Table 7. Chemical Structures and Pharmacological Profile of Decahydroisoquionoline Derivatives 7.1−7.3 at Recombinant AMPA/KA Receptors^a.

			GluA2		GluK1		GluK1/2	GluK1/5
cmpd	X	R	bind.b	funct.c	bind.b	funct.c	bind.b	bind.b
7.1 (LY458545)	O	H	8.3	1.1	1.7	0.04	1.0	7.9
7.2 (LY457691)	NH	H	5.5	0.4	1.6	0.03	1.4	9.9
7.3	NH	Cl	−d	2.0	−d	0.005	−d	−d

^aFunctional data represent K_B values for inhibition of 100 μM glutamate-induced Ca²⁺ influx in HEK 293 cells expressing human homomeric AMPA or KA receptor subtypes. Binding data represent K_i values. [³H]AMPA was used as radioligand for GluA2; others, [³H]KA. The compounds showed no affinity for GluK2 or GluK2/5. All values in [μM].

^bFrom ref (90).

^cFrom ref (86).

^dNot tested.