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Apimostinel

Names

[ CAS No. ]:
1421866-48-9

[ Name ]:
Apimostinel

[Synonym ]:
NRX-1074
L-Threonyl-L-prolyl-2-benzyl-L-prolyl-L-threoninamide
apimostinel
UNII:TTT1F11FZB
TTT1F11FZB
L-Threoninamide, L-threonyl-L-prolyl-2-(phenylmethyl)-L-prolyl-

Biological Activity

[Description]:

Apimostinel is an oral NMDA receptor partial agonist.

[Related Catalog]:

Signaling Pathways >> Membrane Transporter/Ion Channel >> iGluR
Signaling Pathways >> Neuronal Signaling >> iGluR
Research Areas >> Neurological Disease

[In Vitro]

Apimostinel (NRX-1074) modulates the NMDA receptor in a similar fashion to GLYX-13, but has a synthetic modification to one of the amino acids, conferring increased potency and oral bioavailability[1].

[In Vivo]

In preclinical models the two compounds both appear to be highly efficacious across a number of CNS disorders[1].

[References]

[1]. Naurex's First Orally Active Molecule, NRX-1074, Demonstrates Statistically Significant Improvement in Depression Scores within 24 Hours in Phase 2 Study for Major Depressive Disorder. January 28, 2015.


[Related Small Molecules]

(+)-MK 801 Maleate | CNQX | N-Methyl-D-aspartic acid | ifenprodil tartrate | D-AP5(mM/ml) | DNQX | Ro 25-6981 maleate | Flupirtine maleate | Mibampator | CX546 | Naspm | Talampanel | Centrophenoxine hydrochloride | 24-Hydroxycholesterol

Chemical & Physical Properties

[ Density]:
1.3±0.1 g/cm3

[ Boiling Point ]:
878.7±65.0 °C at 760 mmHg

[ Molecular Formula ]:
C25H37N5O6

[ Molecular Weight ]:
503.591

[ Flash Point ]:
485.2±34.3 °C

[ Exact Mass ]:
503.274384

[ LogP ]:
0.22

[ Vapour Pressure ]:
0.0±0.3 mmHg at 25°C

[ Index of Refraction ]:
1.608

[ Storage condition ]:
2-8℃

Related Compounds