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Chemical compound
Arotinolol
Trade names Almarl Other names S-596
AHFS /
Drugs.com
International Drug Names
Routes of administration
Oral (
tablets )
ATC code
Legal status
In general: ℞ (Prescription only)
Bioavailability 2 hours
Elimination half-life 10 hours
(RS )-5-(2-{[3-(tert -butylamino)-2-hydroxypropyl]sulfanyl}- 1,3-thiazol-4-yl)thiophene-2-carboxamide
CAS Number
PubChem
CID
ChemSpider
UNII
KEGG
ChEMBL
CompTox Dashboard (
EPA )
Formula C 15 H 21 N 3 O 2 S 3
Molar mass 371.53 g·mol−1 3D model (
JSmol )
CC(C)(C)NCC(CSC1=NC(=CS1)C2=CC=C(S2)C(=O)N)O
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)
Y Key:BHIAIPWSVYSKJS-UHFFFAOYSA-N
Y
N Y
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Arotinolol (
INN , marketed under the tradename Almarl ) is a
medication in the class of mixed
alpha /
beta blockers .
[1] It also acts as a
β3 receptor
agonist .
[2] A 1979 publication suggests arotinolol as having first been described in the scientific literature by
Sumitomo Chemical as "β-adrenergic blocking, antiarrhythmic compound S-596".
[3]
Medical uses
It is used in the treatment of
high blood pressure
[4] and
essential tremor .
[5]
[6] Recommended dosage is 10 to 30 mg per day.[
citation needed ]
References
^ Zhao J, Golozoubova V, Cannon B, Nedergaard J (July 2001). "Arotinolol is a weak partial agonist on beta 3-adrenergic receptors in brown adipocytes". Canadian Journal of Physiology and Pharmacology . 79 (7): 585–593.
doi :
10.1139/cjpp-79-7-585 .
PMID
11478592 .
^ Takahashi H, Yoshida T, Nishimura M, Nakanishi T, Kondo M, Yoshimura M (September 1992).
"Beta-3 adrenergic agonist, BRL-26830A, and alpha/beta blocker, arotinolol, markedly increase regional blood flow in the brown adipose tissue in anesthetized rats" . Japanese Circulation Journal . 56 (9): 936–942.
doi :
10.1253/jcj.56.936 .
PMID
1383578 .
^ Hara Y, Sato E, Miyagishi A, Aono S, Nakatani H (1979).
"新しいβ-受容体遮断薬,dl-2-(3'-t-Butylamino-2'-hydroxypropylthio)-4-(5'-carbamoyl-2'-thienyl)-thiazole hydrochloride (S-596) の薬理作用" [Pharmacological properties of dl-2-(3'-t-butylamino-2'-hydroxypropylthio)-4-(5'-carbamoyl-2'-thienyl)thiazole hydrochloride (S-596), a new β-adrenergic blocking agent]. Folia Pharmacologica Japonica (English abstract) (in Japanese). 75 (7): 707–720.
doi :
10.1254/fpj.75.707 .
ISSN
1347-8397 .
^ Wu H, Zhang Y, Huang J, Zhang Y, Liu G, Sun N, et al. (September 2001).
"Clinical trial of arotinolol in the treatment of hypertension: dippers vs. non-dippers" (PDF) . Hypertension Research . 24 (5): 605–610.
doi :
10.1291/hypres.24.605 .
PMID
11675958 .
^ Lee KS, Kim JS, Kim JW, Lee WY, Jeon BS, Kim D (August 2003). "A multicenter randomized crossover multiple-dose comparison study of arotinolol and propranolol in essential tremor". Parkinsonism & Related Disorders . 9 (6): 341–347.
doi :
10.1016/S1353-8020(03)00029-4 .
PMID
12853233 .
^
"Almarl (アルマール) Arotinolol HCl Tablets. Full Prescribing Information" (PDF) . Sumitomo Dainippon Pharma Co., Ltd. Archived from
the original (PDF) on 7 May 2012. Retrieved 6 March 2016 .
External links
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