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Xamoterol hemifumarate manufacturers
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| | Xamoterol hemifumarate Basic information |
| Product Name: | Xamoterol hemifumarate | | Synonyms: | ICI 118587 HEMIFUMARATE SALT;bis[N-[2-[[2-hydroxy-3-(4-hydroxyphenoxy)propyl]amino]ethyl]morpholine-4-carboxamide] fumarate;ICI 118587 hemifumarate salt, (±)-N-[2-[[Hydroxy-3-(4-hydroxy)propyl]amino]ethyl-4-morpholinecarboxamide hemifumarate salt;Corwin;Carwin;Corwin：Xamtol;ICI-118587;Xamtol | | CAS: | 73210-73-8 | | MF: | C36H54N6O14 | | MW: | 794.85 | | EINECS: | 277-319-9 | | Product Categories: | ICI 118,587;API | | Mol File: | 73210-73-8.mol |  |
| | Xamoterol hemifumarate Chemical Properties |
| Melting point | 168-169° (dec) | | storage temp. | Store at RT | | solubility | H2O: 10 mg/mL at 60 °C, soluble | | form | solid | | color | white | | CAS DataBase Reference | 73210-73-8 |
| | Xamoterol hemifumarate Usage And Synthesis |
| Description | Xamoterol fumarate is a cardioselective partial beta-agonist, the first of its class to be
developed for use in heart failure. The main advantage of xamoterol fumarate as a
cardiotonic lies in the fact that its beta-blocking effect exerted during high sympathetic
drive will protect the heart from overstimulation. It is claimed to be a viable but safer
alternative to digoxin. | | Description | Xamoterol is a partial agonist of β1-adrenergic receptors (β1-ARs) with an EC50 value of 80 nM for the generation of cyclic AMP (cAMP) in neonatal rat cardiomyocyte cultures. It increases spontaneous contraction of isolated rat right atria (EC50 = 4.67 nM). In vivo, xamoterol increases heart rate in beagle dogs (ED50 = 3.2 μg/kg) and in a rat model of spontaneous heart failure (ED50 = 6 μg/kg), an effect that is reversed by the selective β1-AR antagonist betaxolol but not the selective β2-AR antagonist ICI 118551 . Formulations containing xamoterol have been used in the treatment of heart failure. | | Chemical Properties | Crystallizes in ethanol, melting point 168-169℃ (decomposition). | | Originator | ICI (United Kingdom) | | Uses | Xamoterol Hemifumarate, is a β1-adrenoceptor-selective partial agonist. | | Uses | Stimulant (cardiac). | | Brand name | Corwin | | Biological Activity | β 1 -adrenoceptor-selective partial agonist (pA 2 values are 7.4-7.8 and 5.2-6.2 at β 1 - and β 2 -adrenoceptors respectively). | | storage | Store at RT | | References | [1] R N WILLETTE. In vitro and in vivo characterization of intrinsic sympathomimetic activity in normal and heart failure rats.[J]. Journal of Pharmacology and Experimental Therapeutics, 1999, 289 1: 48-53.
[2] M T KOWALSKI. Comparison of the effects of xamoterol and isoprenaline on rat cardiac beta-adrenoceptors: studies of function and regulation.[J]. British Journal of Pharmacology, 1990, 99 1: 27-30. DOI: 10.1111/j.1476-5381.1990.tb14648.x
[3] A. NUTTALL H. M S. THE CARDIOVASCULAR EFFECTS OF ICI 118,587: A β1-ADRENOCEPTOR PARTIAL AGONIST[J]. British Journal of Pharmacology, 1982, 77 2: 381-388. DOI: 10.1111/j.1476-5381.1982.tb09309.x |
| | Xamoterol hemifumarate Preparation Products And Raw materials |
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