TABLE 2

Binding affinities of reference ligands to the hMT1 receptor as measured with either [125I]-SD6, [3H]-MLT, or 2-[125I]-MLT

Experiments were conducted using the recombinant hMT1 receptor expressed in CHO-K1 cells. Data are given as mean ± S.E.M.

hMT1
pKi ± S.E.M.a [3H]-MLTpKi ± S.E.M.a 2-[125I]-MLTpKi ± S.E.M. [125I]-SD6
MLT10.15 ± 0.129.65 ± 0.029.85 ± 0.01
2-I-MLT12.12 ± 0.2010.71 ± 0.0810.49 ± 0.11
4P-PDOT7.56 ± 0.166.85 ± 0.047.07 ± 0.14
Luzindole8.09 ± 0.316.59 ± 0.016.39 ± 0.05
Ramelteon11.82 ± 0.0610.10 ± 0.0910.52 ± 0.07
SD611.33 ± 0.349.94 ± 0.0110.45 ± 0.11
6-Cl-MLT9.25 ± 0.078.73 ± 0.039.08 ± 0.19
2-Br-MLT12.11 ± 0.0810.82 ± 0.1310.56 ± 0.11
S702547.32 ± 0.317.03 ± 0.096.36 ± 0.28
SD1881/6-I-MLT6.83 ± 0.248.84 ± 0.018.87 ± 0.10
SD1882/4-I-MLT7.95 ± 0.077.76 ± 0.127.66 ± 0.07
SD1918/7-I-MLT7.88 ± 0.107.34 ± 0.157.65 ± 0.16
S221538.25 ± 0.098.24 ± 0.147.97 ± 0.12
S271289.03 ± 0.128.92 ± 0.018.96 ± 0.05
Agomelatine10.17 ± 0.259.92 ± 0.019.93 ± 0.02
D600 (+/−)7.76 ± 0.157.04 ± 0.027.19 ± 0.01
DIV8807.44 ± 0.126.10 ± 0.045.89 ± 0.56
5HT>5>5>5
S209287.27 ± 0.267.10 ± 0.086.73 ± 0.10
S754368.53 ± 0.067.88 ± 0.018.31 ± 0.12
S212787.71 ± 0.146.22 ± 0.106.18 ± 0.12
S738938.60 ± 0.068.36 ± 0.167.98 ± 0.06
S778347.87 ± 0.157.09 ± 0.057.11 ± 0.14
S778408.16 ± 0.116.15 ± 0.086.50 ± 0.11

  • 6-Cl-MLT, 6-chloromelatonin; 2-Br-MLT, 2-bromomelatonin; D600, methoxyverapamil; 5HT, 5-hydroxytryptamine; S20928, (N-[2-(1-naphthyl)ethyl]cyclobutanecarboxamide); S21278, N-[2-(6-methoxybenzimidazol-1-yl)ethyl]acetamide; S22153, N-[2-(5-ethylbenzothiophen-3-yl)ethyl]acetamide; S27128-1, N-[2-(2-iodo-5-methoxy-6-nitro-1H-indol-3-yl)ethyl]acetamide; S73893, N-[3-methoxy-2-(7-methoxy-1-naphthyl)propyl]acetamide; S75436, 2-fluoro-N-[3-hydroxy-2-(7-methoxy-1-naphthyl)propyl]acetamide; S77834, N-[(8-methoxy-10,11-dihydro-5H-dibenzo[a,d][7]annulen-10-yl)methyl]acetamide; S77840, 1-[(8-methoxy-10,11-dihydro-5H-dibenzo[a,d][7]annulen-10-yl)methyl]urea; SD1881, N-[2-(6-iodo-5-methoxy-1H-indol-3-yl)ethyl]acetamide; SD1882, N-[2-(4-iodo-5-methoxy-1H-indol-3-yl)ethyl]acetamide; SD1918, N-[2-(7-iodo-5-methoxy-1H-indol-3-yl)ethyl]acetamide.

  • ↵a Data from Legros et al. (2014).