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Table 1 Binding (Ki) of melanocortin peptides to human MCRs: Indicated values are an average from repeated independent experiments (±SEM)

From: Melanocortin agonists stimulate lipolysis in human adipose tissue explants but not in adipocytes

Test compound

hMC1R

hMC3R

hMC4R

hMC5R

K i (nM)

K i (nM)

K i (nM)

K i (nM)

LY2112688

165 ± 51 (3)

74 ± 27 (3)

0.13 ± 0.01(3)

1713 ± 686 (3)

PG-901

2700 ± 153 (3)

11 ± 0.5 (4)

0.08 ± 0.01 (3)

1.7 ± 0.6 (4)

α-MSH

1.5 ± 0.4 (18)

46 ± 5 (9)

10.16 ± 3.4 (3)

150 ± 30 (7)

ACTH

0.09 ± 0.01 (3)

11.1 ± 1.5 (5)

1.2 ± 0.2 (3)

46 ± 9.5 (5)

  1. Ki values were calculated from competition binding curves of α-MSH, PG-901 and LY2112688 obtained on cells expressing MC1, 3, 4 and 5R as described using a fixed concentration of I125-NDP-α-MSH and increasing amounts of non-labelled competing peptides (1 pM–10 μM)
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BMC Research Notes

ISSN: 1756-0500

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