TABLE 2

Pharmacology of DIPT, 5-MeO-DET, and 5-MeO-AMT at 5-HT_1A and 5-HT_2A receptors: effects on binding and function

For test compounds, n = 3–8 for each assay. Data are expressed as mean ± S.E.M. The standard compounds for purposes of comparison for 5-HT_1A binding and functional assays were serotonin and dihydroergotamine. The standard compounds for 5-HT_2A binding and functional assays were serotonin and LSD.

Assay	Drug
Assay	DIPT	5-MeO-DET	5-MeO-AMT	Serotonin	Dihydroergotamine	LSD
5-HT_1A binding and functional assay
[³H]8-OH-DPAT binding K_i, nM	2270 ± 600	23.8 ± 7.9	194 ± 71	3.42 ± 0.41	1.01 ± 0.35
Hill coefficient	−1.01 ± 0.15	−0.84 ± 0.07	−0.83 ± 0.04	−0.89 ± 0.10	−0.58 ± 0.04
[³⁵S]GTPγS binding EC₅₀, nM	4570 ± 640	380 ± 110	680 ± 250	16.1 ± 5.7	0.82 ± 0.13
5-HT maximal effect, %	58.1 ± 9.8	103.0 ± 6.2	100.6 ± 7.9	100	91 ± 24
5-HT_2A binding and functional assays
[¹²⁵I]DOI binding K_i, nM	910 ± 120	251 ± 92	32.9 ± 5.5	20.4 ± 4.3		0.92 ± 0.16
Hill coefficient	−0.72 ± 0.05	−0.76 ± 0.08	−0.68 ± 0.07	−0.70 ± 0.06		−1.07 ± 0.13
[³H]AA release EC₅₀, nM	450 ± 220	89 ± 34	3.35 ± 0.96	10.3 ± 1.0		1.01 ± 0.31
LSD maximal effect, %	88 ± 10	106 ± 16	108 ± 14			100
IP-1 formation EC₅₀, nM	420 ± 140	280 ± 120	8.4 ± 4.4	49 ± 13		0.277 ± 0.055
Serotonin maximal effect, %	81.4 ± 3.9	102 ± 11	84.2 ± 8.7	99.7 ± 1.4		83.1 ± 5.6