Rapastinel, also known as GLYX-13 and BV-102, is a novel antidepressant drug approved as an adjunctive therapy for the treatment of treatment-resistant major depressive disorder. It is a centrally active, intravenously administered (non-orally active) amidated tetrapeptide (Thr-Pro-Pro-Thr-NH2) that acts as a selective, weak partial agonist (mixed antagonist/agonist) of an allosteric site at the glycine site of the NMDA receptor complex (Emax ≈ 25%).[1][2] The drug is a rapid-acting and long-lasting antidepressant as well as robust cognitive enhancer by virtue of its ability to both inhibit and enhance NMDA receptor-mediated signal transduction.
MedKoo Cat#: 535868
Name: Rapastinel acetate
CAS#: 491872-39-0 (acetate)
Chemical Formula: C20H35N5O8
Exact Mass: 473.2486
Molecular Weight: 473.53
Elemental Analysis: C, 50.73; H, 7.45; N, 14.79; O, 27.03
Solvent | mg/mL | mM | |
---|---|---|---|
Solubility | |||
Soluble in DMSO | 0.0 | 100.00 |
The following data is based on the product molecular weight 473.53 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 |