VU6019650 is a novel M5 orthosteric antagonist with high potency (human M5 IC50 = 36 nM), M5 subtype selectivity (>100-fold selectivity against human M1‑4) and favorable physicochemical properties for systemic dosing in preclinical addiction models. In acute brain slice electrophysiology studies, VU6019650 blocked the nonselective muscarinic agonist oxotremorine-M-induced increases in neuronal firing rates of midbrain dopamine neurons in the ventral tegmental area, a part of the mesolimbic dopaminergic reward circuitry. Moreover, VU6019650 also inhibited oxycodone self-administration in male Sprague-Dawley rats within a dose range that did not impair general motor output.
MedKoo Cat#: 466107
Name: VU6019650
CAS#: unknown
Chemical Formula: C18H22FN3O3S2
Exact Mass: 411.1087
Molecular Weight: 411.51
Elemental Analysis: C, 52.54; H, 5.39; F, 4.62; N, 10.21; O, 11.66; S, 15.58
The following data is based on the product molecular weight 411.51 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 |
