An A1 adenosine receptor agonist
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N6-Cyclohexyladenosine is an adenosine receptor agonist.1 It selectively binds to adenosine A1 receptors in rat cortical membranes (IC50 = 2.3 nM) over A2 receptors in rat striatal membranes (IC50 = 870 nM). N6-Cyclohexyladenosine decreases heart rate and increases coronary flow in a perfused working rat heart model ex vivo (EC25s = 5 and 860 nM, respectively). In vivo, it decreases heart rate and blood pressure in normotensive rats (EC25s = 2.4 and 4.2 μg/kg, respectively).1 N6-Cyclohexyladenosine (100 μM) induces sleep in rats when administered via basal forebrain infusion.2 N6-Cyclohexyladenosine also decreases locomotor activity in mice (ED50 = 60 μg/kg, i.p.).3
1.Hutchison, A.J., Webb, R.L., Oei, H.H., et al.CGS 21680C, an A2 selective adenosine receptor agonist with preferential hypotensive activityJ. Pharmacol. Exp. Ther.251(1)47-55(1989) 2.Blanco-Centurion, C., Xu, M., Murillo-Rodriguez, E., et al.Adenosine and sleep homeostasis in the basal forebrainJ Neurosci.26(31)8092-8100(2006) 3.Nikodijevi?, O., Daly, J.W., and Jacobson, K.A.Characterization of the locomotor depression produced by an A2-selective adenosine agonistFEBS Lett.261(1)67-70(1990)
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