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. Author manuscript; available in PMC: 2017 Nov 6.
Published in final edited form as: J Med Chem. 2015 Apr 21;58(11):4638–4647. doi: 10.1021/acs.jmedchem.5b00184

Table 2.

Pharmacology of Truncated hAGRP Peptide Analogues at the Mouse Melanocortin Receptors (Ki=10-pA2).a

Peptide Structure mMC1R mMC3R mMC4R mMC5R
Agonist
EC50 (μM)		 Antagonist
pA2 		Ki
(nM)		 Antagonist
pA2 		Ki
(nM)		 Agonist
EC50 (μM)
hAGRP (87–132)* graphic file with name nihms913780t4.jpg >100,000 8.9±0.2 1.3 9.4±1.0 0.40 >100,000
miniAGRP (87-120)* graphic file with name nihms913780t5.jpg >100,000 8.1±0.1 7.9 8.5±0.1 3.2 >100,000
hAGRP (109-118)* graphic file with name nihms913780t6.jpg 5.1±3.0 >100,000 6.8±0.2 160 >100,000
SHU9119* Ac-Nle-c[Asp-His-DNal(2′)-Arg-Trp-Lys]-NH2 0.64±0.26 nM 9.5 0.32 10.4 0.040 2.31±0.45nM
1 graphic file with name nihms913780t7.jpg 6.1±1.8 6.1±0.3 790 6.5±0.2 320 >100,000
2 graphic file with name nihms913780t8.jpg 11.7±4.0 6.2±0.2 630 6.8±0.2 160 >100,000
3 graphic file with name nihms913780t9.jpg 7.3±3.1 6.2±0.2 630 7.2±0.1 63 >100,000
4 c[Pro-Tyr-Ala-Arg-Phe-Phe-Asn-Ala-Phe-Ala-Tyr-DPro] 17.6±10.1 >100,000 >100,000 >100,000
5 c[Pro-Tyr-Thr-Arg-Phe-Phe-Asn-Ala-Phe-Thr-Tyr-DPro] 11.6±5.0 5.9±0.1 1,300 6.8±0.2 160 >100,000
6 c[Pro-Arg-Phe-Phe-Asn-Ala-Phe-DPro] 4.5±0.2 6.4±0.2 400 7.7±0.1 20 >100,000
a

The indicated errors represent the standard error of the mean determined from at least three independent experiments >100,000 indicates that the compound was examined but lacked agonist activity at up to 100 μM concentrations. (*) The values indicated for hAGRP(87-132), miniAGRP, hAGRP(109-118) and SHU9119 have previously been reported.28,70