TABLE 4

Agonist properties displayed by 5-HT, DOI, 25I-NBOMe, Cimbi-36, and compounds 1–4 at human 5-HT_2AR, 5-HT_2BR, and 5-HT_2CR expressed in mammalian cell lines in fluorescence-based Ca²⁺ assays I and II

The two Ca²⁺ assays were performed as described in Materials and Methods. The EC₅₀ values are given in nM with the pEC₅₀ ± S.E.M. values in brackets and the R_max ± S.E.M. values given as the percentage of the maximal response induced by 5-HT. The number of experiments (n) for each set of potency and efficacy data are given in superscript.

	Ca²⁺ Assay I			Ca²⁺ Assay II^{^a}
	5-HT_2AR	5-HT_2BR	5-HT_2CR	5-HT_2AR	5-HT_2CR
	EC₅₀ [EC₅₀ ± S.E.M.]	EC₅₀ [EC₅₀ ± S.E.M.]	EC₅₀ [EC₅₀ ± S.E.M.]	EC₅₀ [EC₅₀ ± S.E.M.]	EC₅₀ [EC₅₀ ± S.E.M.]
	R_max ± S.E.M.⁽ⁿ⁾	R_max ± S.E.M.⁽ⁿ⁾	R_max ± S.E.M.⁽ⁿ⁾	R_max ± S.E.M.⁽ⁿ⁾	R_max ± S.E.M.⁽ⁿ⁾
5-HT	0.61 [9.22 ± 0.03]	0.72 [9.14 ± 0.03]	0.30 [9.52 ± 0.03]	1.0 [9.01 ± 0.06]	1.3 [8.89 ± 0.05]
	100 ⁽⁵⁾	100 ⁽⁵⁾	100 ⁽⁵⁾	100 ⁽⁶⁾	100 ⁽⁶⁾
DOI	0.85 [9.07 ± 0.04]	2.0 [8.69 ± 0.03]	3.3 [8.48 ± 0.04]	0.15 [9.81 ± 0.06]	6.6 [8.18 ± 0.10]
	91 ± 1 ⁽⁴⁾	94 ± 1 ⁽³⁾	96 ± 1 ⁽⁴⁾	85 ± 2 ⁽⁴⁾	85 ± 3 ⁽⁴⁾
25I-NBOMe	0.44 [9.35 ± 0.05]	8.9 [8.05 ± 0.06]	1.1 [8.95 ± 0.03]	n.t.	n.t.
	86 ± 2 ⁽³⁾	80 ± 2 ⁽³⁾	96 ± 1 ⁽⁵⁾
Cimbi-36 ^a	1.6 [8.80 ± 0.05]	7.3 [8.13 ± 0.04]	0.98 [9.01 ± 0.04]	0.95 [9.02 ± 0.09]	0.90 [9.04 ± 0.06]
	88 ± 1 ⁽³⁾	79 ± 1 ⁽³⁾	97 ± 2 ⁽⁴⁾	83 ± 3 ⁽⁴⁾	99 ± 7 ⁽⁴⁾
25CN-NBOH (compound 1)	1.2 [8.92 ± 0.04]	59 [7.23 ± 0.05]	23 [7.65 ± 0.03]	0.41 [9.39 ± 0.10]	52 [7.28 ± 0.07]
	77 ± 5 ⁽⁴⁾	60 ± 2 ⁽³⁾	99 ± 1 ⁽³⁾	80 ± 4 ⁽⁴⁾	93 ± 2 ⁽⁵⁾
25CN-NBOMe (compound 2)	1.2 [8.91 ± 0.04]	12 [7.93 ± 0.03]	9.3 [8.03 ± 0.03]	0.40 [9.40 ± 0.10]	36 [7.44 ± 0.08]
	87 ± 1 ⁽³⁾	79 ± 1 ⁽³⁾	100 ± 1 ⁽³⁾	81 ± 5 ⁽³⁾	96 ± 3 ⁽⁵⁾
25CN-NBF (compound 3)	17 [7.78 ± 0.03]	940 [6.03 ± 0.14]	460 [6.34 ± 0.06]	32 [7.50 ± 0.02]	580 [6.24 ± 0.05]
	82 ± 1 ⁽³⁾	24 ± 3 ⁽³⁾	84 ± 3 ⁽³⁾	54 ± 5 ⁽⁴⁾	50 ± 5 ⁽⁶⁾
25CN-NBMD (compound 4)	5.6 [8.25 ± 0.03]	220 [6.65 ± 0.13]	480 [6.32 ± 0.07]	5.8 [8.23 ± 0.12]	570 [6.24 ± 0.05]
	83 ± 1 ⁽⁵⁾	31 ± 2 ⁽⁴⁾	71 ± 3 ⁽⁵⁾	56 ± 6 ⁽⁴⁾	28 ± 4 ⁽⁵⁾

n.t., not tested.
↵^a The data for Cimbi-36 in Ca²⁺ assay II have been published previously (Herth et al., 2016).