Table 1.

Inhibitory effects of thiadiazole derivatives on P2X7R activity.

Compound	% Inhibition (a)	% LDH release (b)
9a	89.2 ± 2.2	58.1 ± 4.8
9b	30 ± 0.6	15.8 ± 1.3
9c	28.25 ± 0.7	10 ± 0.7
9d	62.25 ± 4.02	46.3 ± 5.12
9e	90.2 ± 0.4	36.3 ± 11.0
9f	15.7 ± 0.6	42.5 ± 0.4
9g	90.75 ± 1.1	22.6 ± 0.3
9h	64 ± 3.7	15 ± 1.9
11a	92.5 ± 0.3	34.1 ± 2
11b	89.7 ± 2.6	45.7 ± 1.7
11c	29.2 ± 0.3	24 ± 1.7
11d	69.75 ± 0.7	36.94 ± 10.6
13a	90.5 ± 1.4	8 ± 0.6
13b	90.7 ± 1.6	19.6 ± 0.6
13c	92 ± 0.4	45.3 ± 1.4
13d	71 ± 0.2	38.5 ± 6.2
14a	91 ± 1	32 ± 1
14b	92 ± 2	26.6 ± 1.2
14c	92.5 ± 0.4	10.6 ± 0.5
14d	54.7 ± 0.5	43 ± 5
BBG (c)	78.8 ± 3.8	13.2 ± 2.6

(a) % Inhibition values at 10 μM are expressed as percentage relative to the maximum uptake of propidium stimulated by 1 mM ATP only. Data values are expressed as mean ± SD. All experiments were repeated at least three and five times.

(b) % LDH release values at 10 μM are expressed as percentage relative to the maximum LDH release caused by 0.05% Triton X-100 only. Data values are expressed as mean ± SD. All experiments were repeated at least three and four times.

(c) BBG concentration of 750 nM.

LDH, lactate dehydrogenase; ATP, adenosine triphosphate; BBG, Brilliant Blue G.