Xamoterol
Xamoterol (Corwin; ICI 118587) is an orally active and selective β1-adrenoceptor partial agonist. Xamoterol acts as agonist at low sympathetic tone, antagonist at high sympathetic tone, with context-dependent cardiovascular effects including modulated heart rate, blood pressure, and cardiac output. Xamoterol can be used for the research of heart failure, postural hypotension, and ischemic heart disease.
For research use only. We do not sell to patients.
- CAS No.: 81801-12-9
- Formula: C16H25N3O5
- Molecular Weight:339.39
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
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β1 adrenoceptor |
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Cell Line
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Type | Value | Description | References |
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| CHO-K1 | EC50 |
100 μM
Compound: Xamoterol
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Agonist activity at human beta3 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrs
Agonist activity at human beta3 adrenoceptor expressed in CHOK1 cells assessed as induction of [3H]cAMP accumulation after 5 hrs
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[PMID: 23614528] |
Xamoterol (0.5 nM-50 μM; 2 min) produces weak β2-adrenoceptor-mediated relaxant effects in progesterone-pretreated rat uterus, and non-specific, non-β-adrenoceptor-mediated inhibitory effects in guinea-pig ileal and tracheal preparations, with no β-adrenoceptor-mediated activity in oestrogen-pretreated uterine or rat vas deferens preparations[2].
Xamoterol (70 min) displays selective affinity for β1-adrenoceptors, with a pKD of 7.25 in guinea-pig left atrial membranes (β1) and a pKD of 5.24 in guinea-pig uterine membranes (β2), representing a 100-fold preference for β1 sites[2].
Xamoterol (0.2 nM-6 μM) acts as a β1-selective partial agonist in isolated male AP rat right atria, producing a maximal rate stimulation response 65-70% that of isoprenaline with an EC50 of 4.67 nM[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Xamoterol (600 μg/kg/h; s.c.; continuous infusion; 6 days) does not induce cardiac β-adrenoceptor down-regulation or alter receptor-adenylate cyclase coupling in normal rats[3].
Xamoterol acts as a β1-adrenoceptor partial agonist in anaesthetised areflexic dogs, demonstrating 43% of isoprenaline's intrinsic sympathomimetic activity at β1-receptors without β2-receptor stimulation[5].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:AS rats (200-300 g)[3]
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Dosage:600 μg/kg/h
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Administration:s.c.; continuous infusion; 6 days
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Result:Did not alter the density of total, β1, or β2 cardiac β-adrenoceptors compared to saline control; total Bmax was 17.2 fmol/mg protein (0% change from control), β1 Bmax was 11.8 fmol/mg protein (0% change), and β2 Bmax was 5.3 fmol/mg protein (+8.0% change, not significant).
Left the equilibrium dissociation constant (Kd) of [125I]-pindolol binding unchanged at 38 pM.
Did not significantly modify the effect of Gpp(NH)p on isoprenaline displacement of [125I]-pindolol binding, indicative of β-adrenoceptor-adenylate cyclase coupling.
Resulted in a plasma xamoterol level of 161 nM at the end of the infusion.
Chemical Information
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CAS No. 81801-12-9
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Molecular Weight 339.39
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Formula C16H25N3O5
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SMILES
O=C(N1CCOCC1)NCCNCC(O)COC2=CC=C(O)C=C2
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Synonyms
Corwin; ICI 118587
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
[1]. Ikram H, et al. Xamoterol in severe heart failure. Lancet. 1990 Aug 25;336(8713):517-8. [Content Brief]
[2]. Malta E, et al. The in vitro pharmacology of xamoterol (ICI 118,587). Br J Pharmacol. 1985;85(1):179-187. [Content Brief]
[3]. Kowalski MT, et al. Comparison of the effects of xamoterol and isoprenaline on rat cardiac beta-adrenoceptors: studies of function and regulation. Br J Pharmacol. 1990;99(1):27-30. [Content Brief]
[4]. Mehlsen J, et al. Xamoterol, a new selective beta-1-adrenoceptor partial agonist, in the treatment of postural hypotension. Acta Med Scand. 1986;219(2):173-177. [Content Brief]
[5]. Hashimoto T, et al. The cardiovascular effects of xamoterol, a beta 1-adrenoceptor partial agonist, in healthy volunteers at rest. Br J Clin Pharmacol. 1986;21(3):259-265. [Content Brief]
[6]. Löfdahl CG, et al. Effects of xamoterol (ICI 118,587) in asthmatic patients. Br J Clin Pharmacol. 1984;18(4):597-601. [Content Brief]
[7]. Jennings G, et al. Cardioselectivity, kinetics, hemodynamics, and metabolic effects of xamoterol. Clin Pharmacol Ther. 1984;35(5):594-603. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Xamoterol Related Classifications
Cat. No.: HY-101327
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- Xamoterol
- 81801-12-9
- Corwin
- ICI 118587
- ICI118587
- ICI 118587
- ICI-118587
- Adrenergic Receptor
- ischemic heart disease
- guinea-pig left atrial membranes
- heart failure
- progesterone-pretreated rat uterus
- β2-adrenoceptor
- rat atrial preparations
- cat left atria
- β1-adrenoceptor
- guinea pig
- postural hypotension
- Inhibitor
- inhibitor
- inhibit