Arotinolol

Arotinolol
Clinical data
AHFS/Drugs.com	International Drug Names
Routes of; administration	Oral (tablets)
ATC code	none;
Legal status
Legal status	In general: ℞ (Prescription only);
Pharmacokinetic data
Bioavailability	2 hours
Elimination half-life	10 hours
Identifiers
	show IUPAC name
CAS Number	68377-92-4 ;
PubChem CID	2239;
ChemSpider	2152 ;
UNII	394E3P3B99;
KEGG	D07465 ;
ChEMBL	ChEMBL93298 ;
CompTox Dashboard (EPA)	DTXSID3022619 ;
Chemical and physical data
Formula	C15H21N3O2S3
Molar mass	371.53 g·mol−1
3D model (JSmol)	Interactive image;
	show SMILES
	show InChI
	(what is this?)

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]

Uses[]

It is used in the treatment of high blood pressure^[4] and essential tremor.^[5]^[6]

Recommended dosage is 10–30 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): 585–93. 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): 936–42. 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): 605–10. 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): 341–7. 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[]

(in Japanese) Almarl Full Prescribing Information. Revised November 2009 Sumitomo Dainippon Pharma Co., Ltd.
(in Japanese) Official Sumitomo Dainippon Pharma Website
"Arotinolol Hydrochloride". Drug Monograph. Drug Information Research Institute. Archived from the original on 2011-07-22.

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[pmid11478592-1] 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): 585–93. doi:10.1139/cjpp-79-7-585. PMID 11478592.

[pmid1383578-2] 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): 936–42. doi:10.1253/jcj.56.936. PMID 1383578.

[3] 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.

[pmid11675958-4] 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): 605–10. doi:10.1291/hypres.24.605. PMID 11675958.

[pmid12853233-5] 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): 341–7. doi:10.1016/S1353-8020(03)00029-4. PMID 12853233.

[6] "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.

[1]

[2]

[3]

[4]

[5]

[6]

show v t Beta blockers (C07)
β, non-selective	Alprenolol Bopindolol Bupranolol Carteolol Cloranolol Mepindolol Nadolol Oxprenolol Penbutolol Pindolol/Iodopindolol Propranolol^# Sotalol Tertatolol Timolol^#
β₁-selective	Acebutolol Atenolol Betaxolol Bevantolol Bisoprolol^# Celiprolol Epanolol Esmolol Landiolol Metoprolol Nebivolol Practolol Talinolol
β₂-selective	Butaxamine
α₁- + β-selective	Arotinolol Carvedilol Labetalol
^#WHO-EM ^‡Withdrawn from market Clinical trials: ^†Phase III ^§Never to phase III

Clinical data

AHFS/Drugs.com	International Drug Names
Routes of administration	Oral (tablets)
ATC code	none
Legal status
Legal status	In general: ℞ (Prescription only)
Pharmacokinetic data
Bioavailability	2 hours
Elimination half-life	10 hours
Identifiers
show IUPAC name (RS)-5-(2-{[3-(tert-butylamino)-2-hydroxypropyl]sulfanyl}- 1,3-thiazol-4-yl)thiophene-2-carboxamide
CAS Number	68377-92-4^N
PubChem CID	2239
ChemSpider	2152^Y
UNII	394E3P3B99
KEGG	D07465^Y
ChEMBL	ChEMBL93298^Y
CompTox Dashboard (EPA)	DTXSID3022619
Chemical and physical data
Formula	C₁₅H₂₁N₃O₂S₃
Molar mass	371.53 g·mol⁻¹
3D model (JSmol)	Interactive image
show SMILES CC(C)(C)NCC(CSC1=NC(=CS1)C2=CC=C(S2)C(=O)N)O
show InChI 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
^NY (what is this?)