Table 2.

Structures and Pharmacological Properties of Compounds Used in This Study^a

compound	structure	EC50** (μM)	LC50¶ (μM)	TI*	[SRA]min# (μM)	Kiσ1R (μM)	Kiσ2R (μM)	Selectivity (σ1R/ σ2R or σ2R/ σ1R)	activity
PD 144418		5.2	>22	>4.2	10	0.0011	0.351	σ1R (319.1 x)	antagonist4
BD1047		19	>25	>1.3	0.5	0.0028	0.013	σ1R (4.6 x)	antagonist5
BD1063		12.3	>50	>4.1	1	0.0027	0.1235	σ1R (45.7 x)	antagonist5
PD-28		5.1	7.8	1.5	0.1	0.00256	0.004	σ1R (1.6 x)	σ1R antagonist σ2R agonist3
rimcazole		3.5	10	2.9	0.5	0.1577	0.0496	σ2R (3.2 x)	antagonist2
haloperidol		13.2	>25	>1.9	2.5	0.00328	0.02921	σ1R (8.9 x)	antagonist4, 5
SA 4503 (Cutamesine)		27.2	>50	>1.8	ND	0.0051	0.0175	σ1R (3.4 x)	agonist7
ANAVEX2–73 (Blarcamesine)		39.5	>50	>1.3	ND	0.442	2.026	σ1R (4.5 x)	agonist8
(+)-pentazocine		35.8	>50	>1.4	ND	.00549	2.46711	σ1R (457 x)	agonist12
DTG		68.1	>50	ND	ND	.0719	.0219	σ2R (3.4x)	agonist10
Other compunds:
amiodarone		4.4	6.3	1.4	ND	.0852	0.171	σ2R (2 x)	unknown
JZ107		3.11	11.41	3.71	5.01	0.0079	0.0051	σ2R (1.5 x)	unknown
JZ103		not active up to 7.5 1	ND1	NA1	Not active	0.339	0.292	σ2R (1.2 x)	unknown
BMY-14802		not active up to 50	>50	NA	ND	0.085	0.0825	σ2R ≈ σ2R	antagonist6

^a**EC₅₀ = Effective concentration for 50% reduction of PrP^Sc levels in ScN2a-RML cells.

^¶LC₅₀ = Lethal concentration for 50% reduction of cell viability based on MTT assay.

^*Therapeutic Index,

^#Minimum concentration capable of preventing hippocampal spine retraction. Numbered footnotes indicate information reported in the following references: 1¹⁴, 2²⁹, 3³⁰, 4³¹, 5³², 6³³, 7²⁴, 8²⁵, 9³⁴, 10³⁵, 11³⁶, 12³⁷. ND = not determined, NA = not applicable.