Arotinolol

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Arotinolol
Clinical data

AHFS/Drugs.com	International Drug Names
Routes of administration	Oral (tablets)
ATC code	none
Legal status
Legal status	℞ (Prescription only)
Pharmacokinetic data
Bioavailability	2 hours
Biological half-life	10 hours
Identifiers
IUPAC name (RS)-5-(2-{[3-(tert-butylamino)-2-hydroxypropyl]sulfanyl}- 1,3-thiazol-4-yl)thiophene-2-carboxamide
CAS Number	41287-43-8^N
PubChem (CID)	2239
ChemSpider	2152^Y
UNII	394E3P3B99^Y
KEGG	D07465^Y
ChEMBL	CHEMBL93298^Y
Chemical and physical data
Formula	C₁₅H₂₁N₃O₂S₃
Molar mass	371.54 g/mol
3D model (Jmol)	Interactive image
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)

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[edit]

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

Recommended dosage is 10–30 mg per day.

References[edit]

^ 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. 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, 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. doi:10.1254/fpj.75.707. ISSN 1347-8397.
^ 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. doi:10.1291/hypres.24.605. ISSN 1348-4214. PMID 11675958.
^ 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. 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. Retrieved 6 March 2016.

External links[edit]

(Japanese) Almarl Full Prescribing Information. Revised November 2009 Sumitomo Dainippon Pharma Co., Ltd.
(Japanese) Official Sumitomo Dainippon Pharma Website
https://web.archive.org/web/20110722132720/http://sdic.sookmyung.ac.kr/drug_monograph/view.asp?id=92

v t e 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 S-Atenolol Talinolol

β₂-selective	Butaxamine

α₁- + β-selective	Arotinolol Carvedilol Labetalol

^#WHO-EM ^‡Withdrawn from market Clinical trials: ^†Phase III ^§Never to phase III

Adrenergic receptor modulators

α₁

Agonists 6-FNE Amidephrine Anisodine Buspirone Cirazoline Corbadrine Dexisometheptene Dipivefrine Dopamine Droxidopa (L-DOPS) Ephedrine Epinephrine Etilefrine Etilevodopa Ethylnorepinephrine Indanidine Isometheptene L-DOPA (levodopa) L-Phenylalanine L-Tyrosine Melevodopa Metaraminol Methoxamine Methyldopa Midodrine Naphazoline Norepinephrine Octopamine (drug) Oxymetazoline Phenylephrine Phenylpropanolamine Pseudoephedrine Synephrine Tetryzoline Tiamenidine XP21279 Xylometazoline

Antagonists Abanoquil Adimolol Ajmalicine Alfuzosin Amosulalol Anisodamine Arotinolol Atiprosin Atypical antipsychotics (e.g., clozapine, olanzapine, quetiapine, risperidone) Benoxathian Buflomedil Bunazosin Carvedilol Corynanthine Dapiprazole Domesticine Doxazosin Ergolines (e.g., ergotamine, dihydroergotamine, lisuride, terguride) Etoperidone Eugenodilol Fenspiride Hydroxyzine Indoramin Ketanserin L-765,314 Labetalol mCPP Mepiprazole Metazosin Monatepil Moxisylyte Naftopidil Nantenine Nefazodone Neldazosin Niaprazine Nicergoline Niguldipine Pardoprunox Pelanserin Phendioxan Phenoxybenzamine Phentolamine Piperoxan Prazosin Quinazosin Ritanserin Silodosin Spiperone Talipexole Tamsulosin Terazosin Tiodazosin Tolazoline Trazodone Tetracyclic antidepressants (e.g., amoxapine, maprotiline, mianserin) Tricyclic antidepressants (e.g., amitriptyline, clomipramine, doxepin, imipramine, trimipramine) Trimazosin Typical antipsychotics (e.g., chlorpromazine, fluphenazine, loxapine, thioridazine) Urapidil WB-4101 Zolertine

α₂

Agonists (R)-3-Nitrobiphenyline 4-NEMD 6-FNE Amitraz Apraclonidine Brimonidine Cannabivarin Clonidine Corbadrine Detomidine Dexmedetomidine Dihydroergotamine Dipivefrine Dopamine Droxidopa (L-DOPS) Etilevodopa Ephedrine Ergotamine Epinephrine Etilefrine Ethylnorepinephrine Guanabenz Guanfacine Guanoxabenz L-DOPA (levodopa) L-Phenylalanine L-Tyrosine Lofexidine Medetomidine Melevodopa Methyldopa Mivazerol Naphazoline Norepinephrine Oxymetazoline Phenylpropanolamine Piperoxan Pseudoephedrine Rilmenidine Romifidine Talipexole Tetrahydrozoline Tiamenidine Tizanidine Tolonidine Urapidil XP21279 Xylazine Xylometazoline

Antagonists 1-PP Adimolol Aptazapine Atipamezole Atypical antipsychotics (e.g., asenapine, clozapine, lurasidone, paliperidone, quetiapine, risperidone, zotepine) Azapirones (e.g., buspirone, tandospirone) BRL-44408 Buflomedil Cirazoline Efaroxan Esmirtazapine Fenmetozole Fluparoxan Idazoxan mCPP Mianserin Mirtazapine NAN-190 Olanzapine Pardoprunox Phentolamine Phenoxybenzamine Piperoxan Piribedil Rauwolscine Rotigotine SB-269970 Setiptiline Spiroxatrine Sunepitron Tolazoline Typical antipsychotics (e.g., chlorpromazine, fluphenazine, loxapine, thioridazine) Yohimbine

Agonists Abediterol Alifedrine Amibegron Arbutamine Arformoterol Arotinolol BAAM Bambuterol Befunolol Bitolterol Broxaterol Buphenine Carbuterol Carmoterol Cimaterol Clenbuterol Corbadrine Denopamine Dipivefrine Dobutamine Dopamine Dopexamine Droxidopa (L-DOPS) Ephedrine Epinephrine Etafedrine Etilefrine Etilevodopa Ethylnorepinephrine Fenoterol Formoterol Hexoprenaline Higenamine Indacaterol Isoetarine Isoprenaline Isoxsuprine L-DOPA (levodopa) L-Phenylalanine L-Tyrosine Levosalbutamol Mabuterol Melevodopa Methoxyphenamine Methyldopa Mirabegron Norepinephrine Orciprenaline Oxyfedrine PF-610355 Phenylpropanolamine Pirbuterol Prenalterol Ractopamine Procaterol Pseudoephedrine Reproterol Rimiterol Ritodrine Salbutamol Salmeterol Solabegron Terbutaline Tretoquinol Tulobuterol Vilanterol Xamoterol XP21279 Zilpaterol Zinterol

Antagonists Acebutolol Adaprolol Adimolol Afurolol Alprenolol Alprenoxime Amosulalol Ancarolol Arnolol Arotinolol Atenolol Befunolol Betaxolol Bevantolol Bisoprolol Bopindolol Bornaprolol Brefonalol Bucindolol Bucumolol Bufetolol Bufuralol Bunitrolol Bunolol Bupranolol Butaxamine Butidrine Butofilolol Capsinolol Carazolol Carpindolol Carteolol Carvedilol Celiprolol Cetamolol Cicloprolol Cinamolol Cloranolol Cyanopindolol Dalbraminol Dexpropranolol Diacetolol Dichloroisoprenaline Dihydroalprenolol Dilevalol Diprafenone Draquinolol Ecastolol Epanolol Ericolol Ersentilide Esatenolol Esprolol Eugenodilol Exaprolol Falintolol Flestolol Flusoxolol Hydroxycarteolol Hydroxytertatolol ICI-118,551 Idropranolol Indenolol Indopanolol Iodocyanopindolol Iprocrolol Isoxaprolol Isamoltane Labetalol Landiolol Levobetaxolol Levobunolol Levomoprolol Medroxalol Mepindolol Metipranolol Metoprolol Moprolol Nadolol Nadoxolol Nebivolol Nifenalol Nipradilol Oxprenolol Pacrinolol Pafenolol Pamatolol Pargolol Penbutolol Pindolol Practolol Primidolol Procinolol Pronethalol Propafenone Propranolol Ridazolol Ronactolol Soquinolol Sotalol Spirendolol SR 59230A Sulfinalol Talinolol Tazolol Tertatolol Tienoxolol Tilisolol Timolol Tiprenolol Tolamolol Toliprolol Xibenolol Xipranolol

See also: List of adrenergic drugs
Dopaminergics
Melatonergics
Serotonergics
Monoamine reuptake and release modulators
Monoamine metabolism modulators
Monoamine neurotoxins

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