Arotinolol

Arotinolol
	File:Arotinolol.svg
Systematic (IUPAC) name
	(RS)-5-(2-{[3-(tert-butylamino)-2-hydroxypropyl]sulfanyl}- 1,3-thiazol-4-yl)thiophene-2-carboxamide
Clinical data
AHFS/Drugs.com	International Drug Names
Legal status	℞ (Prescription only);
Routes of; administration	Oral
Pharmacokinetic data
Bioavailability	2h
Half-life	10h
Identifiers
CAS Registry Number	41287-43-8 7px
ATC code	None
PubChem	CID 2239
ChemSpider	2152 7px
UNII	394E3P3B99 7px
KEGG	D07465 7px
ChEMBL	CHEMBL93298 7px
Chemical data
Formula	C15H21N3O2S3
Molecular mass	371.54 g/mol
	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) 7px ; Key:BHIAIPWSVYSKJS-UHFFFAOYSA-N 7px ;
14px (what is this?) (verify)

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Arotinolol (INN, marketed under the tradename Almarl) is a medication in the class of mixed alpha/beta blockers.^[1] 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".^[2]

Uses

It is used in the treatment of high blood pressure.^[3]

It has been proposed for use in treatment of essential tremor.^[4]

Recommended dosage 10–30 mg

References

^ Zhao, Jin; Golozoubova, Valeria; Cannon, Barbara; Nedergaard, Jan (July 2001). "Arotinolol is a weak partial agonist on beta 3-adrenergic receptors in brown adipocytes". Can J Physiol Pharmacol 79 (7): 585–593. PMID 11478592. doi:10.1139/cjpp-79-7-585. Closed access
^ Hara, Youichi; Sato, Etsuro; Miyagishi, Akira; Aono, Shunzi; Nakatani, Hiroshi (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): 707–720. ISSN 1347-8397. doi:10.1254/fpj.75.707. open access publication - free to read
^ Wu, Haiying; Zhang, Yuqing; Huang, Jianfeng; Zhang, Yuhui; Liu, Guozhang; Sun, Ningling; Yu, Zhenqui; Zhou, Yanrong (September 2001). "Clinical trial of arotinolol in the treatment of hypertension: dippers vs. non-dippers" (PDF). Hypertension Research 24 (5): 605–10. ISSN 1348-4214. PMID 11675958. doi:10.1291/hypres.24.605. open access publication - free to read
^ Lee, Kwang-Soo; Kim, Joong-Seok; Kim, Jae-Woo; Lee, Won-Yong; Jeon, Beum-Seok; Kim, Dongjae (August 2003). "A multicenter randomized crossover multiple-dose comparison study of arotinolol and propranolol in essential tremor" (PDF). Parkinsonism & Related Disorders 9 (6): 341–347. PMID 12853233. doi:10.1016/S1353-8020(03)00029-4. Closed access

External links

Invalid language code. Almarl アルマール (PDF) Dainippon Sumitomo Pharma. April 2002.
Invalid language code. Official Dainippon Sumitomo Pharma Website
http://sdic.sookmyung.ac.kr/drug_monograph/view.asp?id=92

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[pmid11478592-1] Zhao, Jin; Golozoubova, Valeria; Cannon, Barbara; Nedergaard, Jan (July 2001). "Arotinolol is a weak partial agonist on beta 3-adrenergic receptors in brown adipocytes". Can J Physiol Pharmacol 79 (7): 585–593. PMID 11478592. doi:10.1139/cjpp-79-7-585. Closed access

[2] Hara, Youichi; Sato, Etsuro; Miyagishi, Akira; Aono, Shunzi; Nakatani, Hiroshi (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): 707–720. ISSN 1347-8397. doi:10.1254/fpj.75.707. open access publication - free to read

[pmid11675958-3] Wu, Haiying; Zhang, Yuqing; Huang, Jianfeng; Zhang, Yuhui; Liu, Guozhang; Sun, Ningling; Yu, Zhenqui; Zhou, Yanrong (September 2001). "Clinical trial of arotinolol in the treatment of hypertension: dippers vs. non-dippers" (PDF). Hypertension Research 24 (5): 605–10. ISSN 1348-4214. PMID 11675958. doi:10.1291/hypres.24.605. open access publication - free to read

[pmid12853233-4] Lee, Kwang-Soo; Kim, Joong-Seok; Kim, Jae-Woo; Lee, Won-Yong; Jeon, Beum-Seok; Kim, Dongjae (August 2003). "A multicenter randomized crossover multiple-dose comparison study of arotinolol and propranolol in essential tremor" (PDF). Parkinsonism & Related Disorders 9 (6): 341–347. PMID 12853233. doi:10.1016/S1353-8020(03)00029-4. Closed access

[1]

[2]

[3]

[4]

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Arotinolol

Uses

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Systematic (IUPAC) name
File:Arotinolol.svg
(RS)-5-(2-{[3-(tert-butylamino)-2-hydroxypropyl]sulfanyl}- 1,3-thiazol-4-yl)thiophene-2-carboxamide
Clinical data
AHFS/Drugs.com	International Drug Names
Legal status	℞ (Prescription only)
Routes of administration	Oral
Pharmacokinetic data
Bioavailability	2h
Half-life	10h
Identifiers
CAS Registry Number	41287-43-8^7pxN
ATC code	None
PubChem	CID 2239
ChemSpider	2152^7pxY
UNII	394E3P3B99^7pxY
KEGG	D07465^7pxY
ChEMBL	CHEMBL93298^7pxY
Chemical data
Formula	C₁₅H₂₁N₃O₂S₃
Molecular mass	371.54 g/mol
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) ^7pxY Key:BHIAIPWSVYSKJS-UHFFFAOYSA-N ^7pxY
14pxN (what is this?) (verify)