TABLE 2

Action of a series of ligands at wild-type and D116A mutant of the 5-HT_1A receptor coupled to Ca²⁺ response in CHO cells

Agonist efficacies are expressed relative to those of 5-HT and (+)-8-OH-DPAT (100% at 10 μM) for 5-HT_1A and 5-HT_1A-D116A receptors, respectively, and pEC₅₀ and E_max values were determined as described under Materials and Methods.

Ligand	5-HT_1A		5-HT_1A-D116A		5-HT_1A + Gα₁₅		5-HT_1A-D116A + Gα₁₅
Ligand	pEC₅₀	E_max	pEC₅₀	E_max	pEC₅₀	E_max	pEC₅₀	E_max
		%		%		%		%
5-HT	6.88 ± 0.15	102 ± 2	IA	IA	7.55 ± 0.07	101 ± 1	IA	IA
5-CT	7.70 ± 0.15	120 ± 9	IA	IA	8.42 ± 0.13	105 ± 8	IA	IA
F13640	7.32 ± 0.12	116 ± 8	IA	IA	7.85 ± 0.10	105 ± 5	IA	IA
F13714	7.29 ± 0.10	79 ± 13	NC	55 ± 10^a	7.92 ± 0.13	102 ± 6	N.C.	113 ± 8^a
L694247	6.65 ± 0.04	41 ± 11	IA	IA	7.70 ± 0.20	93 ± 8	IA	IA
(−)-8-OH-DPAT	IA	IA	IA	IA	7.28 ± 0.19	30 ± 3	IA	IA
Buspirone	IA	IA	IA	IA	6.86 ± 0.04^b	29 ± 2^b	IA	IA
(+)-8-OH-DPAT	6.64 ± 0.20	51 ± 16	6.13 ± 0.12	107 ± 2	7.48 ± 0.09	86 ± 7	6.78 ± 0.11	101 ± 1
(+)-Flesinoxan	IA	IA	5.49 ± 0.07	112 ± 11	7.51 ± 0.15	58 ± 6	6.32 ± 0.05	106 ± 9
LY228,729	7.33 ± 0.21	43 ± 12	5.53 ± 0.09	279 ± 12	8.22 ± 0.08	94 ± 6	6.35 ± 018	192 ± 24
S14506	6.22 ± 0.13	44 ± 11	6.49 ± 0.12	490 ± 64	6.97 ± 0.17	75 ± 5	7.07 ± 0.19	216 ± 44
WAY100,635	IA	IA	IA	IA	IA	IA	7.49 ± 0.16	34 ± 12

IA, inactive; N.C., not computable.
↵a Efficacy at 10 μM.
↵b Data previously acquired using the same procedure is shown for comparison (Wurch and Pauwels, 2003). (−)-Pindolol and spiperone are inactive in all conditions.