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. Author manuscript; available in PMC: 2012 Jun 11.
Published in final edited form as: Eur J Pharmacol. 2011 Jan 1;660(1):80–87. doi: 10.1016/j.ejphar.2010.10.101

Table 1.

Summary of in vitro mouse melanocortin receptor pharmacology.

Name Structure Functional
Activity
(nM)
mMC3R
Binding
Affinity (nM)
mMC3R
Functional
Activity
(nM)
mMC4R
Binding
Affinity
(nM)
mMC4R
α-MSH Ac-Ser-Tyr-Ser-Met-Glu-His-Phe-Arg-Trp-Gly-Lys-Pro-Val-NH2 Agonist
0.80±0.14
ND Agonist
5.40±0.62
ND
NDP-MSH Ac-Ser-Tyr-Ser-Nle-Glu-His-DPhe-Arg-Trp-Gly-Lys-Pro-Val-NH2 Agonist
0.098±0.013
0.52±0.10 Agonist
0.21±0.03
0.91±0.85
MTII Ac-Nle-c[Asp-His-DPhe-Arg-Trp-Lys]-NH2 Agonist
0.16±0.03
1.85±0.35 Agonist
0.087±0.008
0.50±0.13
SHU9119 Ac-Nle-c[Asp-His-DNal(2’)-Arg-Trp-Lys]-NH2 Antagonist*
0.32
3.2±1.1 Antagonist
0.040
0.38±0.10
JRH887-9 Ac-His-DPhe-Arg-Trp-NH2 Agonist
160±9.2
ND Agonist
17±2.8
ND
JRH322-18 Ac-His-(pI)DPhe-Arg-Trp-NH2 Antagonist*
50±1.1
270±146 Agonist
25±9.8
4.81±4.5
AGRP(87-132) Antagonist
1.4
2.8±0.4 Antagonist
0.41
3.0±0.3

ND indicates values not reported.

*

Indicates that the antagonists also possess partial agonist activity at the mMC3R. The indicated error represents the standard error of the mean.