MS1768 is a potent D2 Dopamine Receptor G Protein-Biased Partial Agonist. MS1768 selectively activates the Gi/o pathway over β-arrestin2. Unlike the dual D2R/D3R partial agonist cariprazine, MS1768 showed selective agonist activity for D2R over D3R.MS1768 exhibited potent antagonism of dopamine-stimulated β-arrestin2 recruitment. MS1768 directly interacts with S1935.42 on TM5 but has no interactions with extracellular loop 2, which appears to be in contrast to the binding poses of D2R β-arrestin2-biased ligands. In in vivo studies, MS1768showed high D2R receptor occupancy in mice and effectively inhibited phencyclidine-induced hyperlocomotion.
MedKoo Cat#: 464850
Name: MS1768
CAS#: 2349365-88-2
Chemical Formula: C20H30ClN3O
Exact Mass: 363.2077
Molecular Weight: 363.93
Elemental Analysis: C, 66.01; H, 8.31; Cl, 9.74; N, 11.55; O, 4.40
The following data is based on the product molecular weight 363.93 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
