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. Author manuscript; available in PMC: 2015 Feb 1.
Published in final edited form as: Bioorg Med Chem Lett. 2013 Dec 25;24(3):850–854. doi: 10.1016/j.bmcl.2013.12.086

Table 1.

Inhibition of VGLUT by QDCs at 250 µM.*

Compound Structure 3H-L-Glu
Uptake
(% of control
5,6-benz-quinoline-2,4-dicarboxylic acid: 5,6-BQDC (1) graphic file with name nihms552120t1.jpg 75 ± 4
7,8-benzo-quinoline-2,4-dicarboxylic acid: 7,8-BQDC (2) graphic file with name nihms552120t2.jpg 34 ± 1
5,6-naphtho-quinoline-2,4-dicarboxylic acids: 5,6-NQDC (3) graphic file with name nihms552120t3.jpg 17 ± 3
7,8-naphtho-quinoline-2,4-dicarboxylic acid: 7,8-NQDC (4) graphic file with name nihms552120t4.jpg 26 ± 1
Estrone (Es) graphic file with name nihms552120t5.jpg 98 ± 8
Estrone sulfate (Es-S) graphic file with name nihms552120t6.jpg 52 ± 8
Estrone hemisuccinate (Es-Hs) graphic file with name nihms552120t7.jpg 109 ± 20
Pregnenolone (PGNE) graphic file with name nihms552120t8.jpg 100 ± 4
Pregnenolone acetate (PGNE-OAc) graphic file with name nihms552120t9.jpg 86 ± 5
Pregnenolone sulfate (PGNE-S) graphic file with name nihms552120t10.jpg 31 ± 3
Pregnanolone (PGNA) graphic file with name nihms552120t11.jpg 100 ± 6
Pregnanolone sulfate (PGNA-S) graphic file with name nihms552120t12.jpg 15 ± 4
*

Inhibitory activity is reported as mean % of control (uptake of 250 µM 3H-L-Glu in the absence of QDCs) ± SEM, n ≥ 3. Lower uptake values represent a greater degree of inhibition.