Table 5.
Affinity of substituted methcathinones and standard compounds at h5-HT1A, h5-HT2A and h5-HT2C receptors.
| Inhibition of radioligand binding Ki ± sem (µM) (n) | |||
|---|---|---|---|
| Drug | h5-HT1A [3H]8OH-DPAT |
h5-HT2A [125I]DOI |
h5-HT2C [125I]DOI |
| Butylone | >96# (3) | 118 ± 17(3) | 41 ± 12(3) |
| 4-FMC | 71.6 ± 3.4(3) | 10.0 ± 1.0(3) | 12.6 ± 2.4(4) |
| MDPV | 14.8 ± 3.8(3) | 207 ± 29 (3) | 107 ± 30(3) |
| Mephedrone | >91# (3) | 9.0 ± 1.5(4) | 9.1 ± 2.1(4) |
| Methylone | 63.28 ± 0.98 (3) | 48.5 ± 8.0 (3) | 10.6 ± 1.8(3) |
| Naphyrone | 4.64 ± 0.60 (4) | 17.7 ± 2.6(4) | 23.2 ± 6.4 (3) |
| METH | 5.90 ± 0.85 (3) | 43.5 ± 9.1 (4) | 10.2 ± 2.9(9) |
| MDMA | 14.1 ± 2.4(5) | 8.3 ± 1.2 (4) | 1.36 ± 0.44(6) |
| Methcathinone | 29.1 ± 3.6(4) | 29.2 ± 3.3 (4) | 16.0 ± 4.2 (4) |
| 5-HT | 0.00304 ± 0.00053(6) | 0.0076 ± 0.0013(10) | 0.00170 ± 0.00054(7) |
| LSD | 0.00132 ± 0.00032(10) | 0.000148 ± 0.000030(4) | 0.00129 ± 0.00016(3) |
| WAY 100,635 | 0.000161 ± 0.000040(3) | ||
| Ketanserin | 0.0156 ± 0.0048(4) | ||
| SB242084 | 0.00247 ± 0.00050(8) | ||
(n) Number of independent experiments conducted in duplicate.
#
If some experiments yielded Ki values less than 100 µM and other experiments yielded Ki values greater than 100 µM, the latter experiments were assigned a value of 100 µM and averages calculated. The actual value is greater than that average and no standard error is reported.
Binding Hill slopes for [3H]8-OH-DPAT ranged from −0.59 to −1.04, for h5-HT2A [125I]DOI ranged from −0.85 to −1.17, and for h5-HT2C [125I]DOI ranged from −0.65 to −1.46.