Page last updated: 2024-11-04

arotinolol

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth Market Indicators

Description

arotinolol: structure given in first source; arotinolol is the (+-)-isomer [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID2239
CHEMBL ID93298
CHEBI ID135569
SCHEMBL ID80713
MeSH IDM0082824

Synonyms (49)

Synonym
CHEMBL93298
5-[2-({3-[(1,1-dimethylethyl)amino]-2-hydroxypropyl}thio)-1,3-thiazol-4-yl]thiophene-2-carboxamide
arotinolol
nsc-317940
nsc317940
68377-92-4
D07465
arotinolol (inn)
arotinololum [latin]
2-thiophenecarboxamide, 5-(2-((3-((1,1-dimethylethyl)amino)-2-hydroxypropyl)thio)-4-thiazolyl)-
2-(3-tert-butylamino-2-hydroxypropylthio)-4-(5-carbamoyl-2-thienyl)thiazole
arotinolol [inn]
(+-)-5-(2-((3-(tert-butylamino)-2-hydroxypropyl)thio)-4-thiazolyl)-2-thiophenecarboxamide
c15h21n3o2s3
L013390
CHEBI:135569
5-[2-[3-(tert-butylamino)-2-hydroxypropyl]sulfanyl-1,3-thiazol-4-yl]thiophene-2-carboxamide
cas_52560-77-7
bdbm81885
394e3p3b99 ,
nsc 317940
unii-394e3p3b99
(+-)-arotinolol
arotinololum
AKOS016014208
FT-0601557
arotinolol [mi]
(+/-)-5-(2-((3-(tert-butylamino)-2-hydroxypropyl)thio)-4-thiazolyl)-2-thiophenecarboxamide
arotinolol [who-dd]
SCHEMBL80713
5-(2-((3-(tert-butylamino)-2-hydroxypropyl)thio)thiazol-4-yl)thiophene-2-carboxamide
DTXSID3022619
DB09204
mfcd00865895
5-(2-{[3-(tert-butylamino)-2-hydroxypropyl]sulfanyl}-1,3-thiazol-4-yl)-2-thiophenecarboxamide
SR-01000944984-1
sr-01000944984
5-(2-(3-(tert-butylamino)-2-hydroxypropylthio)thiazol-4-yl)thiophene-2-carboxamide
Q4795601
HY-122537A
CS-0102757
AMY14182
C76165
68377-92-4 (free base)
5-(2-((3-(tert-butylamino)-2-hydroxypropyl)thio)-4-thiazolyl)-2-thiophenecarboxamide
arotinolol free base
2-thiophenecarboxamide,5-[2-[[3-[(1,1-dimethylethyl)amino]-2-hydroxypropyl]thio]-4-thiazolyl]-
A867056
BS-42433

Research Excerpts

Overview

Arotinolol (S-596, ARL) is a beta-adrenoceptor blocking drug. It may be classified into the fourth generation.

ExcerptReferenceRelevance
"Arotinolol appears to be a useful drug in the long-term treatment of hypertension in patients with chronic renal failure."( Effects of long-term therapy with arotinolol on blood pressure and renal function in hypertensive patients with chronic renal failure.
Shiigai, T,
)
1.13
"Arotinolol (S-596, ARL) is a beta-adrenoceptor blocking drug with weak alpha-adrenoceptor blocking activity, and may be classified into the fourth generation. "( Chronic effects of arotinolol (S-596) in spontaneously hypertensive rats.
Kawashima, K; Kishi, K; Saito, K; Sokabe, H, 1985
)
2.04

Pharmacokinetics

ExcerptReferenceRelevance
" The method was demonstrated with acceptable accuracy, precision and specificity for the determination of arotinolol enantiomers and has been successfully applied to a stereoselective pharmacokinetic study."( Enantiospecific determination of arotinolol in rat plasma by LC-MS/MS: application to a stereoselective pharmacokinetic study.
Hong, Z; Qian, Z; Shen, X; Xu, Y; Zhang, J; Zheng, L, 2015
)
0.91

Compound-Compound Interactions

The therapy approached of arotinolol combined with nifedipine or amlodipine could be effective and well-tolerated, and they can be used as the better chosen antihypertensive drug.

ExcerptReferenceRelevance
"The current study addresses the 24-h antihypertensive efficacy and safety of arotinolol combined with a different calcium channel blocker."( The efficacy and safety of arotinolol combined with a different calcium channel blocker in the treatment of Chinese patients with essential hypertension: a one-year follow-up study.
Chen, W; Fang, H; Liu, X; Xu, W, 2014
)
0.93
"The result showed that the effective rate of one year antihypertensive treatment of arotinolol combined with nifedipine was 51 of 53, significantly effective (pā€‰<ā€‰0."( The efficacy and safety of arotinolol combined with a different calcium channel blocker in the treatment of Chinese patients with essential hypertension: a one-year follow-up study.
Chen, W; Fang, H; Liu, X; Xu, W, 2014
)
0.92
"The therapy approached of arotinolol combined with nifedipine or amlodipine could be effective and well-tolerated, and they can be used as the better chosen antihypertensive drug."( The efficacy and safety of arotinolol combined with a different calcium channel blocker in the treatment of Chinese patients with essential hypertension: a one-year follow-up study.
Chen, W; Fang, H; Liu, X; Xu, W, 2014
)
1

Dosage Studied

Arotinolol, which can be dosed twice daily, is an effective antihypertensive agent. It effectively lowers blood pressure during the day while reducing nighttime blood pressure more in non-dippers than in dippers.

ExcerptRelevanceReference
" At dosage levels similar to arotinolol, both pindolol and labetalol were less effective in preventing cerebral lesions despite lower blood pressure."( Prevention of cerebral stroke by arotinolol in salt-loaded SHRSP.
Hara, Y; Maniwa, T; Miyagishi, A; Noguchi, T, 1991
)
0.85
"In pithed rats two recently-introduced beta-blockers, nipradilol and arotinolol, as well as labetalol shifted the pressor dose-response curve for phenylephrine to the right."( Alpha-blockade and vasodilatation induced by nipradilol, arotinolol and labetalol in pithed rats.
Chin, WP; Imai, S; Nakagawa, Y; Nakahara, H, 1985
)
0.75
" In spinal cats the tyramine and noradrenaline dose-response curve was shifted to the right by S-596."( Effects of the new beta-adrenoceptor blocking agent, S-596 on the peripheral autonomic nervous system and smooth muscles.
Hara, Y; Miyagishi, A; Nakahara, H; Nakatani, H, 1983
)
0.27
" In conclusion, Arotinolol, which can be dosed twice daily, is an effective antihypertensive agent which effectively lowers blood pressure during the day while reducing nighttime blood pressure more in non-dippers than in dippers, without excessive lowering blood pressure in the latter."( Clinical trial of arotinolol in the treatment of hypertension: dippers vs. non-dippers.
Huang, J; Liu, G; Sun, N; Wu, H; Yu, Z; Zhang, Y; Zhou, Y, 2001
)
0.99
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Drug Classes (2)

ClassDescription
thiophenesCompounds containing at least one thiophene ring.
aromatic amideAn amide in which the amide linkage is bonded directly to an aromatic system.
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Bioassays (2)

Assay IDTitleYearJournalArticle
AID1871989Antimycobacterial activity against Mycobacterium tuberculosis H37Rv by microplate alamar blue assay2022European journal of medicinal chemistry, Feb-05, Volume: 229Tuberculosis drug discovery: Progression and future interventions in the wake of emerging resistance.
AID227700Anticonvulsant activity2003Bioorganic & medicinal chemistry letters, Aug-18, Volume: 13, Issue:16
Topological virtual screening: a way to find new anticonvulsant drugs from chemical diversity.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (64)

TimeframeStudies, This Drug (%)All Drugs %
pre-199023 (35.94)18.7374
1990's20 (31.25)18.2507
2000's15 (23.44)29.6817
2010's5 (7.81)24.3611
2020's1 (1.56)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 34.03

According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be moderate demand-to-supply ratio for research on this compound.

MetricThis Compound (vs All)
Research Demand Index34.03 (24.57)
Research Supply Index4.39 (2.92)
Research Growth Index4.33 (4.65)
Search Engine Demand Index45.13 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (34.03)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials12 (17.65%)5.53%
Reviews1 (1.47%)6.00%
Case Studies4 (5.88%)4.05%
Observational0 (0.00%)0.25%
Other51 (75.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Clinical Trials (2)

Trial Overview

TrialPhaseEnrollmentStudy TypeStart DateStatus
Effect of Arotinolol Hydrochloride on Cardiovascular Events in Hypertensive Haemodialysis Patients: An Open Labelled, Randomized, Multicentered, Controlled Trial [NCT01351636]Phase 4300 participants (Actual)Interventional2011-04-30Completed
Efficacy and Safety of Arotinolol Hydrochloride on Morning Blood Pressure and Heart Rate in Patients With Essential Hypertension [NCT02612298]Phase 4198 participants (Actual)Interventional2015-08-31Completed
[information is prepared from clinicaltrials.gov, extracted Sep-2024]