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. 2022 Oct 1;27(19):6492. doi: 10.3390/molecules27196492

Table 1.

Agonist properties of compounds Norbo 1–28 at the 5-HT1A receptor.

graphic file with name molecules-27-06492-i001.jpg
5-HT1A Receptor G-Protein Stimulation
Compd X pEC50 EC50 (95% CI, nM) Emax (%) ± SEM
Norbo-1
(exo) 		graphic file with name molecules-27-06492-i002.jpg 5.92 ± 0.09 1200 (778–1850) 174 ± 4.15 *
Norbo-2
(endo) 		graphic file with name molecules-27-06492-i003.jpg 5.78 ± 0.08 1633 (1111–2400) 188 ± 4.9 **
Norbo-3
(exo) 		graphic file with name molecules-27-06492-i004.jpg 6.75 ± 0.1 177 (110–285) && 185 ± 3.2 ***
Norbo-4
(endo) 		graphic file with name molecules-27-06492-i005.jpg 6.74 ± 0.08 181 (123–266) &&& 181 ± 2.4 ***
Norbo-5
(exo) 		graphic file with name molecules-27-06492-i006.jpg 5.0 ± 0.49 96,070 (9001–102,500) & 140 ± 25.2 &&
Norbo-6
endo 		graphic file with name molecules-27-06492-i007.jpg 5.5 ± 0.12 3218 (1228–8435) 131 ± 5.5 &&
Norbo-7
(exo) 		graphic file with name molecules-27-06492-i008.jpg 6.46 ± 0.12 348 (191–632) && 169 ± 3.5 *
Norbo-8
(endo) 		graphic file with name molecules-27-06492-i009.jpg 6.78 ± 0.09 165 (107–253) &&& 167 ± 2.3 *
Norbo-9
(exo) 		graphic file with name molecules-27-06492-i010.jpg 6.68 ± 0.16 207 (95–450) & 149 ± 3.1
Norbo-10
(endo) 		graphic file with name molecules-27-06492-i011.jpg 6.7 ± 0.1 198 (117–333) &&& 163 ± 2.4 #
Norbo-11
(exo) 		graphic file with name molecules-27-06492-i012.jpg no activity no activity no activity
Norbo-12
(endo) 		graphic file with name molecules-27-06492-i013.jpg 5.7 ± 0.25 1875 (549–6407) # 127 ± 5.1 ###,&&&
Norbo-13
(exo) 		graphic file with name molecules-27-06492-i014.jpg no activity no activity no activity
Norbo-14
(endo) 		graphic file with name molecules-27-06492-i015.jpg no activity no activity no activity
Norbo-15
(exo) 		graphic file with name molecules-27-06492-i016.jpg 6.0 ± 0.13 926 (503–1706) 161 ± 4.5
Norbo-16
(endo) 		graphic file with name molecules-27-06492-i017.jpg 6.0 ± 0.11 939 (533–1654) 182 ± 5.5 **,#
Norbo-17
(exo) 		graphic file with name molecules-27-06492-i018.jpg 6.2 ± 0.17 553 (242–1264) 122 ± 2.0 &&&
Norbo-18
(endo) 		graphic file with name molecules-27-06492-i019.jpg 5.6 ± 0.15 2321 (1132–4761) 143 ± 5.1 &&&
Norbo-19
(exo) 		graphic file with name molecules-27-06492-i020.jpg 6.5 ± 0.08 283 (1880–4276) && 162 ± 2.1 *
Norbo-20
(endo) 		graphic file with name molecules-27-06492-i021.jpg 6.7 ± 0.05 195 (1483–2559) &&& 167 ± 1.4 **
Norbo-21
(exo) 		graphic file with name molecules-27-06492-i022.jpg 6.2 ± 0.06 588 (433–798) 181 ± 2.5 **
Norbo-22
(endo) 		graphic file with name molecules-27-06492-i023.jpg 6.1 ± 0.09 782 (513–1192) 186 ± 4.4 ***
Norbo-23
(exo) 		graphic file with name molecules-27-06492-i024.jpg 5.62 ± 0.1 2398 (1143–3567) 181 ± 4.1 **
Norbo-24
(endo) 		graphic file with name molecules-27-06492-i025.jpg 5.76 ± 0.1 1720 (1049–2819) 177 ± 6.1 *
Norbo-25
(exo) 		graphic file with name molecules-27-06492-i026.jpg 5.7 ± 0.1 1911 (1156–3159) # 184 ± 6.4 **
Norbo-26
(endo) 		graphic file with name molecules-27-06492-i027.jpg 5.1 ± 0.1 7502 (2448–23000) 178 ± 22.6 *
Norbo-27
(exo) 		graphic file with name molecules-27-06492-i028.jpg no activity no activity no activity
Norbo-28
(endo) 		graphic file with name molecules-27-06492-i029.jpg no activity no activity no activity
8-OH-DPAT 7.5 ± 0.11 27.2 (18–52) 154 ± 2.3

One-way ANOVA, Bonferroni post-hoc test. Statistical significance was marked as follows: * NORBO vs. 8-OH-DPAT; # exo isomer vs. endo isomer; & vs. corresponding 4-phenylpiperazin-1-yl substituted isomer. One, two or three symbols represent significance levels of 0.05, 0.01, and 0.001, respectively. EC50—half-maximal effective concentration (potency), Emax—efficiency.