2-Phenylaminoadenosine

2-Phenylaminoadenosine is an adenosine receptor agonist.¹ It binds to adenosine A₁ receptors in rat cortical membranes (IC₅₀ = 910 nM) and A₂ receptors in rat striatal membranes (IC₅₀ = 115 nM). 2-Phenylaminoadenosine increases coronary flow in a perfused working rat heart model ex vivo (EC₂₅ = 110 nM). It decreases blood pressure in normotensive (ED₂₅ = 28 μg/kg) and spontaneously hypertensive rats (SHR; ED₃₀ = 5.32 μg/kg).^1,2 2-Phenylaminoadenosine (500 nmol/kg) increases L-dihydroxyphenylalanine (L-DOPA; Item No. 13248) accumulation in rat striatum.³ It also inhibits conditioned avoidance responding (CAR) to electric shock in rats (ED₅₀ = 1.3 mg/kg).⁴

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1. Hutchison, A.J., Webb, R.L., Oei, H.H., et al. CGS 21680C, an A₂ selective adenosine receptor agonist with preferential hypotensive activity. J. Pharmacol. Exp. Ther. 251(1), 47-55 (1989).

2. Abiru, T., Yamaguchi, T., Watanabe, Y., et al. The antihypertensive effect of 2-alkynyladenosines and their selective affinity for adenosine A₂ receptors. Eur. J. Pharmacol. 196(1), 69-76 (1991).

3. Choksi, N.Y., Hussain, A., and Booth, R.G. 2-Phenylaminoadenosine stimulates dopamine synthesis in rat forebrain in vitro and in vivo via adenosine A₂ receptors. Brain Res. 761(1), 151-155 (1997).

4. Martin, G.E., Rossi, D.J., and Jarvis, M.F. Adenosine agonists reduce conditioned avoidance responding in the rat. Pharmacol. Biochem. Behav. 45(4), 951-958 (1993).