AMOSULALOL

First approved in 2023

Details

Stereochemistry	RACEMIC
Molecular Formula	C18H24N2O5S
Molecular Weight	380.459
Optical Activity	( + / - )
Defined Stereocenters	0 / 1
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

COC1=C(OCCNCC(O)C2=CC=C(C)C(=C2)S(N)(=O)=O)C=CC=C1

InChI

InChIKey=LVEXHFZHOIWIIP-UHFFFAOYSA-N

InChI=1S/C18H24N2O5S/c1-13-7-8-14(11-18(13)26(19,22)23)15(21)12-20-9-10-25-17-6-4-3-5-16(17)24-2/h3-8,11,15,20-21H,9-10,12H2,1-2H3,(H2,19,22,23)

HIDE SMILES / InChI

Molecular Formula	C18H24N2O5S
Molecular Weight	380.459
Charge	0
Count

Stereochemistry	RACEMIC
Additional Stereochemistry	No
Defined Stereocenters	0 / 1
E/Z Centers	0
Optical Activity	( + / - )

Description
Sources: http://www.ncbi.nlm.nih.gov/pubmed/2862302
Curator's Comment: description was created based on several sources, including, http://www.currenttherapeuticres.com/article/S0011-393X(05)80514-4/pdf

Amosulalol is a beta- and alpha-1 adrenoceptor-blocking agent developed for the treatment of hypertension. Amosulalol does not cross blood brain barrier and does not have adverse affect on CNS system.The drug is marketed under the name Lowgan in Japan and Korea.

CNS Activity

Originator

Approval Year

Targets

Primary Target	Pharmacology	Condition	Potency
Adrenergic receptor alpha-1 169 Target ID: CHEMBL2094251 Sources: http://www.ncbi.nlm.nih.gov/pubmed/2862302	Antagonist 2778
Adrenergic receptor beta 87 Target ID: CHEMBL2094118 Sources: http://www.ncbi.nlm.nih.gov/pubmed/2862302	Antagonist 2778

Conditions

Condition	Modality	Targets	Highest Phase	Product
Hypertension 567 Sources: http://www.currenttherapeuticres.com/article/S0011-393X(05)80514-4/pdf	Primary		Approved 8429	LOWGAN Approved Use Unknown

PubMed

Title	Date	PubMed
Emotional stress activates MAP kinase in the rat heart.	2001 Sep 7	11693273
Determination of amosulalol in human plasma using solid-phase extraction combined with liquid chromatography and ultraviolet detection.	2005 Apr 25	15734149
Pharmacokinetics and metabolism of an alpha,beta-blocker, amosulalol hydrochloride, in mice: biliary excretion of carbamoyl glucuronide.	2007 Aug	17666826
Development of a list of potentially inappropriate drugs for the korean elderly using the delphi method.	2010 Dec	21818443

Patents

Sample Use Guides

In Vivo Use Guide

The daily dosage is from 40 mg to 60 mg.

Route of Administration: Oral

In Vitro Use Guide

Smooth muscle cells of the guinea-pig mesenteric artery and vein and the main pulmonary artery were incubated with amosulalol. In the mesenteric artery, the noradrenaline-induced depolarization was inhibited significantly by amosulalol in concentrations over 10(-8)M, and the depolarization ceased by amosulalol in concentrations over 10(-7)M. In the pulmonary artery, membrane depolarizations produced by 5 x 10(-6)M noradrenaline were significantly reduced by amosulalol in concentrations over 10(-7)M, and ceased after pretreatment with 10(-5)M amosulalol. In the mesenteric vein, membrane depolarization produced by exogenously applied noradrenaline (10(-5)M) was not blocked by amosulalol, up to 10(-5)M.

Substance Class	Chemical Created by `admin` on `Fri Dec 15 15:29:12 GMT 2023` Edited by `admin` on `Fri Dec 15 15:29:12 GMT 2023`
Record UNII	C69JI1BAU8
Record Status	`Validated (UNII)`
Record Version

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Name

Type

Language

AMOSULALOL

Official Name

English

AMOSULALOL [MI]

Common Name

English

(±)-5-(1-HYDROXY-2-((2-(O-METHOXYPHENOXY)ETHYL)AMINO)ETHYL)-O-TOLUENESULFONAMIDE

Common Name

English

Amosulalol [WHO-DD]

Common Name

English

amosulalol [INN]

Common Name

English

Classification Tree Code System Code

NCI_THESAURUS

C72900