-Adrenergic Receptor inhibition in spontaneously hypertensive rats (SHR)[1].

[Related Catalog]:

Research Areas >> Cardiovascular Disease
Signaling Pathways >> GPCR/G Protein >> Adrenergic Receptor

[Target]

α1-adrenergic receptor

Beta-1 adrenergic receptor


[In Vivo]

Amosulalol (3-30 mg/kg; 口服; 单剂量) 降低高血压大鼠的急性收缩压[1]。 Amosulalol (50 mg/kg; 口服; 每天 2 次, 共 12 周) 产生不耐受的降压作用，还降低高血压大鼠模型中心率和血浆肾素活性 (PRA) 增加[1]。

[References]

[1]. Honda K, et al. Autonomic and antihypertensive activity of oral amosulalol (YM-09538), a combined alpha- and beta-adrenoceptor blocking agent in conscious rats. Jpn J Pharmacol. 1985 May;38(1):31-41.  

Chemical & Physical Properties

[ Density]:
1.268g/cm3

[ Boiling Point ]:
608.7ºC at 760mmHg

[ Molecular Formula ]:
C18H24N2O5S

[ Molecular Weight ]:
380.45900

[ Flash Point ]:
321.9ºC

[ Exact Mass ]:
380.14100

[ PSA ]:
119.26000

[ LogP ]:
3.52500

Synthetic Route

Click to get detail synthetic route

Precursor & DownStream

Precursor

DownStream

Related Compounds