. 2018 Jun 22;23(7):1512. doi: 10.3390/molecules23071512

Table 2.

Data from electrophysiological studies of GABA(A) receptor agonists.

Cmpd	Source	Assay	Subtype	c(GABA)	P_max [%]	c [µM]	EC₅₀ [µM]	Ref.
5	Piper nigrum	Xenopus oocytes	α₁β₂γ_2S	EC_5–10	302 ± 26	300	52 ± 9	[25]
6	Piper nigrum	Xenopus oocytes	α₁β₂γ_2S	EC_5–10	187 ± 10	300	56 ± 19	[25]
20		Xenopus oocytes	α₁β₂γ₂	1 µM	295 ± 50	300		[33]
31–33	Cussonia zimmermannii	Xenopus oocytes	α₁β₂γ₂		110–440		0.6–3.5	[40]
46	Scuttelaria baicalensis	Xenopus oocytes	α₁β₂γ₂	EC₁	57 ± 6	30	3	[48]
66		Xenopus oocytes	α₁β₂γ₂	EC_2–5	47 ± 5	10		[57]
82		Xenopus oocytes	α₄β₄δ		68 ± 5	100		[76]
88	Sophora flavescens	Xenopus oocytes	α₁β₂γ_2S	EC_3–10	578.5 ± 68.8		8.1 ± 1.4	[79]
89	Sophora flavescens	Xenopus oocytes	α₁β₂γ_2S	EC_3–10	267.6 ± 56.6		5.0 ± 2.3	[79]
90	Sophora flavescens	Xenopus oocytes	α₁β₂γ_2S	EC_3–10	604.9 ± 108.2		15.0 ± 3.6	[79]
92	Morus alba	Xenopus oocytes	α₁β₂γ_2S		730.4 ± 76.7	100	13.8 ± 1.5	[81]
93	Morus alba	Xenopus oocytes	α₁β₂γ_2S		715.8 ± 56.1	100	16.7 ± 2.0	[81]
94	Morus alba	Xenopus oocytes	α₁β₂γ_2S		719.3 ± 63.3	100	13.4 ± 1.6	[81]
95	Adenocarpus cinncinatus	Xenopus oocytes	α₁β₂γ_2S	EC_5–10	552.73 ± 84.07	500	2.8 ± 1.4	[82]
97	Glycyrrhiza glabra	Dorsal raphe neurons	α₂β_2/3γ_2L	2 µM	581 ± 91	3		[83]
98		Dorsal raphe neurons		EC₁₀	151	10		[84]
99	Sophora flavescens	Xenopus oocytes	α₁β₂γ_2S	EC_3–10	891.5 ± 163.0		4.0 ± 2.4	[79]
101		HEK-293T cells	α₁β₂γ₂				290 ± 28	[86]
102	Acorus calamus	Xenopus oocytes	α₁β₂γ_2S	EC_5–10	1200 ± 163	500	171.5 ± 34.6	[87]
103	Magnolia officinalis	Xenopus oocytes	α₁β₂γ_2S		1315 ± 281	300	36.2 ± 14.7	[88]
106		HEK-293T cells					10.1 ± 10.5	[93]
107		HEK-293T cells					16.9 ± 0.3	[93]
108		HEK-293T cells					10.5 ± 2.3	[93]
109		Cortical neurons		10 µM	158 ± 20	1	0.04258	[94]
110	Piper methysticum	Neonatal rat gastric-brainstem preparation			31.5 ± 3.9	300	93	[95]
111	Kadsura longipedunculata	Xenopus oocytes	α₁β₂γ_2S	EC_5–10	218.1 ± 20.8		21.8 ± 7.5	[96]
112	Kadsura longipedunculata	Xenopus oocytes	α₁β₂γ_2S	EC_5–10	245.0 ± 59.6		52.2 ± 24.8	[96]
113	Kadsura longipedunculata	Xenopus oocytes	α₁β₂γ_2S	EC_5–10	885.8 ± 291.2		135.6 ± 85.7	[96]
114	Kadsura longipedunculata	Xenopus oocytes	α₁β₂γ_2S	EC_5–10	168.7 ± 41.5		36.6 ± 16.4	[96]
115	Kadsura longipedunculata	Xenopus oocytes	α₁β₂γ_2S	EC_5–10	129.7 ± 36.8		118.7 ± 54.4	[96]
116	Kadsura longipedunculata	Xenopus oocytes	α₁β₂γ_2S	EC_5–10	395.6 ± 27.2		31.5 ± 7.1	[96]
117	Kadsura longipedunculata	Xenopus oocytes	α₁β₂γ_2S	EC_5–10	288.8 ± 23.7		12.8 ± 3.1	[96]
118	Kadsura longipedunculata	Xenopus oocytes	α₁β₂γ_2S	EC_5–10	793.4 ± 107.4		79.2 ± 19.4	[96]
119	Kadsura longipedunculata	Xenopus oocytes	α₁β₂γ_2S	EC_5–10	362.5 ± 87.1		54.6 ± 28.8	[96]
121	Cnidium monnieri	Xenopus oocytes	α₁β₂γ_2S				54 ± 13	[99]
121	Angelica pubescens	Xenopus oocytes	α₁β₂γ_2S	EC_5–10	25.8 ± 12.7	300		[100]
122		Xenopus oocytes	α₁β₂γ_2S				57 ± 4	[99]
124		Xenopus oocytes	α₁β₂γ_2S		550 ± 71	100	25 ± 8	[99]
125		Xenopus oocytes	α₁β₂γ_2S				34 ± 6	[99]
126	Angelica pubescens	Xenopus oocytes	α₁β₂γ_2S	EC_5–10	204.5 ± 33.2	300		[89]
127	Cnidium monnieri	Xenopus oocytes	α₁β₂γ_2S		124 ± 11	100	14 ± 1	[99]
127	Angelica pubescens	Xenopus oocytes	α₁β₂γ_2S	EC_5–10	273.6 ± 39.4	300		[100]
128	Angelica pubescens	Xenopus oocytes	α₁β₂γ_2S	EC_5–10	61.2 ± 20.2	300		[100]
129	Angelica pubescens	Xenopus oocytes	α₁β₂γ_2S	EC_5–10	38.0 ± 21.3	300		[100]
131	Haloxylon scoparium	Xenopus oocytes	α₁β₂γ_2S		144.6 ± 35.3	500	140.2 ± 51.2	[106]
132	Rhizoma curcumae oil	HEK-293T cells	α₁β₂γ₂	1 µM	120 ± 6	50		[107]
133		Xenopus oocytes	α₁β₂γ_2L	EC₁₀ (3 µM)	126 ± 15	100	58.24	[108]
135	Pholidota chinensis	Xenopus oocytes	α₁β₂γ_2S	EC_3–10	786.8 ± 72.1	300	175.5 ± 25.5	[109]
136	Pholidota chinensis	Xenopus oocytes	α₁β₂γ_2S	EC_3–10	1512.9 ± 176.5	300	52.5 ± 17.0	[109]
137	Adenocarpus cinncinatus	Xenopus oocytes	α₁β₂γ_2S	EC_5–10	771.09 ± 57.94	500	40.7 ± 4.08	[82]
138	Adenocarpus cinncinatus	Xenopus oocytes	α₁β₂γ_2S	EC_5–10	640.02 ± 53.56	500	8.6 ± 1.6	[82]
139	Adenocarpus cinncinatus	Xenopus oocytes	α₁β₂γ_2S	EC_5–10	490.97 ± 22.34	500	18.8 ± 2.3	[82]
140	Juncus effusus	Xenopus oocytes	α₁β₂γ_2S	EC_5–10	188 ± 20	300	31 ± 8	[110]
141	Juncus effusus	Xenopus oocytes	α₁β₂γ_2S	EC_5–10	239 ± 18	300	27 ± 6	[110]
149		Xenopus oocytes	α₁β₂γ_2L	EC_5–14	1251 ± 73	300	247.7	[115]
150		Xenopus oocytes	α₁β₂γ_2L	EC_15–24	1106 ± 73	300	236.9	[115]
151		Xenopus oocytes	α₁β₂γ_2L	EC_25–39	571 ± 123	300	111.2	[115]
152		Xenopus oocytes	α₁β₂γ_2L	EC_15–24	968 ± 88	300	190.5	[115]
153		Xenopus oocytes	α₁β₂γ_2L	EC_15–24	377 ± 156	300	469.1	[115]
160		Xenopus oocytes	α₁β₃γ_2S	EC₂₀	416 ± 72	100		[123]
161		Xenopus oocytes	α₁β₂γ₂	1 µM	224 ± 85	300		[33]
162		Xenopus oocytes	α₁β₂γ₂	1 µM	453 ± 176	300		[33]
163		Xenopus oocytes	α₁β₂γ₂	1 µM	340 ± 70	300		[33]
164		Xenopus oocytes	α₁β₂γ₂	1 µM	213 ± 105	300		[33]
165		Xenopus oocytes	α₁β₂γ₂	1 µM	477 ± 68	300		[33]
166		Xenopus oocytes	α₁β₂γ₂	1 µM	809 ± 118	300		[33]
167		HEK-293T cells	α₁β₂γ₂	1 µM	156 ± 26	1000		[33]
168		HEK-293T cells	α₁β₂γ₂	1 µM	168 ± 42	1000		[33]
169		HEK-293T cells	α₁β₂γ₂	1 µM	116 ± 56	1000		[33]
170		HEK-293T cells	α₁β₂γ₂	1 µM	179 ± 55	1000		[33]
171		Xenopus oocytes	α₁β₂γ₂	1 µM	737 ± 234	300		[33]
175		Xenopus oocytes	α₁β₂γ_2S	EC₂₀	496 ± 113	100		[131]
175		Xenopus oocytes	α₁β₂γ_2S	EC₂₀	96.2 ± 3.8	50		[132]
176	Kadsura longipedunculata	Xenopus oocytes	α₁β₂γ_2S	EC_5–10	834.6 ± 77.5		70.6 ± 12.2	[96]
177		HEK-293T cells	α₁β₂γ₂	1 µM	117 ± 57	1000		[33]
178		HEK-293T cells	α₁β₂γ₂	1 µM	115 ± 52	1000		[33]
179	Rhizoma curcumae oil	HEK-293T cells	α₁β₂γ₂	1 µM	133 ± 10	50		[107]
180	Rhizoma curcumae oil	HEK-293T cells	α₁β₂γ₂	1 µM	251 ± 16	300	34.4 ± 2.9	[107]
182	Valeriana officinalis	Xenopus oocytes	α₁β₂γ_2S	EC_5–10	400.0 ± 77.6	100	13.6 ± 4.1	[135]
183	Kadsura longipedunculata	Xenopus oocytes	α₁β₂γ_2S	EC_5–10	383.5 ± 89.3		57.3 ± 19.7	[96]
184	Kadsura longipedunculata	Xenopus oocytes	α₁β₂γ_2S	EC_5–10	413.4 ± 66.3		118.4 ± 29.9	[96]
188	Acorus calamus	Xenopus oocytes	α₁β₂γ_2S	EC_5–10	241 ± 23.1	500	34.0 ± 6.7	[87]
189	Acorus calamus	Xenopus oocytes	α₁β₂γ_2S	EC_5–10	669 ± 112	1000	64.8 ± 19.8	[87]
190	Acorus calamus	Xenopus oocytes	α₁β₂γ_2S	EC_5–10	164 ± 42.9	500	109.4 ± 46.6	[87]
191	Acorus calamus	Xenopus oocytes	α₁β₂γ_2S	EC_5–10	886 ± 105	1000	135.1 ± 34.4	[87]
192	Acorus calamus	Xenopus oocytes	α₁β₂γ_2S	EC_5–10	588 ± 126	300	65.3 ± 21.6	[87]
193	Aristolochia manshuriensis	Xenopus oocytes	α₁β₂γ_2S	EC_5–10	70.7 ± 2.6	1000	56.02 ± 5.09	[140]
194	Atractylodes macrocephala	Xenopus oocytes	α₁β₂γ_2S	EC_1–10	96 ± 3	300	12 ± 1	[141]
195	Atractylodes macrocephala	Xenopus oocytes	α₁β₂γ_2S	EC_1–10	166 ± 122	300	70 ± 17	[141]
196	Atractylodes macrocephala	Xenopus oocytes	α₁β₂γ_2S	EC_1–10	157 ± 12	300	99 ± 20	[141]
198	Acremonium strictum	Xenopus oocytes	α₁β₁γ_2S	EC₂₀	180	1	0.05 ± 0.02	[145]
202	Boswellia serrata	Xenopus oocytes	α₁β₂γ_2S	EC_5–10	397.5 ± 34.0	100	8.7 ± 1.3	[148]
203	Platycladus orientalis	Xenopus oocytes	α₁β₂γ_2S	EC_5–10	425.2 ± 96.5	500	141.6 ± 68.0	[149]
204	Platycladus orientalis	Xenopus oocytes	α₁β₂γ_2S	EC_5–10	855.7 ± 114.9	500	33.2 ± 8.7	[149]
207	Curcuma kwangsiensis	Xenopus oocytes	α₁β₂γ_2S	EC_3–10	309.4 ± 35.6	300	24.9 ± 8.8	[151]
208	Curcuma kwangsiensis	Xenopus oocytes	α₁β₂γ_2S	EC_3–10	211.0 ± 26.0	300	35.7 ± 8.8	[151]
220	Panax ginseng	Xenopus oocytes	α₁β₂γ_2S	10 µM			53.2 ± 12.3	[162]
221	Panax ginseng	Xenopus oocytes	α₁β₂γ_2S	10 µM	23.3 ± 1.4	100	23.1 ± 8.6	[163]
222	Panax ginseng	Xenopus oocytes	α₁β₂γ_2S	10 µM	54.1 ± 1.7	100	17.1 ± 2.2	[163]
228	Actaea racemosa	Xenopus oocytes	α₁β₂γ_2S	EC_3–10	378 ± 64	300	36 ± 14	[167]
229	Actaea racemosa	Xenopus oocytes	α₁β₂γ_2S	EC_3–10	256 ± 40	300	28 ± 17	[167]
230	Actaea racemosa	Xenopus oocytes	α₁β₂γ_2S	EC_3–10	289 ± 45	300	26 ± 7	[167]
231	Actaea racemosa	Xenopus oocytes	α₁β₂γ_2S	EC_3–10	1947 ± 185	300	27 ± 8	[167]