Table 1.

K_e values for ring A and N6 analogs at 5-HT_2A and α_1A receptors

Compd	R1	R2	R3	X1	X2	Ke ± SEM (nM)a
						5-HT2A	α 1A
6a	n-Hex	Me	Me	H	H	71±19	>10,000
6b	Isobu	Me	Me	H	H	367±82	>10,000
6c	Isopen	Me	Me	H	H	NDb	>10,000
6d	2-EthylBu	Me	Me	H	H	806±152	>10,000
6e	CyclobutylMe	Me	Me	H	H	NDb	>10,000
6f	CyclopentylMe	Me	Me	H	H	NDb	>10,000
6g	CyclohexylMe	Me	Me	H	H	1722±258	>10,000
6h	Allyl	Me	Me	H	H	70±15	>10,000
6i	HydroxyPr	Me	Me	H	H	708±316	>10,000
14a	Me	Et	Me	H	H	378±92	52±13
14b	Me	n-Pr	Me	H	H	389±93	133±45
14c	Me	n-Bu	Me	H	H	943±283	234±52
14d	Me	n-Pen	Me	H	H	>10,000	449±169
14e	Me	CyclopropylMe	Me	H	H	484±123	195±86
14f	Me	Benzyl	Me	H	H	154±76	1917±226
15	Me	Me	Me	Br	H	53±14	>10,000
16	Me	Me	Me	Br	Br	43±11	>10,000
18a	Me	Me	Et	H	H	>10,000	26±6
18b	Me	Me	n-Pr	H	H	>10,000	38±3
18c	Me	Me	n-Bu	H	H	>10,000	210±50
18d	Me	Me	n-Pen	H	H	>10,000	720±204
18e	Me	Me	CyclopropylMe	H	H	>10,000	319±60
2	Me	Me	Me	H	H	850±6c	36±7
prazosin							1.1 ± 0.4
ketanserin						32c,d

^aValues represent mean ± SEM for three independent experiments.

^bND = K_e not determined (compounds were weak agonists).

^cData from reference 25

^dIC₅₀ determined in the presence of 5-HT EC₈₀