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. Author manuscript; available in PMC: 2024 Jun 21.

Published in final edited form as: ACS Chem Neurosci. 2024 Jun 7;15(12):2396–2407. doi: 10.1021/acschemneuro.4c00086

Table 1.

Southern Region SAR


Cmpd No.	Aryl	R	R’	% Inhibition at 10 μM^a					D_4.4 IC₅₀ (nM)^a	D_4.4 K_i(nM)^a
Cmpd No.	Aryl	R	R’	D_4.4	D_2S	D_2L	D₃	D₁	D_4.4 IC₅₀ (nM)^a	D_4.4 K_i(nM)^a
4		H	H	88%	8%	9%	9%	21%	2790	250
5		H	H	94%	25%	24%	27%	35%	200	56
6		H	H	90%	15%	3%	25%	−4%	150	43
7		H	H	20%	-	-	-	-	-	-
8		H	H	62%	-	-	-	-	-	-
9		H	H	91%	25%	24%	62%	24%	81	22
10		H	H	66%	-	-	-	-	-	-
11		H	H	66%	-	-	-	-	-	-
12		H	H	92%	24%	16%	19%	27%	280	76
13		CH₃	H	85%	-	-	-	-	990	270
14		H	CH₃	89%	-	-	-	-	1920	530

^a

Values were obtained from Eurofins Discovery. See Supporting Information for more details.