Arotinolol

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]

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-{[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)
Chemical and physical data
FormulaC15H21N3O2S3
Molar mass371.53 g·mol−1
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) Y
  • Key:BHIAIPWSVYSKJS-UHFFFAOYSA-N Y
 NY (what is this?)  (verify)

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.

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): 585–93. doi:10.1139/cjpp-79-7-585. PMID 11478592.
  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.
  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.
  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.
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