Table 3.
Additional In Vitro Binding and Functional Data for Selected Compounds.
| compd | D3 mitogenesis IC50±S.E.M., nMa | D2 mitogenesis IC50±S.E.M., nMa | D3 beta arrestin IC50 ± S.E.M., nM | 5-HT1A [3H]-8-OH-DPAT Ki ± S.E.M., nMa | 5HT1A [35S]GTPγS EC50 ± S.E.M., nM (% agonist)a | 5-HT2A [125I]DOI Ki ± S.E.M., nMa |
|---|---|---|---|---|---|---|
| 8a | 390±130 | NDe | 699±18 | 49.0±13 | 71.6±1.3 (73) | 2060±460 |
| 8b | 256±79 | NDe | IAf | 159±37 | 1080±380 (123) | 98±34 |
| 8c | 440±130 | NDe | NDe | 37.9±9.4 | 134±44 (60) | 4800±1300 |
| 8d | 430±120 | NDe | IAf | 1150±340 | NDe | >8800 |
| 8e | 780±170 | NDe | 1240±220 | 73.0±17 | 600±170 (76) | 3000±1100 |
| 8f | 1430±480 | 1600±300 | IAf | 501±65 | NDe | 274±56 |
| 8g | 820±300 | NDe | IAf | 101±19 | 1430±670 (83) | 3240±840 |
| 8h | 520±170 | NDe | 1220±310 | 223±60 | 2140±510 (88) | 212±77 |
| 8i | 214±47 | NDe | IAf | 299±30 | NDe | >10,000 |
| 8j | 800±310 | NDe | IAf | 6000±1400 | ND | 4800±1200 |
| 8k | 83±30 | 421±47 | 3210±140 | 139±33 | 440±150 (57%) | 3030±400 |
| 8l | 17.0±5.2 | NDe | 3770±2900 | 2140±640 | NDe | 3290±480 |
| 8m | 1140±310 | NDe | 2990±100 | 1170±190 | NDe | 3540±910 |
| 8n | 320±100; 4.9±1.3 (14.9)b | NDe | IAf | IAf | NDe | 272±79 |
| 8o | 255±43 | NDe | IAf | IAf | NDe | 1910±350 |
| 15b | 918±61 | NDe | NDe | IAf | NDe | 2580±400 |
| (±)2 | 29.9±5.76c | 4370±59.4 171.2±60.5 (22%)b,c |
495 (n=2) | 104±23.5c | NDe | ND |
| sulpiride | 66.22±10.89 | 10.28±1.23 | 560±170 | NDe | NDe | NDe |
a
Data were obtained through the NIDA Addiction Treatment Discovery Program contract with Oregon Health & Science University (Y1 DA 5007-05).
b
The first value is the antagonist IC50, the second value is the agonist EC50 with % stimulation in parentheses.
c
data previously reported in ref. 11.
d
data previously reported in ref. 6.
e
ND = Not determined;
f
IA= <50% inhibition at a concentration of 10 μM.