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.
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- No. CAS: 81801-12-9
- Fòrmula: C16H25N3O5
- Peso molecular:339.39
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Almacenamiento:
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Actividad biológica
Descripciòn
IC50 & Target
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β1 adrenoceptor |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| 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] |
In Vitro
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.
In Vivo
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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No. CAS 81801-12-9
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Peso molecular 339.39
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Fòrmula 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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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
[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
HY-101327 Related Classifications
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Keywords
- 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