Source comparison
Document PT-141 Research: Protocol Comparison
Receptor Binding Assay Single IC50 value, MC4R only IC50 values for MC3R, MC4R, MC5R at 3 concentrations Full inhibition curves (6+ points) across all 5 MC subtypes plus functional assays (cAMP, β-arrestin) Without multi-receptor characterization, off-target e
This comparison does not assign a generated winner or score.
- Receptor Binding Assay
- Single IC50 value, MC4R only
- IC50 values for MC3R, MC4R, MC5R at 3 concentrations
- Full inhibition curves (6+ points) across all 5 MC subtypes plus functional assays (cAMP, β-arrestin)
- Without multi-receptor characterization, off-target effects cannot be attributed vs ruled out. This is the single most common reason melanocortin studies get rejected during peer review
- Pharmacokinetic Sampling
- Tmax and one elimination point (2 total)
- 0h, 0.5h, 1h, 2h, 4h, 8h, 12h (7 points minimum)
- Add 0.25h, 1.5h, 6h, 24h for full biphasic curve (11 points)
- Seven-point sampling captures both phases; fewer than seven means you cannot distinguish distribution from elimination kinetics
- Dose Levels Tested
- Single dose (typically 1.75mg)
- Three doses spanning 0.5–3.0mg
- Four or more doses including sub-threshold and supra-therapeutic ranges
- Biphasic dose-response relationships in melanocortin agonists mean three doses can miss the efficacy plateau entirely. Four is the regulatory minimum
- Arousal Assessment Timing
- Single post-dose time point
- Baseline + 60min + 120min (3 assessments)
- Baseline + 30min + 60min + 90min + 120min + 180min (6 assessments)
- Tmax-synchronized arousal must be documented to prove central effect; single-point assessment cannot rule out placebo or contextual arousal
- Adverse Event Stratification
- Total incidence rate only
- Stratified by dose level
- Stratified by dose, onset time, and resolution time
- Nausea at 15min vs 90min post-dose has completely different mechanistic implications. Temporal stratification is what separates mechanistic understanding from descriptive reporting