プロカテロール
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出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2014/06/14 13:14:25」(JST)
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Procaterol
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| Systematic (IUPAC) name |
| (±)-(1R,2S)-rel-8-Hydroxy-5-[1-hydroxy-2-(isopropylamino)butyl]-quinolin-2(1H)-one |
| Clinical data |
| AHFS/Drugs.com |
Micromedex Detailed Consumer Information |
| Legal status |
? |
| Routes |
Oral, inhalation |
| Identifiers |
| CAS number |
59828-07-8 Y |
| ATC code |
R03AC16 R03CC08 |
| PubChem |
CID 4916 |
| ChemSpider |
599984 N |
| UNII |
X7I3EMM5K0 Y |
| KEGG |
D08424 Y |
| Chemical data |
| Formula |
C16H22N2O3 |
| Mol. mass |
290.357 g/mol |
SMILES
- CC(C)NC(CC)C(O)c2ccc(O)c1NC(=O)C=Cc12
|
| N (what is this?) (verify) |
Procaterol, applied as procaterol hydrochloride (USAN), is an intermediate-acting β2-adrenergic receptor agonist used for the treatment of asthma. It has never been filed for FDA evaluation in the United States, where it is not marketed. The drug is readily oxidised in the presence of moisture and air, making it unsuitable for therapeutic use by inhalation.[1] Pharmaceutical company Parke-Davis/Warner-Lambert researched a stabilizer to prevent oxidation, but an effective one was never developed.[1]
References
- ^ a b US 4616022, Ghebre-sellassie, Issac & Russell U. Nesbitt Jr., "Procaterol stabilization", published 1984, issued 1986
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Adrenergics
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Receptor ligands
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α1
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- 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
- Hydroxyzine
- 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.
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α2
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- 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.
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β
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Reuptake inhibitors
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NET
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- 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
- Ethanol
- EXP-561
- Fezolamine
- Ginkgo biloba
- Indeloxazine
- Nefazodone
- Nefopam
- Pridefrine
- Tapentadol
- Tedatioxetine
- Teniloxazine
- Tofenacin
- Tramadol
- Ziprasidone
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VMAT
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- Ibogaine
- Reserpine
- Tetrabenazine
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Enzyme inhibitors
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Anabolism
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PAH
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TH
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- 3-Iodotyrosine
- Aquayamycin
- Bulbocapnine
- Metirosine
- Oudenone
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AAAD
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- Benserazide
- Carbidopa
- DFMD
- Genistein
- Methyldopa
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DBH
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- Bupicomide
- Disulfiram
- Dopastin
- Fusaric acid
- Nepicastat
- Phenopicolinic acid
- Tropolone
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PNMT
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- CGS-19281A
- SKF-64139
- SKF-7698
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Catabolism
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MAO
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- 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
- Brofaromine
- Cimoxatone
- Clorgiline
- Eprobemide
- 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.
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COMT
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- Entacapone
- Nitecapone
- Tolcapone
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Others
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Precursors
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- L-Phenylalanine → L-Tyrosine → L-DOPA (Levodopa) → Dopamine
- L-DOPS (Droxidopa)
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Cofactors
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- 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+)
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Others
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- Activity enhancers: BPAP
- PPAP; Release blockers: Bethanidine
- Bretylium
- Guanadrel
- Guanazodine
- Guanclofine
- Guanethidine
- Guanoxan; Toxins: 6-OHDA
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List of adrenergic drugs
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Drugs for obstructive airway diseases: asthma/COPD (R03)
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| Adrenergics, inhalants |
| Short acting β2-agonists |
- Bitolterol
- Carbuterol
- Fenoterol
- Pirbuterol
- Procaterol
- Reproterol
- Rimiterol
- Salbutamol#/Levosalbutamol
- Terbutaline
- Tulobuterol
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| Long acting β2-agonists (LABA) |
- Arformoterol
- Bambuterol
- Clenbuterol
- Formoterol
- Salmeterol
- Ultra LABA: Indacaterol, Olodaterol, Vilanterol
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| other |
- Epinephrine#
- Hexoprenaline
- Isoprenaline (Isoproterenol)
- Orciprenaline (Metaproterenol)
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| Glucocorticoids |
- Beclometasone#
- Betamethasone
- Budesonide
- Ciclesonide
- Flunisolide
- Fluticasone
- Mometasone
- Triamcinolone
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Anticholinergics/
muscarinic antagonist |
- Aclidinium bromide
- Glycopyrronium bromide
- Ipratropium bromide#
- Oxitropium bromide
- Tiotropium bromide
- Umeclidinium bromide
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| Mast cell stabilizers |
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| Xanthines |
- Acefylline
- Ambuphylline
- Bamifylline
- Doxofylline
- Enprofylline
- Etamiphylline
- Proxyphylline
- Theobromine
- Theophylline/Aminophylline/Choline theophyllinate
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| Eicosanoid inhibition |
| Leukotriene antagonists |
- Montelukast
- Pranlukast
- Zafirlukast
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| Lipoxygenase inhibitor |
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| Thromboxane receptor antagonists |
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| Non-xanthine PDE4 inhibitors |
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| Others/unknown |
- Amlexanox
- Eprozinol
- Fenspiride
- Omalizumab
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| Combination products |
- Budesonide/formoterol
- Fluticasone/salmeterol
- Ipratropium bromide/salbutamol
- Mometasone/formoterol
- Beclometasone/formoterol
- Fluticasone furoate/vilanterol
- Umeclidinium bromide/vilanterol
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- #WHO-EM
- ‡Withdrawn from market
- Clinical trials:
- †Phase III
- §Never to phase III
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anat (n, x, l, c)/phys/devp
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noco (c, p)/cong/tumr, sysi/epon, injr
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proc, drug (R1/2/3/5/6/7)
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English Journal
- Randomized, Multicenter Clinical Study of Tratinterol Hydrochloride Tablets for the Treatment of Bronchial Asthma.
- Kong L1, Liu J1, Gu G2, Huo J3, Ma Z4, Shao Y5, Sun S6, Yuan Y1, Zhu S7, Yao C7, Du G8, Cheng M9, Kang J10.
- Clinical therapeutics.Clin Ther.2015 Jun 1;37(6):1248-58. doi: 10.1016/j.clinthera.2015.03.013. Epub 2015 Apr 7.
- PURPOSE: The aim of this study was to determine the efficacy and safety profile of tratinterol hydrochloride tablets in the treatment of bronchial asthma.METHODS: This multicenter, randomized, double-blind clinical research study was completed at 6 centers in the People's Republic of China from Marc
- PMID 25857594
- Design of highly sensitive phosphorescence sensor for determination of procaterol hydrochloride based on inhibition of KClO3 oxidation fluorescein isothiocyanate.
- Liu JM1, Huang Q, Liu ZB, Zhang LH, Zheng ZY, Lin CQ.
- Luminescence : the journal of biological and chemical luminescence.Luminescence.2015 Jun;30(4):382-7. doi: 10.1002/bio.2743. Epub 2014 Jul 18.
- Procaterol hydrochloride (Prh) can inhibit KClO3 oxidation of fluorescein isothiocyanate (FITC) to form a non-phosphorescent compound, which causes room temperature phosphorescence (RTP) of FITC in the system to enhance sharply the linear relationship between ∆Ip and the Prh content. Thus, a rapid
- PMID 25044504
- UGT1A1*28 is associated with greater decrease in serum K(+) levels following oral intake of procaterol.
- Yokoe N1, Yamaguchi E, Nishimura M, Tanaka H, Takahashi A, Baba K, Gosho M, Okada S.
- The Journal of asthma : official journal of the Association for the Care of Asthma.J Asthma.2015 Apr;52(3):240-5. doi: 10.3109/02770903.2014.957766. Epub 2014 Sep 10.
- BACKGROUND AND OBJECTIVE: Procaterol is a potent β2-agonist frequently used for the management of asthma and chronic obstructive pulmonary disease. The efficacy and adverse effects of β2-agonists are heterogeneous in individual patients, which may be partly caused by genetic variations in metaboli
- PMID 25171434
Japanese Journal
- リザーバー式吸入粉末剤における振とう操作と薬物放出量に関する検討
- 慢性閉塞性肺疾患急性増悪後の呼吸リハビリテーションにおけるプロカテロールの効果
- 顔面肩甲上腕型筋ジストロフィーと診断されていたDOK7型筋無力症の1例
Related Links
- プロカテロール(procaterol)は短時間作用性β2アドレナリン受容体刺激剤であり、 気管支喘息、慢性気管支炎、肺気腫などの慢性閉塞性肺疾患の対症療法に使われる。 概要 [編集]. プロカテロールはβ2刺激剤の一種であり、定量噴霧式吸入器(MDI)、経口( ...
- Procaterol, applied as procaterol hydrochloride (USAN), is a intermediate-acting β2-adrenergic receptor agonist used for the treatment of asthma. It has never been filed for FDA evaluation in the United States, where it is not marketed.
Related Pictures
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- 塩酸プロカテロール, procaterol hydrochloride、塩酸プロカテロール水和物, プロカテロール塩酸塩水和物, procaterol hydrochloride hydrate
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プロカテロール、塩酸プロカテロール