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. 2021 Mar 6;48:101206. doi: 10.1016/j.molmet.2021.101206

Table 2.

Functional pharmacology of the melanocortin ligands in cloned murine and human melanocortin receptors.

Peptide Murine receptorsa
 Human receptors
MC1R
 MC3R
 MC4R
 MC5R
 MC1R
 MC3R
 MC4R
 MC5R
EC50 (nM) EC50 (nM) pA2 EC50 (nM) pA2 EC50 (nM) EC50 (nM) pA2 EC50 (nM) pA2 EC50 (nM) pA2 EC50 (nM) pA2
α-MSH 0.039 [203]
0.15 [191]
0.23 [189]
0.55 [204]
0.70 [205]		 0.73 [189]
0.76 [191]
0.79 [204]
1.21 [168]
2.10 [205]
3.8(r) [169]		 2.6 [205]
3.07 [189]
4.0 [191]
5.37 [204]
18(r) [206]		 0.41 [189]
0.44 [204]
0.58(r) [207]
0.59 [191]
1.07 [170]
2.00 [205]		 0.0022 [203]
0.091 [157]
1.01 [175]		 0.669 [157]
∼1 [12]
1.04 [175]
16.7 [208]		 0.210 [157]
0.88 [202]
1.34 [209]
1.5 [210]
2.56 [181]
4.69 [175]
9.2 [208]		 0.807 [157]
10.5 [175]
35.3 [208]
57 [211]
β-MSHb 12(r) [207] 4.24 [175] 1.59 [175] 6.62 [175] 23.7 [175]
209 [211]
β-MSH(5–22) 1.1 [168] 6.5 [170] 9.33 [181]
β-MSH(1–22) 0.21 [203] 3.8(r) [169] 0.013 [203] ∼10 [12] 0.24 [202]
0.30 [209]
3.24 [181]
γ2-MSH >100 [203]
680 [205]
1090 [191]		 0.64 [168]
3.8(r) [169]
34.6 [191]
38 [205]		 420 [205]
869 [191]		 35.1 [191]
42 [205]
42.9 [170]		 0.082 [203]
3.05 [175]
300 [212]		 0.487 [175]
5.9 [183]
700 [212]		 93.7 [175]
>100 [210]
107 [209]
170 [202]
260 [183]
710 [212]		 490 [183]
500 [175]
550 [212]
2700 [205]
ACTH(1–24) 0.46(r) [207] 0.86 [202]
1.63 [209]		 30 [211]
ACTH(1–39) 0.37 [203] 3.3 [168]
3.8(r) [169]		 24(r) [206] 6.02 [170]
6.2(r) [207]		 0.0083 [203] ∼1 [12] 0.68 [210]
Setmelanotide 0.28(r) [185] 0.26 [184],d
5.8 [175,185]		 0.69 [184],d
5.3 [175,185]
30.9 [208]		 <0.032 [184],d
0.27 [175,185]
1.7(L) [184],c,d
5.7 [208]		 109.7 [208] 1600 [175,185]
Bremelanotide 0.095 [184],d 2.4 [184],d 0.25 [184],d
4.1(L) [184],c,d
MTII 0.020 [204]
0.037 [213]
0.06 [214]		 0.011 [213]
0.16 [204]
0.18 [214]		 0.083 [213]
0.087 [204]
0.15 [214]		 0.14 [214]
0.16 [204]
0.17 [213]		 <0.032 [184],d
0.199 [175]
0.30 [215]		 0.204 [184],d
0.512 [175]
0.75 [216]
1.3 [215]
33.9 [208]		 0.011 [209]
0.017 [202]
<0.032 [184],d
0.0542 [175]
0.19 [216]
0.35(L) [184],c,d
2.9 [215]
8.6 [208]		 2.8 [216]
3.3 [215]
5.33 [175]
33.9 [208]
Ac-His-DPhe-Arg-Trp-NH2 14.1 [191]
25.6 [189]		 55.5 [191]
195 [189]		 10.2 [189]
13.7 [191]		 3.46 [189]
9.8 [191]		 4.3 [217]
228 [178]		 7.1 [217] 0.57 [209]
0.72 [202]
548 [217]
793 [178]		 3.9 [217]
NDP-MSH 0.0015 [203]
0.030 [218,219]
0.038 [204]
0.04 [214]
0.21 [218]
1.0 [205]		 0.09 [205]
0.098 [204]
0.10 [189]
0.19 [218]
0.23 [214]
0.24 [191]
0.43 [168]
1.6(r) [169]		 0.10 [205]
0.21 [204]
0.32 [189]
0.41 [220]
0.46 [191]
0.47 [214]		 0.050 [170]
0.071 [204]
0.086 [189]
0.18 [220,221]
0.22 [205]
0.31 [191]
1.0(r) [207]		 0.0016 [203]
0.023 [157]
0.462 [175]		 0.109 [175]
0.132 [157]
0.24 [183]
6.8 [208]		 0.011 [210]
0.017 [157]
0.022 [202]
0.023 [209]
0.0752 [175]
0.20 [183]
0.4 [208]		 0.23 [183]
0.253 [175]
0.53 [205]
1.1 [208]
1.8 [211]
SHU9119 0.64 [213]
0.98 [214]		 Partial agonist [214] 8.8 [214]
9.5 [213]		 9.3 [214]
10.4 [213]		 Partial agonist [214]
2.31 [213]		 0.036 [157]
1.5 [215]		 Partial agonist [157] 8.3 [157]
8.7 [216]		 9.1 [216]
9.3 [157]		 0.25 [216]
0.434 [157]
1.2 [215]
Agouti 9.3 [222] 8.2 [222] 9.9 [222] 8.9 [222]
AgoutiYY 8.4 [197] 8.6 [197] 9.3 [197]
AGRP (87–132) >100,000 [204] 8.7 [220]
8.9 [204]		 8.7 [220]
9.4 [204]		 >100,000 [204] 8.4 [199] 8.20 [202]
8.6 [199]
8.76 [209]
a

Values labelled with a (r) represent data from cloned rat receptors. Unlabelled numbers represent mouse receptors.

b

Potency EC50 β-MSH values were split depending on the sequence used. If a sequence was not provided in the paper, values are listed in the β-MSH row.

c

Values labelled with a (L) were reported using a low receptor expression.

d

Values shown were converted from pEC50 values reported in the source publication.