- 日
- 関
Wikipedia preview
出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2012/08/06 14:32:35」(JST)
[Wiki en表示]
Tulobuterol
|
| Systematic (IUPAC) name |
| (RS)-2-(tert-butylamino)-1-(2-chlorophenyl)ethanol |
| Clinical data |
| AHFS/Drugs.com |
International Drug Names |
| Pregnancy cat. |
? |
| Legal status |
? |
| Routes |
Inhaled, oral |
| Identifiers |
| CAS number |
41570-61-0 N |
| ATC code |
R03AC11 |
| PubChem |
CID 5606 |
| ChemSpider |
5404 Y |
| UNII |
591I9SU0F7 Y |
| KEGG |
D02151 Y |
| ChEMBL |
CHEMBL1159717 Y |
| Chemical data |
| Formula |
C12H18ClNO |
| Mol. mass |
227.730 g/mol |
|
|
InChI
-
InChI=1S/C12H18ClNO/c1-12(2,3)14-8-11(15)9-6-4-5-7-10(9)13/h4-7,11,14-15H,8H2,1-3H3 Y
Key:YREYLAVBNPACJM-UHFFFAOYSA-N Y
|
N (what is this?) (verify)
|
Tulobuterol (INN) is a long-acting beta2-adrenergic receptor agonist, marketed in Japan as a transdermal patch under the name Hokunalin tape (ホクナリンテープ).
|
Adrenergics
|
|
|
Receptor ligands
|
|
|
α1
|
- Agonists: 5-FNE
- 6-FNE
- Amidephrine
- Anisodamine
- Anisodine
- Cirazoline
- Dipivefrine
- Dopamine
- Ephedrine
- Epinephrine
- Etilefrine
- Ethylnorepinephrine
- Indanidine
- Levonordefrin
- Metaraminol
- Methoxamine
- Methyldopa
- Midodrine
- Naphazoline
- Norepinephrine
- Octopamine
- Oxymetazoline
- Phenylephrine
- Phenylpropanolamine
- Pseudoephedrine
- Synephrine
- Tetrahydrozoline
Antagonists: Abanoquil
- Adimolol
- Ajmalicine
- Alfuzosin
- Amosulalol
- Arotinolol
- Atiprosin
- Benoxathian
- Buflomedil
- Bunazosin
- Carvedilol
- CI-926
- Corynanthine
- Dapiprazole
- DL-017
- Domesticine
- Doxazosin
- Eugenodilol
- Fenspiride
- GYKI-12,743
- GYKI-16,084
- Indoramin
- Ketanserin
- L-765,314
- Labetalol
- Mephendioxan
- Metazosin
- Monatepil
- Moxisylyte
- Naftopidil
- Nantenine
- Neldazosin
- Nicergoline
- Niguldipine
- Pelanserin
- Phendioxan
- Phenoxybenzamine
- Phentolamine
- Piperoxan
- Prazosin
- Quinazosin
- Ritanserin
- RS-97,078
- SGB-1,534
- Silodosin
- SL-89.0591
- Spiperone
- Talipexole
- Tamsulosin
- Terazosin
- Tibalosin
- Tiodazosin
- Tipentosin
- Tolazoline
- Trimazosin
- Upidosin
- Urapidil
- Zolertine
* Note that many TCAs, TeCAs, antipsychotics, ergolines, and some piperazines like buspirone and trazodone all antagonize α1-adrenergic receptors as well, which contributes to their side effects such as orthostatic hypotension.
|
|
|
α2
|
- Agonists: (R)-3-Nitrobiphenyline
- 4-NEMD
- 6-FNE
- Amitraz
- Apraclonidine
- Brimonidine
- Cannabivarin
- Clonidine
- Detomidine
- Dexmedetomidine
- Dihydroergotamine
- Dipivefrine
- Dopamine
- Ephedrine
- Ergotamine
- Epinephrine
- Esproquin
- Etilefrine
- Ethylnorepinephrine
- Guanabenz
- Guanfacine
- Guanoxabenz
- Levonordefrin
- Lofexidine
- Medetomidine
- Methyldopa
- Mivazerol
- Naphazoline
- Norepinephrine
- Oxymetazoline
- Phenylpropanolamine
- Piperoxan
- Pseudoephedrine
- Rilmenidine
- Romifidine
- Talipexole
- Tetrahydrozoline
- Tizanidine
- Tolonidine
- Urapidil
- Xylazine
- Xylometazoline
Antagonists: 1-PP
- Adimolol
- Aptazapine
- Atipamezole
- BRL-44408
- Buflomedil
- Cirazoline
- Efaroxan
- Esmirtazapine
- Fenmetozole
- Fluparoxan
- GYKI-12,743
- GYKI-16,084
- Idazoxan
- Mianserin
- Mirtazapine
- MK-912
- NAN-190
- Olanzapine
- Phentolamine
- Phenoxybenzamine
- Piperoxan
- Piribedil
- Rauwolscine
- Rotigotine
- SB-269,970
- Setiptiline
- Spiroxatrine
- Sunepitron
- Tolazoline
- Yohimbine
* Note that many atypical antipsychotics and azapirones like buspirone (via metabolite 1-PP) antagonize α2-adrenergic receptors as well.
|
|
|
β
|
|
|
|
|
|
Reuptake inhibitors
|
|
|
NET
|
- Selective norepinephrine reuptake inhibitors: Amedalin
- Atomoxetine (Tomoxetine)
- Ciclazindol
- Daledalin
- Edivoxetine
- Esreboxetine
- Lortalamine
- Mazindol
- Nisoxetine
- Reboxetine
- Talopram
- Talsupram
- Tandamine
- Viloxazine; Norepinephrine-dopamine reuptake inhibitors: Amineptine
- Bupropion (Amfebutamone)
- Fencamine
- Fencamfamine
- Lefetamine
- Levophacetoperane
- LR-5182
- Manifaxine
- Methylphenidate
- Nomifensine
- O-2172
- Radafaxine; Serotonin-norepinephrine reuptake inhibitors: Bicifadine
- Desvenlafaxine
- Duloxetine
- Eclanamine
- Levomilnacipran
- Milnacipran
- Sibutramine
- Venlafaxine; Serotonin-norepinephrine-dopamine reuptake inhibitors: Brasofensine
- Diclofensine
- DOV-102,677
- DOV-21,947
- DOV-216,303
- JNJ-7925476
- JZ-IV-10
- Methylnaphthidate
- Naphyrone
- NS-2359
- PRC200-SS
- SEP-225,289
- SEP-227,162
- Tesofensine; Tricyclic antidepressants: Amitriptyline
- Butriptyline
- Cianopramine
- Clomipramine
- Desipramine
- Dosulepin
- Doxepin
- Imipramine
- Lofepramine
- melitracen
- Nortriptyline
- Protriptyline
- Trimipramine; Tetracyclic antidepressants: Amoxapine
- Maprotiline
- Mianserin
- Oxaprotiline
- Setiptiline; Others: Cocaine
- CP-39,332
- EXP-561
- Fezolamine
- Ginkgo biloba
- Indeloxazine
- Nefazodone
- Nefopam
- Pridefrine
- Tapentadol
- Tedatioxetine
- Teniloxazine
- Tofenacin
- Tramadol
- Ziprasidone
|
|
|
VMAT
|
- Ibogaine
- Reserpine
- Tetrabenazine
|
|
|
|
|
|
|
|
Enzyme inhibitors
|
|
|
Anabolism
|
|
PAH
|
|
|
|
TH
|
- 3-Iodotyrosine
- Aquayamycin
- Bulbocapnine
- Metirosine
- Oudenone
|
|
|
AAAD
|
- Benserazide
- Carbidopa
- DFMD
- Genistein
- Methyldopa
|
|
|
DBH
|
- Bupicomide
- Disulfiram
- Dopastin
- Fusaric acid
- Nepicastat
- Phenopicolinic acid
- Tropolone
|
|
|
PNMT
|
- CGS-19281A
- SKF-64139
- SKF-7698
|
|
|
|
Catabolism
|
|
MAO
|
- Nonselective: Benmoxin
- Caroxazone
- Echinopsidine
- Furazolidone
- Hydralazine
- Indantadol
- Iproclozide
- Iproniazid
- Isocarboxazid
- Isoniazid
- Linezolid
- Mebanazine
- Metfendrazine
- Nialamide
- Octamoxin
- Paraxazone
- Phenelzine
- Pheniprazine
- Phenoxypropazine
- Pivalylbenzhydrazine
- Procarbazine
- Safrazine
- Tranylcypromine; MAO-A selective: Amiflamine
- Bazinaprine
- Befloxatone
- Befol
- Brofaromine
- Cimoxatone
- Clorgiline
- Esuprone
- Harmala alkaloids (Harmine,
- Harmaline
- Tetrahydroharmine
- Harman
- Norharman, etc)
- Methylene blue
- Metralindole
- Minaprine
- Moclobemide
- Pirlindole
- Sercloremine
- Tetrindole
- Toloxatone
- Tyrima; MAO-B selective:
- Ladostigil
- Lazabemide
- Milacemide
- Mofegiline
- Pargyline
- Rasagiline
- Safinamide
- Selegiline (also [[D-Deprenyl]])
* Note that MAO-B inhibitors also influence norepinephrine/epinephrine levels since they inhibit the breakdown of their precursor dopamine.
|
|
|
COMT
|
- Entacapone
- Nitecapone
- Tolcapone
|
|
|
|
|
|
Others
|
|
|
Precursors
|
- L-Phenylalanine → L-Tyrosine → L-DOPA (Levodopa) → Dopamine
- L-DOPS (Droxidopa)
|
|
|
Cofactors
|
- Ferrous Iron (Fe2+)
- S-Adenosyl-L-Methionine
- Vitamin B3 (Niacin
- Nicotinamide → NADPH)
- Vitamin B6 (Pyridoxine
- Pyridoxamine
- Pyridoxal → Pyridoxal Phosphate)
- Vitamin B9 (Folic acid → Tetrahydrofolic acid)
- Vitamin C (Ascorbic acid)
- Zinc (Zn2+)
|
|
|
Others
|
- Activity enhancers: BPAP
- PPAP; Release blockers: Bethanidine
- Bretylium
- Guanadrel
- Guanazodine
- Guanclofine
- Guanethidine
- Guanoxan; Toxins: 6-OHDA
|
|
|
|
|
List of adrenergic drugs
|
|
|
Drugs for obstructive airway diseases: asthma/COPD (R03)
|
|
| Adrenergics, inhalants |
|
Short acting β2-agonists
|
Salbutamol#/Levosalbutamol • Fenoterol • Terbutaline • Pirbuterol • Procaterol • Bitolterol • Rimiterol • Carbuterol • Tulobuterol • Reproterol
|
|
|
Long acting β2-agonists (LABA)
|
Arformoterol • Bambuterol • Clenbuterol • Formoterol • Salmeterol Ultra LABA: Indacaterol
|
|
|
other
|
Epinephrine# • Hexoprenaline • Isoprenaline (Isoproterenol) • Orciprenaline (Metaproterenol)
|
|
|
| Glucocorticoids |
Beclometasone# • Budesonide • Ciclesonide • Fluticasone • Mometasone • Flunisolide • Betamethasone • Triamcinolone
|
|
Anticholinergics/
muscarinic antagonist |
Aclidinium bromide • Ipratropium bromide# • Oxitropium bromide • Tiotropium bromide
|
|
| Mast cell stabilizers |
Cromoglicate • Nedocromil
|
|
| Xanthines |
Doxofylline • Enprofylline • Theobromine • Theophylline/Aminophylline/Choline theophyllinate
|
|
| Eicosanoid inhibition |
|
Leukotriene antagonists
|
Montelukast • Pranlukast • Zafirlukast
|
|
|
Lipoxygenase inhibitor
|
Zileuton
|
|
|
Thromboxane receptor antagonists
|
Ramatroban • Seratrodast
|
|
|
| Combination products |
Budesonide/formoterol • Fluticasone/salmeterol • Ipratropium bromide/salbutamol • Mometasone/formoterol
|
|
- #WHO-EM
- ‡Withdrawn from market
- Clinical trials:
- †Phase III
- §Never to phase III
|
|
anat(n, x, l, c)/phys/devp
|
noco(c, p)/cong/tumr, sysi/epon, injr
|
|
|
|
|
English Journal
- Broad screening and identification of β-agonists in feed and animal body fluid and tissues using ultra-high performance liquid chromatography-quadrupole-orbitrap high resolution mass spectrometry combined with spectra library search.
- Li T1, Cao J2, Li Z2, Wang X1, He P3.
- Food chemistry.Food Chem.2016 Feb 1;192:188-96. doi: 10.1016/j.foodchem.2015.06.104. Epub 2015 Jun 30.
- Broad screening and identification of β-agonists in feed, serum, urine, muscle and liver samples was achieved in a quick and highly sensitive manner using ultra high performance liquid chromatography-quadrupole-orbitrap high resolution mass spectrometry (UHPLC-Q-Orbitrap HRMS) combined with a spect
- PMID 26304337
- The pharmacokinetics of the β2-adrenoceptor agonist, tulobuterol, in Beagle dogs following transdermal and intravenous administration.
- Kim JH1, Kim TH2, Park HJ1, Choi YJ1, Kang JH3, Song KH1, Koo TS4, Seo KW5.
- Veterinary journal (London, England : 1997).Vet J.2016 Feb;208:90-2. doi: 10.1016/j.tvjl.2015.10.012. Epub 2015 Oct 13.
- Tulobuterol is a β2-adrenergic agonist that was the first bronchodilator approved as a transdermal patch for humans. Previous studies have examined the pharmacokinetics of tulobuterol in humans but not in the veterinary species. In this study, the pharmacokinetics of tulobuterol was examined in hea
- PMID 26639828
- Determination of tulobuterol in rat plasma using a liquid chromatography-tandem mass spectrometry method and its application to a pharmacokinetic study of tulobuterol patch.
- Han X1, Liu R1, Ji L1, Hui M1, Li Q1, Fang L1, Bi K2.
- Journal of chromatography. B, Analytical technologies in the biomedical and life sciences.J Chromatogr B Analyt Technol Biomed Life Sci.2016 Jan 1;1008:108-14. doi: 10.1016/j.jchromb.2015.11.017. Epub 2015 Nov 28.
- A sensitive and accurate liquid chromatography-tandem mass spectrometry (LC-MS/MS) method has been developed and validated for determination of tulobuterol in rat plasma for the first time. Plasma samples were extracted by liquid-liquid extraction method with methyl tert-butyl ether and the analyte
- PMID 26638035
Japanese Journal
- 高齢喘息患者におけるブデソニド/ホルモテロール配合剤の臨床的有効性についての検討 : ブデソニドとツロブテロール貼付薬の併用治療との比較
- 大成 洋二郎,春田 吉則,向田 賢市 [他],近藤 圭一
- アレルギー 61(6), 820-831, 2012-06-30
- 【背景・目的】高齢喘息患者の長期管理には,吸入薬だけでなく経皮吸収型気管支拡張薬(貼付LABA)が使用されることがあるが,本邦に特徴的な薬剤であることもあり,エビデンスが少ない.そこで,高齢喘息患者を対象に,ICS+貼付LABAとlCS/LABA配合剤の治療効果を比較した.【方法】ブデソニド(BUD)400μg/日とツロブテロール貼付薬(Tulo)2mg/日の併用により治療中の70歳以上の喘息患者 …
- NAID 110009470779
- 高齢喘息患者におけるブデソニド/ホルモテロール配合剤の臨床的有効性についての検討 : ブデソニドとツロブテロール貼付薬の併用治療との比較
- Study of the Physicochemical Properties of Tulobuterol Dry Syrups Using Taste and Smell Sensors
- 井上 裕,嶋崎 広典,村田 勇,木村 昌行,金本 郁男
- Chemical and Pharmaceutical Bulletin 60(4), 442-448, 2012-04
- … The purpose of the present study was to evaluate the taste and smell of Tulobuterol Dry Syrup (TB-DS) in its original form (formulation A) and generic form (formulations B and C) by means of gustatory sensation tests and taste and smell sensors. …
- NAID 120005352580
Related Links
- Y Key:YREYLAVBNPACJM-UHFFFAOYSA-N Yes Y. N (what is this?) (verify). Tulobuterol (INN) is a long-acting beta2-adrenergic receptor agonist, marketed in Japan as a transdermal patch under the name Hokunalin tape (ホクナリンテープ).
- ツロブテロール(Tulobuterol)の検索ならお薬検索QLife（キューライフ）。お医者さんが 処方する処方薬と、薬局で買える市販薬(OTC)、の効果と副作用、写真、添付文書、 保管方法等を掲載。商品名だけでなく一般名や剤形、色などからも検索可能。
Related Pictures
★リンクテーブル★
[★]
- 英
- tulobuterol
- 化
- ツロブテロール塩酸塩 塩酸ツロブテロール tulobuterol hydrochloride
- 商
- セキナリン、ツロブテン、ツロブニスト、ベラチン、ホクナリン
[★]
ツロブテロール。塩酸ツロブテロール