AMOSULALOL HYDROCHLORIDE

First approved in 2023

Details

Stereochemistry	RACEMIC
Molecular Formula	C18H24N2O5S.ClH
Molecular Weight	416.92
Optical Activity	( + / - )
Defined Stereocenters	0 / 1
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

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

InChI

InChIKey=JRVCPDVOFCWKAG-UHFFFAOYSA-N

InChI=1S/C18H24N2O5S.ClH/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);1H

HIDE SMILES / InChI

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-1 171 Target ID: CHEMBL2094251 Sources: http://www.ncbi.nlm.nih.gov/pubmed/2862302	Antagonist 2849
Adrenergic receptor beta 89 Target ID: CHEMBL2094118 Sources: http://www.ncbi.nlm.nih.gov/pubmed/2862302	Antagonist 2849

Conditions

Condition	Modality	Targets	Highest Phase	Product
Hypertension 575 Sources: http://www.currenttherapeuticres.com/article/S0011-393X(05)80514-4/pdf	Primary		Approved 8583	LOWGAN Approved Use Unknown

C_max

Value	Dose	Analyte	Population
0.2 μg/mL OTHER GOV'T https://www.info.pmda.go.jp/go/interview/2/171911_2149018F1021_1_LWT_2F.pdf#page=21 \| https://pubmed.ncbi.nlm.nih.gov/6478731/	12.5 mg single, oral dose: 12.5 mg route of administration: Oral experiment type: SINGLE co-administered:	AMOSULALOL plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
0.49 μg/mL OTHER GOV'T https://www.info.pmda.go.jp/go/interview/2/171911_2149018F1021_1_LWT_2F.pdf#page=21 \| https://pubmed.ncbi.nlm.nih.gov/6478731/	25 mg single, oral dose: 25 mg route of administration: Oral experiment type: SINGLE co-administered:	AMOSULALOL plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
1.11 μg/mL OTHER GOV'T https://www.info.pmda.go.jp/go/interview/2/171911_2149018F1021_1_LWT_2F.pdf#page=21 \| https://pubmed.ncbi.nlm.nih.gov/6478731/	50 mg single, oral dose: 50 mg route of administration: Oral experiment type: SINGLE co-administered:	AMOSULALOL plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
1.87 μg/mL OTHER GOV'T https://www.info.pmda.go.jp/go/interview/2/171911_2149018F1021_1_LWT_2F.pdf#page=21 \| https://pubmed.ncbi.nlm.nih.gov/6478731/	100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered:	AMOSULALOL plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
4.09 μg/mL OTHER GOV'T https://www.info.pmda.go.jp/go/interview/2/171911_2149018F1021_1_LWT_2F.pdf#page=21 \| https://pubmed.ncbi.nlm.nih.gov/6478731/	150 mg single, oral dose: 150 mg route of administration: Oral experiment type: SINGLE co-administered:	AMOSULALOL plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
0.311 μg/mL OTHER GOV'T https://www.info.pmda.go.jp/go/interview/2/171911_2149018F1021_1_LWT_2F.pdf#page=22	30 mg single, oral dose: 30 mg route of administration: Oral experiment type: SINGLE co-administered:	AMOSULALOL plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED
0.498 μg/mL OTHER GOV'T https://www.info.pmda.go.jp/go/interview/2/171911_2149018F1021_1_LWT_2F.pdf#page=22	30 mg single, oral dose: 30 mg route of administration: Oral experiment type: SINGLE co-administered:	AMOSULALOL plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED

AUC

Value	Dose	Analyte	Population
1.67 μg × h/mL OTHER GOV'T https://www.info.pmda.go.jp/go/interview/2/171911_2149018F1021_1_LWT_2F.pdf#page=21 \| https://pubmed.ncbi.nlm.nih.gov/6478731/	12.5 mg single, oral dose: 12.5 mg route of administration: Oral experiment type: SINGLE co-administered:	AMOSULALOL plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
3.64 μg × h/mL OTHER GOV'T https://www.info.pmda.go.jp/go/interview/2/171911_2149018F1021_1_LWT_2F.pdf#page=21 \| https://pubmed.ncbi.nlm.nih.gov/6478731/	25 mg single, oral dose: 25 mg route of administration: Oral experiment type: SINGLE co-administered:	AMOSULALOL plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
6.07 μg × h/mL OTHER GOV'T https://www.info.pmda.go.jp/go/interview/2/171911_2149018F1021_1_LWT_2F.pdf#page=21 \| https://pubmed.ncbi.nlm.nih.gov/6478731/	50 mg single, oral dose: 50 mg route of administration: Oral experiment type: SINGLE co-administered:	AMOSULALOL plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
12.58 μg × h/mL OTHER GOV'T https://www.info.pmda.go.jp/go/interview/2/171911_2149018F1021_1_LWT_2F.pdf#page=21 \| https://pubmed.ncbi.nlm.nih.gov/6478731/	100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered:	AMOSULALOL plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
22.09 μg × h/mL OTHER GOV'T https://www.info.pmda.go.jp/go/interview/2/171911_2149018F1021_1_LWT_2F.pdf#page=21 \| https://pubmed.ncbi.nlm.nih.gov/6478731/	150 mg single, oral dose: 150 mg route of administration: Oral experiment type: SINGLE co-administered:	AMOSULALOL plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
2.661 μg × h/mL OTHER GOV'T https://www.info.pmda.go.jp/go/interview/2/171911_2149018F1021_1_LWT_2F.pdf#page=22	30 mg single, oral dose: 30 mg route of administration: Oral experiment type: SINGLE co-administered:	AMOSULALOL plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED
3.287 μg × h/mL OTHER GOV'T https://www.info.pmda.go.jp/go/interview/2/171911_2149018F1021_1_LWT_2F.pdf#page=22	30 mg single, oral dose: 30 mg route of administration: Oral experiment type: SINGLE co-administered:	AMOSULALOL plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED

T_1/2

Value	Dose	Analyte	Population
4.4 h OTHER GOV'T https://www.info.pmda.go.jp/go/interview/2/171911_2149018F1021_1_LWT_2F.pdf#page=21 \| https://pubmed.ncbi.nlm.nih.gov/6478731/	12.5 mg single, oral dose: 12.5 mg route of administration: Oral experiment type: SINGLE co-administered:	AMOSULALOL plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
5.2 h OTHER GOV'T https://www.info.pmda.go.jp/go/interview/2/171911_2149018F1021_1_LWT_2F.pdf#page=21 \| https://pubmed.ncbi.nlm.nih.gov/6478731/	25 mg single, oral dose: 25 mg route of administration: Oral experiment type: SINGLE co-administered:	AMOSULALOL plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
4.8 h OTHER GOV'T https://www.info.pmda.go.jp/go/interview/2/171911_2149018F1021_1_LWT_2F.pdf#page=21 \| https://pubmed.ncbi.nlm.nih.gov/6478731/	50 mg single, oral dose: 50 mg route of administration: Oral experiment type: SINGLE co-administered:	AMOSULALOL plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
5.6 h OTHER GOV'T https://www.info.pmda.go.jp/go/interview/2/171911_2149018F1021_1_LWT_2F.pdf#page=21 \| https://pubmed.ncbi.nlm.nih.gov/6478731/	100 mg single, oral dose: 100 mg route of administration: Oral experiment type: SINGLE co-administered:	AMOSULALOL plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
5.7 h OTHER GOV'T https://www.info.pmda.go.jp/go/interview/2/171911_2149018F1021_1_LWT_2F.pdf#page=21 \| https://pubmed.ncbi.nlm.nih.gov/6478731/	150 mg single, oral dose: 150 mg route of administration: Oral experiment type: SINGLE co-administered:	AMOSULALOL plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
3.6 h OTHER GOV'T https://www.info.pmda.go.jp/go/interview/2/171911_2149018F1021_1_LWT_2F.pdf#page=22	30 mg single, oral dose: 30 mg route of administration: Oral experiment type: SINGLE co-administered:	AMOSULALOL plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FED
3.1 h OTHER GOV'T https://www.info.pmda.go.jp/go/interview/2/171911_2149018F1021_1_LWT_2F.pdf#page=22	30 mg single, oral dose: 30 mg route of administration: Oral experiment type: SINGLE co-administered:	AMOSULALOL plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED

F_unbound

Value	Dose	Co-administered	Analyte	Population
2% OTHER GOV'T https://www.info.pmda.go.jp/go/interview/2/171911_2149018F1021_1_LWT_2F.pdf#page=23			AMOSULALOL plasma	Homo sapiens population: HEALTHY age: ADULT sex: UNKNOWN food status: UNKNOWN

Doses

Dose	Population	Adverse events
150 mg single, oral Highest studied dose Dose: 150 mg Route: oral Route: single Dose: 150 mg Sources: https://pubmed.ncbi.nlm.nih.gov/6478731/	healthy, ADULT Health Status: healthy Age Group: ADULT Sex: M Food Status: FASTED Sources: https://pubmed.ncbi.nlm.nih.gov/6478731/	Other AEs: Dizziness... Other AEs: Dizziness (grade 1, 50%) Sources: https://pubmed.ncbi.nlm.nih.gov/6478731/
0.16 mg/kg single, intravenous Highest studied dose Dose: 0.16 mg/kg Route: intravenous Route: single Dose: 0.16 mg/kg Sources: https://pubmed.ncbi.nlm.nih.gov/6478731/	healthy, ADULT Health Status: healthy Age Group: ADULT Sex: M Food Status: FASTED Sources: https://pubmed.ncbi.nlm.nih.gov/6478731/	Sources: https://pubmed.ncbi.nlm.nih.gov/6478731/

AEs

AE	Significance	Dose	Population
Dizziness	grade 1, 50%	150 mg single, oral Highest studied dose Dose: 150 mg Route: oral Route: single Dose: 150 mg Sources: https://pubmed.ncbi.nlm.nih.gov/6478731/	healthy, ADULT Health Status: healthy Age Group: ADULT Sex: M Food Status: FASTED Sources: https://pubmed.ncbi.nlm.nih.gov/6478731/

PubMed

Title	Date	PubMed
Development of a list of potentially inappropriate drugs for the korean elderly using the delphi method.	2010-12	21818443
Pharmacokinetics and metabolism of an alpha,beta-blocker, amosulalol hydrochloride, in mice: biliary excretion of carbamoyl glucuronide.	2007-08	17666826
Determination of amosulalol in human plasma using solid-phase extraction combined with liquid chromatography and ultraviolet detection.	2005-04-25	15734149
Emotional stress activates MAP kinase in the rat heart.	2001-09-07	11693273

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.

Name

Type

Language

AMOSULALOL MONOHYDROCHLORIDE

Preferred Name

English

AMOSULALOL HYDROCHLORIDE

Common Name

English

AMOSULALOL HCL

Common Name

English

YM-09538

Code

English

AMOSULALOL MONOHYDROCHLORIDE [MI]

Common Name

English

AMOSULALOL HYDROCHLORIDE [JAN]

Common Name

English

Amosulalol hydrochloride [WHO-DD]

Common Name

English

AMOSULALOL HYDROCHLORIDE [MART.]

Common Name

English

BENZENESULFONAMIDE, 5-(1-HYDROXY-2-((2-(2-METHOXYPHENOXY)ETHYL)AMINO)ETHYL)-2-METHYL-, HYDROCHLORIDE (1:1)

Systematic Name

English

BENZENESULFONAMIDE, 5-(1-HYDROXY-2-((2-(2-METHOXYPHENOXY)ETHYL)AMINO)ETHYL)-2-METHYL-, HYDROCHLORIDE, (±)-

Systematic Name

English

LOWGAN

Brand Name

English

Code System Code Type Description

FDA UNII

4O4S698PEE