TABLE 1

Functional activity of muscarinic agonists at wild-type and Y381A mutated M1 receptors

EC₅₀ values and percentage of maximum acetylcholine response are presented as mean ± S.E.M. of three to six determinations. Shift is EC₅₀ value on Y381A mutant/EC₅₀ value on wild-type M1.

	hM1-WT		Y381A		Shift
	EC₅₀	Max	EC₅₀	Max	Shift
	nM	%	nM	%
Acetylcholine	21 ± 6	100	3837 ± 677	100	183
Xanomeline	19 ± 7	81 ± 3	42 ± 7	69 ± 3	2.2
AC-42	805 ± 251	71 ± 2	220 ± 16	83 ± 3	0.27
TBPB	22 ± 2	77 ± 2	2 ± 1	90 ± 1	0.09
N-Desmethylclozapine	115 ± 28	50 ± 5	14 ± 2	96 ± 2	0.12