Table 1

Structure and anticonvulsant potency of representative nucleoside AK inhibitors

Compound	R	R′	X	Y	Z	ED₅₀ [95% CI]^1-a(mg/kg)
5′-adADO						153 [71.6–326]
ITU	CH₂OH	H	NH₂	I	CH	6.2 [3.5–10.1]
5′-dITU	CH₃	H	NH₂	I	CH	0.3 [0.2–0.6]
GP836	CH₂NH₂	H	NH₂	I	CH	7.1 [3.9–13.0]
GP683	CH₃	H	NHPh	Ph	CH	1.1 [0.6–2.1]
GP947	H	CH₃	NHPh	Ph	CH	0.2 [0.1–0.3]
GP790	H	CH₂OH	NHPh	Ph	CH	1.6 [0.8–3.0]
GP515	CH₂NH₂	H	NH₂	Br	N	15.9 [10.2–24.8]
GP665	CH₃	H	NHPh	Ph	N	11.7 [6.1–22.6]
GP547	CH₂NH₂	H	NH₂	I	N	9.7 [3.8–24.7]

↵1-a ED₅₀ values and 95% confidence intervals (95% CI) for inhibition of MES seizures in rats at 1 h after i.p. administration (see Fig. 2 and 3).