Table 2

Classification of the investigated compounds and their allosteric modulation of recombinant α1β2γ2 receptors

No.Substance  ClassAM
 1 DiazepamI+
 2 FlunitrazepamI+
 3 Ro 05-4865IND
 4 Ro 06-6657IND
 5 Ro 05-3448IND
 6 Ro 07-5220IND
 7 Ro 05-4864IND
 8 Ro 05-4654ND
 9 MidazolamII+
10 Ro 21-5259II+
11 Ro 21-6476II+
12 Ro 15-8670II+
13 Ro 23-8125II±  (+)
14 FlumazenilIII±
15 Ro 19-1943III±
16 Ro 15-6750IIIND
17 Ro 15-2486IIIND
18 Ro 40-8547IIIND
19 Ro 41-7889IIIND
20 Ro 42-2320IIIND
21 Ro 40-6129III±
22 Ro 41-0639III±  (+)
23 Ro 41-3380III+
24 Ro 41-2985IIIND
25 Ro 15-3505IIIND
26 Ro 19-0528IIIND
27 Ro 16-0858IIIND
28 Ro 19-1880IIIND
29 Ro 16-0154IIIND
30 Ro 41-8157IIIND
31 BretazenilIIIND
32 Zolpidem+
33 Cl 218872ND
34 DMCM−

Compounds were classified according to their effect on control currents induced by GABA (100%). Relative current amplitudes amounted to 175–400% for positive allosteric modulators, 106–115% for very weak positive allosteric modulators, 94–106% for antagonists, and <94% for negative allosteric modulators.

    • AM, allosteric modulation; +, positive allosteric modulator; ± (+), very weak positive allosteric modulator; ±, antagonist; ± (−), very weak negative allosteric modulator; −, negative allosteric modulator.

    • ND, not determined.