. Author manuscript; available in PMC: 2008 Mar 24.

Published in final edited form as: Curr Top Med Chem. 2007;7(11):1107–1119. doi: 10.2174/156802607780906645

Table 1.

Melanotropin Peptide Analogues Selective for Human Melanocortin-3 Receptor

a) Agonists/Partial Agonists
Ref.	Sequence	hMC1R			hMC3R			hMC4R			hMC5R
Ref.	Sequence	IC₅₀,nM	EC₅₀,nM	% max effect	IC₅₀,nM	EC₅₀,nM	% max effect	IC₅₀,nM	EC₅₀,nM	% max effect	IC₅₀,nM	EC₅₀,nM	% max effect
[43]	H-Tyr-Val-Met-Gly-His-Phe-Arg-D-Trp-Asp-Arg-Phe-Gly-OH	ND	ND	ND	6.7 ± 1	0.33 ± 0.01	100	600 ± 70	100 ± 11	99	340 ± 40	82 ± 10	97
[69]	c[Nle-Arg-D-Phe-Arg-Trp-Glu]-NH₂	1,400±10 0	>10,000	0	140±10	1.2±0.2	112	270±26	174±18	63	68.0±2	>10,000	0
[62]	H-D-Phe-c[Asp-Pro-D-Phe-Arg-Trp-Lys)-NH₂	ND	ND	ND	3.7±0.05	4.87±0.5	61	700±100	>10,000	0	1,100±180	>10,000	0
b) Antagonists
Ref.	Sequence	hMC1R			hMC3R			hMC4R			hMC5R
Ref.	Sequence	IC₅₀,nM	EC₅₀,nM	% max effect	IC₅₀,nM	EC₅₀,nM	% max effect	IC₅₀,nM	EC₅₀,nM	% max effect	IC₅₀,nM	EC₅₀,nM	% max effect
[60]	c[(O)C-(CH₂)₃,-C(O)-His-D-Nal(2′)Arg-Trp-Lys]-NH₂	ND	ND	ND	5.9±0.19	>10,000	0	220±13	1,200±200	22.8	26±1.4	1.01±0.09	81
[61]	Ac-Nle-c[Asp-Tic-D-Nal(2′)Arg-Trp-Lys]-NH₂	ND	ND	ND	6.7±0.6	>10,000	0	3.7±0.3	>10,000	0	1.24±0.13	2.05±0.2	102
[61]	Ac-Nle-c[Asp-Acpc-D-Na1(2′)-Arg-Trp-Lys]-NH₂	ND	ND	ND	2.5±0.2	>10,000	0	270±30	>10,000	0	4.1±0.5	390±50	50
[63]	Ac-c[Cys-Glu-Pro-D-Nal(2′)-Arg-Trp-Cy5]-Pro-Pro-Lys-Asp-NH₂	ND	ND	ND	31±10	>10,000	0	17,000	>10,000	0	97,000	>10,000	0
[63]	Ac-c[Pen-Glu-His-D-Nal(2′)-Arg-Trp-Cys]-Pro-Pro-Lys-Asp-NH₂	ND	ND	ND	3.0±0.5	>10,000	0	750±100	>10,000	0	94±11	>10,000	0
[52]	H-Tyr-Val-Nle-Gly-His-D-Phe-Arg-D-Nal(2′)-Asp-Arg-Phe-Gly-OH	0.7±0.1	2.0±0.2	87	6.0±0.5	>10,000	0	6,0±1	36±4	100	5.0±1	200±20	67
[69]	c[Nle-Val-D-Nal(2′)-Arg-Trp-Glu]-NH₂	4,000	>10,000	0	1.7±0.1	>10,000	0	180±20	16±0.3	13	2.2±0.5	>10,000	0
[71]	Ac-Nle-c[Asp-Aba-D-Phe-Arg-Trp-Lys]-NH₂	>10,000	>10,000	0	50±6	>10,000	0	>10,000	>10,000	0	2,900±300	>10,000	0