xamoterol

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出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2016/01/29 21:32:15」(JST)

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Xamoterol

Systematic (IUPAC) name
(RS)-N-(2-{[2-hydroxy-3-(4-hydroxyphenoxy)propyl]amino}ethyl)morpholine-4-carboxamide
Identifiers
CAS Number	81801-12-9 N
ATC code	C01CX07
PubChem	CID 155774
IUPHAR/BPS	538
ChemSpider	137213 Y
UNII	7HE0JQL703 Y
KEGG	D06328 Y
ChEMBL	CHEMBL75753 Y
Chemical data
Formula	C16H25N3O5
Molar mass	339.387 g/mol
SMILES O=C(NCCNCC(O)COc1ccc(O)cc1)N2CCOCC2
InChI InChI=1S/C16H25N3O5/c20-13-1-3-15(4-2-13)24-12-14(21)11-17-5-6-18-16(22)19-7-9-23-10-8-19/h1-4,14,17,20-21H,5-12H2,(H,18,22) Y Key:DXPOSRCHIDYWHW-UHFFFAOYSA-N Y
NY (what is this?)  (verify)

Xamoterol is a cardiac stimulant. It works by binding to the β1 adrenergic receptor. It is a 3rd generation adrenergic beta receptor partial agonist. It provides cardiac stimulation at rest but it acts as a blocker during exercise.

References

UpToDate Contents

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• 1. 収縮能障害による心不全における強心剤 inotropic agents in heart failure due to systolic dysfunction
• 2. 収縮能障害による心不全におけるジゴキシンの使用 use of digoxin in heart failure due to systolic dysfunction
• 3. 心房細動における心拍数のコントロール：薬理療法 control of ventricular rate in atrial fibrillation pharmacologic therapy

English Journal

• Pro-apoptotic effect of anti-β(1)-adrenergic receptor antibodies in periodontitis patients.

• Reina S, Ganzinelli S, Sterin-Borda L, Borda E.SourcePharmacology Unit, School of Dentistry, University of Buenos Aires, Buenos Aires, Argentina; National Research Council of Argentina, Buenos Aires, Argentina.
• International immunopharmacology.Int Immunopharmacol.2012 Oct 24. pii: S1567-5769(12)00303-7. doi: 10.1016/j.intimp.2012.10.011. [Epub ahead of print]
• An anti-β(1)-adrenergic antibody from the sera of periodontitis patients (anti-β(1)-AR IgG) against the second extracellular loop of the human β(1)-adrenoceptor (β(1)-AR) has been shown to cause rat atria apoptosis. The anti-β(1)-AR IgG binds and activates atria β(1)-AR, increasing the intrace
• PMID 23103827

• Norepinephrine suppresses IFN-γ and TNF-α production by murine intestinal intraepithelial lymphocytes via the β₁ adrenoceptor.

• Takayanagi Y, Osawa S, Ikuma M, Takagaki K, Zhang J, Hamaya Y, Yamada T, Sugimoto M, Furuta T, Miyajima H, Sugimoto K.SourceFirst Department of Medicine, Hamamatsu University School of Medicine, Hamamatsu 431-3192, Japan.
• Journal of neuroimmunology.J Neuroimmunol.2012 Apr;245(1-2):66-74. Epub 2012 Mar 6.
• We examined whether norepinephrine (NE) had direct effects on cytokine production by murine intestinal intraepithelial lymphocytes (IELs), compared with splenocytes. CD3⁺ IELs and CD3⁺ splenocytes expressed α(1B), α(1D), α(2C), β₁, β₂, and β₃ adrenoceptors (ARs). NE significantly sup
• PMID 22398028

Japanese Journal

• Characterization of β-Adrenoceptor Subtype in Bladder Smooth Muscle in Cynomolgus Monkey

• Takeda Hiroo,Yamazaki Yoshinobu,Akahane Masuo [他],AKAHANE Satoshi,MIYATA Hiroshi,IGAWA Yasuhiko,NISHIZAWA Osamu
• The Japanese journal of pharmacology 88(1), 108-113, 2002-01-01
• … xamoterol. …
• NAID 10007944942

• Cardiomyopathic Hamster Hearts : Long-Term Effects of Drugs on Catecholamine Contents and Binding Characteristics of α_1- and β_1-Adrenergic Receptors

• 渡辺 賢一,柴田 昭,若林 広行,嶋田 健次,佐々木 佳子,長友 孝文
• Ｂｉｏｌｏｇｉｃａｌ　＆　Ｐｈａｒｍａｃｅｕｔｉｃａｌ　Ｂｕｌｌｅｔｉｎ 16(7), 660-663, 1993-07-15
• … In addition, the effects of bunazosin, atenolol, xamoterol, ketanserin, and verapamil on the catecholamine content and [^3H]prazosin, [^3H]CGP12177 bindings to α_1- and β_1-adrenergic receptors of myocardium were compared with those of the controls. … (3) Xamoterol induced a higher K_d value for β_1-adrenoceptors and lower dopamine content than for those with cardiomyopathy. …
• NAID 110003640317

• Xamoterol in sinus node disease

• AVERY PG
• Int J Cardiol 40, 45-49, 1993
• NAID 30006519401

Related Links

• Xamoterol - Wikipedia, the free encyclopedia

Xamoterol is a cardiac stimulant. It works by binding to the β1 adrenergic receptor . It is a 3rd generation adrenergic beta receptor partial agonist. It provides cardiac stimulation at rest but it acts as a blocker during exercise.

• The pharmacology of xamoterol

1 Xamoterol (Corwin, Carwin, Corwil, Xamtol, ICI 118,587) is a β-adrenoceptor partial agonist which is of benefit in the chronic treatment of heart failure (e.g. The German and Austrian Xamoterol Study Group, 1988). These results contrast with ...