At a constitutively active MC4R, the EC50 value of MTII (with alpha-MSH and NDP-MSH) was identical to that at the wild-type receptor.
In plain wordsIn lab tests, MTII (with two other melanocortin agonists) acted on the engineered active receptor with the same potency as on the normal receptor.
- Peptide
- Melanotan II
- Outcome
- No significant changeAgonist EC50 at constitutively active MC4R versus wild-type MC4R
- Study
n: not reported in source
constitutively active MC4R- Comparator
- Wild-type MC4R
- Outcome group
- Receptor activity and mechanism · Nervous system and cognition
- Studied dose
- Dose not stated
Source sentences
A constitutively active MC4R has been generated which possess EC(50) values for melanocortin agonists (alpha-MSH, NDP-MSH, and MTII) and a pA2 value for the synthetic peptide antagonist SHU9119 identical to the wildtype receptor