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Arotinolol

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Chemical compound Pharmaceutical compound
Arotinolol
Clinical data
Trade namesAlmarl
Other namesS-596
AHFS/Drugs.comInternational Drug Names
Routes of
administration		Oral (tablets)
ATC code
  • none
Legal status
Legal status
  • In general: ℞ (Prescription only)
Pharmacokinetic data
Bioavailability2 hours
Elimination half-life10 hours
Identifiers
IUPAC name
  • (RS)-5-(2-{sulfanyl}- 1,3-thiazol-4-yl)thiophene-2-carboxamide
CAS Number
PubChem CID
ChemSpider
UNII
KEGG
ChEMBL
CompTox Dashboard (EPA)
Chemical and physical data
FormulaC15H21N3O2S3
Molar mass371.53 g·mol
3D model (JSmol)
SMILES
  • CC(C)(C)NCC(CSC1=NC(=CS1)C2=CC=C(S2)C(=O)N)O
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)
  • Key:BHIAIPWSVYSKJS-UHFFFAOYSA-N
  (what is this?)  (verify)

Arotinolol (INN, marketed under the tradename Almarl) is a medication in the class of mixed alpha/beta blockers. It also acts as a β3 receptor agonist. 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".

Medical uses

It is used in the treatment of high blood pressure and essential tremor. Recommended dosage is 10 to 30 mg per day.

References

  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): 585–593. doi:10.1139/cjpp-79-7-585. PMID 11478592.Closed access icon
  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): 936–942. 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.Open access icon
  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): 605–610. doi:10.1291/hypres.24.605. PMID 11675958.Open access icon
  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): 341–347. doi:10.1016/S1353-8020(03)00029-4. PMID 12853233.Closed access icon
  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.

External links

Beta blockers (C07)
β, non-selective
β1-selective
β2-selective
α1- + β-selective
Adrenergic receptor modulators
α1
Agonists
Antagonists
α2
Agonists
Antagonists
β
Agonists
Antagonists
Categories: