AROTINOLOL

Details

Stereochemistry	RACEMIC
Molecular Formula	C15H21N3O2S3
Molecular Weight	371.541
Optical Activity	( + / - )
Defined Stereocenters	0 / 1
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

CC(C)(C)NCC(O)CSC1=NC(=CS1)C2=CC=C(S2)C(N)=O

InChI

InChIKey=BHIAIPWSVYSKJS-UHFFFAOYSA-N

InChI=1S/C15H21N3O2S3/c1-15(2,3)17-6-9(19)7-21-14-18-10(8-22-14)11-4-5-12(23-11)13(16)20/h4-5,8-9,17,19H,6-7H2,1-3H3,(H2,16,20)

HIDE SMILES / InChI

Description
Sources: https://www.ncbi.nlm.nih.gov/pubmed/11675958
Curator's Comment: description was created based on several sources, including http://www.ncbi.nlm.nih.gov/pubmed/6200619

Arotinolol (INN, marketed under the tradename Almarl) is a medication in the class of mixed alpha/beta blockers. It is used in the treatment of high blood pressure and essential tremor. The recommended dosage is 10–30 mg per day.

Originator

Approval Year

Targets

Primary Target	Pharmacology	Condition	Potency
Adrenergic receptor beta 87 Target ID: CHEMBL2094118 Sources: http://www.ncbi.nlm.nih.gov/pubmed/6200619	Antagonist 2778
Adrenergic receptor alpha 64 Target ID: CHEMBL2095203 Sources: http://www.ncbi.nlm.nih.gov/pubmed/6200619	Antagonist 2778

Conditions

Condition	Modality	Targets	Highest Phase	Product
Hypertension 567 Sources: https://www.ncbi.nlm.nih.gov/pubmed/11675958	Primary		Preclinical	Unknown Approved Use Unknown

PubMed

Title	Date	PubMed
Synthesis and beta-adrenergic blocking action of a new thiazolylthiopropanolamine derivative.	1978 Sep	29117
Effects of beta-adrenergic blockers with different ancillary properties on lipid peroxidation in hyperthyroid rat cardiac muscle.	1989 Oct	2575990
Arotinolol is a weak partial agonist on beta 3-adrenergic receptors in brown adipocytes.	2001 Jul	11478592
Comparison of the effects of an ACE inhibitor and alphabeta blocker on the progression of renal failure with left ventricular hypertrophy: preliminary report.	2001 Mar	11325074
Clinical trial of arotinolol in the treatment of hypertension: dippers vs. non-dippers.	2001 Sep	11675958
Micellar electrokinetic capillary chromatography determination of +S and -R arotinolol in serum using UV detection and solid phase extraction.	2002 Jan	11748803
A multicenter randomized crossover multiple-dose comparison study of arotinolol and propranolol in essential tremor.	2003 Aug	12853233
Relapse of Graves' disease in a patient with pheochromocytoma.	2003 Dec	14709850
Enantioselective determination of arotinolol in human plasma by HPLC using teicoplanin chiral stationary phase.	2003 Oct	14598329
Pantothenate kinase-associated neurodegeneration initially presenting as postural tremor alone in a Japanese family with homozygous N245S substitutions in the pantothenate kinase gene.	2004 Oct 15	15465096
Spectrofluorometric determination of some beta-blockers in tablets and human plasma using 9,10-dimethoxyanthracene-2-sodium sulfonate.	2005 Apr	15881605
Effect of zonisamide on essential tremor: a pilot crossover study in comparison with arotinolol.	2005 Mar	15734668
Carvedilol, a nonselective beta-blocker, suppresses the production of tumor necrosis factor and tissue factor by inhibiting early growth response factor-1 expression in human monocytes in vitro.	2007 Apr	17383596
Effect of arotinolol on left ventricular function in patients with idiopathic dilated cardiomyopathy.	2007 Dec	18254186
Are adrenergic receptor blockers effective or contraindicated in pulmonary arterial hypertension?	2009 Dec	19940372
Effects of a pure alpha/beta-adrenergic receptor blocker on monocrotaline-induced pulmonary arterial hypertension with right ventricular hypertrophy in rats.	2009 Dec	19822980
Development of a list of potentially inappropriate drugs for the korean elderly using the delphi method.	2010 Dec	21818443
Carteolol hydrochloride suppresses the generation of reactive oxygen species and rescues cell death after ultraviolet irradiation of cultured lens epithelial cells.	2010 Oct 12	21283534
Overview of essential tremor.	2010 Sep 7	20856604

Patents

Sample Use Guides

In Vivo Use Guide

10-20 mg twice daily for 4 weeks

Route of Administration: Oral

In Vitro Use Guide

Unknown

Name

Type

Language

AROTINOLOL

Official Name

English

(±)-5-(2-((3-(TERT-BUTYLAMINO)-2-HYDROXYPROPYL)THIO)-4-THIAZOLYL)-2-THIOPHENECARBOXAMIDE

Systematic Name

English

arotinolol [INN]

Common Name

English

AROTINOLOL [MI]

Common Name

English

NSC-317940

Code

English

Arotinolol [WHO-DD]

Common Name

English

Classification Tree Code System Code

NCI_THESAURUS

C29576