Table 5: These ligands bound with potent affinity for α1; ligands bound with values <20 nM at this subtype.

Cook code

WY-TSC-4 (WYS8)0.0070.991.6351.04
SH-TSC-2 (BCCT)0.030.04190.03569.32
QH-II-090 (CGS-8216)0.050.080.120.2517
XLI-2860.0510.0640.1180.684
QH-II-0770.060.080.050.124
QH-II-0920.070.030.04ND0.17ND
JYI-570.0760.0760.131ND0.036ND
QH-II-0850.080.060.02ND0.08ND
XHE-II-0240.090.180.32140.2411
PWZ-007A0.110.10.09ND0.210
CGS82160.13NDNDNDND46
SPH-1210.141.191.72ND4479
QH-II-0750.180.210.25ND1.340
PZII-0280.2ND0.2ND0.321.9
CGS98950.21NDNDNDND9.3
PWZ-00710.230.170.12ND0.4417.31
XHE-III-240.25ND822210328
JYI-420.2570.1460.278ND0.256ND
CGS98960.28NDNDNDND181
JYI-64 (C17H12N4FBr)0.3051.1110.62ND0.875000
PZII-0290.34ND0.79ND0.5210
BRETAZENIL0.350.640.2ND0.512.7
FG82050.42.081.16ND1.54227
YT-50.4210.603436.06ND1.695ND
6-PBC0.491.212.2 ND2.391343
QH-1460.49ND0.76ND7.710000
DM-II-90 (C17H12N4BrCl)0.50510.63ND0.375000
SPH-1650.632.794.85ND10.41150
BCCt0.721518.9ND110.85000
SH-I-048A0.7740.17230.383ND0.11ND
alprazolam0.80.591.43ND1.5410000
Ro15-17880.80.91.05ND0.6148
WYS10 C14H9F3N2O20.883625.6ND548.715.3
WY-B-150.920.830.5820804.42646
WY-A-99-2 (WYS8)0.97211110220002081980
XHE-III-06a12151.837
Xli366 C22H21N3O21NDNDNDNDND
JYI-59 (C22H13N3O2F4)1.082.611.82ND11.55000
WYSC1 C16H16N2O21.0945.4412.3ND69.821.2
MLT-I-701.11.21.1ND40.31000
SVO-8-301.15.35.32.80.615
BCCE1.24.95.7ND26.82700
XHE-III-041.221.12190.4500
XLi350 C17H11ClN2O1.2241.188NDND2.9ND
XHE-III-491.35.54.238.711.385.1
PWZ-009A11.341.311.26ND0.842.03
DM-2391.5ND0.53ND0.146.89
XLi351 C21H21ClN2OSi1.5070.967NDND1.985ND
XLi352 C18H13ClN2O1.560.991NDND1.957ND
TG-4-391.634245.61.423
TG-II-821.62.92.8 ND11000
CM-A871.624.5414.7310004.611000
QH-II-0821.71.81.6ND6.1100
JYI-49 (C20H12N3O2F4Br)1.872.38NDND6.73390
LJD-III-15E1.931419ND70.81000
SPH-3825.410.8ND18.53000
XHE-I-09327.18.91107201162
MSA-IV-352.11621ND9953000
JYI-19 (C23H23N3O3S)2.176205NDND3412.7
FLUNITRAZEPAM2.22.54.5ND2.12000
YCT-52.211.4616.3 ND20010000
TJH-IV-512.3917.414.5ND31610000
WYS13 C20H18N2O32.4421327.5ND1635000
YT-III-252.5315.7865.691ND0.095ND
XHE-III-142.6101327
WYS9 C16H15IN2O22.7222.223.1ND562122
JYI-472.7592.2820.511ND0.427ND
CM-A82a2.788.9324.5110007.491000
TG-4-292.83.92.72.10.183.9
XLi268 C17H13BrN42.81450.6862NDND0.6243ND
JYI-54 (C24H15N3O3F4)2.891726.7ND571890
MMB-II-74324.541.7500125.71000
MMB-III-01631.97210740.26211
MMB-III-1631.97210740.26211
QH-II-080b33.74.7ND241000
YCT-7A323.830.5ND24010000
JYI-32 (C20H15N3O2BrF)3.074.96NDND2.9252.24
Ro15-45133.32.62.5ND0.263.8
XHE-II-0173.310725817294
XLi-JY-DMH ANX33.30.581.9ND4.45000
MLT-II-183.411.711ND22510000
TJH-V-883.4130 ND140.910000
XLI-2TC3.4421.67344.08ND1.121
WYS15 C22H20N2O23.632.0244.3ND76.55000
CM-A573.72740ND2541000
XHE-II-006b3.7151218971441000
JYI-60 3.731.6354.3ND1.75000
RY-0083.757.24.14ND1.1144.3
MLT-II-183.912.224.4ND21010000
OMB-183.91.23.417330.85
WY-B-09-13.9983210004612000
SHU-1-194127481484
ZK 934234.14.26ND4.51000
WY-B-23-2 (WYS11)4.237.739200017669.4
WY-B-23-2 (WYS11)4.237.773 ND17669.4
WY-B-99-14.44.55.582000472000
WY-B-26-24.4544.5742.6620001242000
XHE-II-006a4.74.4201876893531
CM-B014.8313410002861000
PWZ-0854.86138.5ND0.5540
MLT-II-165.0510.4118.4ND26010000
3 PBC5.352.368.8ND5911000
MA-3-PROPOXYL5.352.368.8ND5911000
TJH-IV-435.4230.1948.9ND47510000
DMCM5.698.294ND1.04134
DM-1395.8ND169ND9.25325
XHE-II-073A (R ENRICHED)5.91110151.18140
MSR-I-0326.218.74ND3.374.9
JYI-70 (C19H13N4F)6.32.1NDND0.565000
XLi343 C20H19ClN2OSi6.37517.71NDND150.5ND
3 EBC6.4325.128.2ND8261000
DM-1466.44ND148 ND4.23247
DM-2156.74ND7.42 ND0.2938.28
ZG69A6.816.39.2ND0.8554.6
ZG-69a (Ro15-1310)6.816.39.2ND0.8554.6
WY-B-14 (WYS7)6.84303620001081000
YT-II6.9320.87123.518ND5.119ND
SVO-8-6774126152.3191
MLT-II-347.0415.9522.3ND1581000
SPH-1957.2168.5283.5ND27110000
XHE-I-0657.2171850057500
ZG-2347.2522.149.84ND0.35.25
SH-I-047.36.1365.1 ND7.664ND
XHE-I-0387.3534ND1321000
XHE-III-137.3 ND7.18801.6311
WY-B-257.6406620002632000
CM-A49 (R)7.732.543ND691000
SVO-8-1482586.90.914
TG-4-298.310.26.9ND0.47.61
XHE-II-0028.318133.91.511
WY-B-14 (WYS7)8.5165245 ND17865000
XHE-II-011960393233901000
WY-B-27-29.191117220004492000
QH-II-0639.49.331ND7.73000
JC184 C13H9BrN2OS9.60610.5NDND6.709ND
ZG-2089.711.210.9ND0.384.6
RY-I-31104519ND61000
WY-B-23-110334310001892000
RY-09810.122.216.5ND1.68100
Hz148 C18H15N310.985000NDND2565000
SVO-8-20114028198.6138
XHE-II-073B (S-ENRICHED)111712332.1269
SH-I-08511.084.86613.75ND0.24ND
PWZ-09611.13616.9ND1.0751.5
ZG-16811.210.79.2ND0.479.4
CM-A7711.5151.9105.16100042.621000
WY-B-2012394720001223000
ABECARNIL12.415.37.5ND61000
SH-I-89S12.788.5628.145ND3.23ND
ZG-21312.849.830.2ND3.522.5
EDC-I-07112.983.1NDND3145000
MMB-III-1413136.93331.1333
DM-17313.1ND38.1ND0.78118
XLI-34813.5611.171.578ND82.05ND
EDC-I-09313.6423NDND29125000
diazepam142015ND11ND
XLi223 C22H20BrN3O2148.7181000102000
WYSC2 C15H11F3N2O214.14113170ND51861.2
SH-I-03014.4211.0419.09ND1.89ND
CM-A10014.4944.91123.8100065.311000
RY-03314.85625.3ND1.7222.9
HJ-I-03715.078.12728.29ND0.818ND
YT-615.3187.860.49ND1.039ND
EDC-II-04415.4ND293ND3231000
CM-A5816120184ND10001012
QH-II-067a163152ND1993000
CD-21416.448.242.5ND9.8168
JYI-06 (C23H23N3O4)16.55.485000ND12.65000
CM-A50 (S)175988ND1441000
RY-06117136.7ND0.331
ZG-22417.133.750ND2.530.7
ZG-63A17.321.629.1ND0.654
DM-II-30 (C20H13N3O2BrF3)17.613.428.51ND7.85000
CM-A641860116ND2161000
RY-071195691ND7.2266
WZ-11319.213.213.4ND11.5300
YT-III-2319.8323.6519.87ND1.105ND
CM-E09b202219550.4569
MMB-II-9020245.790.2536

Affinity of compounds at /BzR recombinant subtypes was measured by competition for [3H]flunitrazepam or [3H] Ro15-4513 binding to HEK cell membranes expressing human receptors of compositions 132, 232, 332, 432, 532, and 632 [139]. Data represent the average of at least three determinations with a SEM of ±5%. The structures of these ligands are in the Ph.D. thesis of Clayton (2011) [22] and Supporting Information.