At 13 polymorphic human MC4Rs with reduced endogenous agonist potency, MTII showed nanomolar to subnanomolar agonist potency.
In plain wordsIn lab tests, MTII still activated 13 variant forms of the human MC4R receptor at very low concentrations.
- Peptide
- Melanotan II
- Outcome
- Not applicableAgonist potency at 13 polymorphic hMC4Rs
- Study
humann: not reported in source
polymorphic human MC4Rs- Outcome group
- Receptor activity and mechanism · Pharmacology
- Studied dose
- Dose not stated
Source sentences
These studies resulted in the NDP-MSH, MTII, AMW3-130, THIQ, and AMW3-106 ligands possessing nanomolar to subnanomolar agonist potency at the hMC4R polymorphisms examined in this study
1 context sentence(design, population, supporting numbers)
Herein, we have studied 13 polymorphic hMC4Rs that have been identified to possess statistically significant decreased endogenous agonist potency with synthetic peptides and small molecules attempting to identify ligands that can pharmacologically rescue the hMC4R polymorphic agonist response.