Xamoterol  (Synonyms: Corwin; ICI 118587)

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^{[1][2][3][4][5][6][7]}.

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 pK_D of 7.25 in guinea-pig left atrial membranes (β₁) and a pK_D 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 (0.1-33 μg/kg; i.v.; single bolus injection) acts as a β₁-selective partial agonist in anaesthetised, catecholamine-depleted rats with an ED₅₀ of 0.361 μg/kg^[3].
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.

339.39

C₁₆H₂₅N₃O₅

81801-12-9

O=C(N1CCOCC1)NCCNCC(O)COC2=CC=C(O)C=C2

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [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]