CX1739
 | |
| Clinical data | |
|---|---|
| Other names | CX-1739 |
| Legal status | |
| Legal status | |
| Identifiers | |
| |
| CAS Number | |
| PubChem CID | |
| ChemSpider | |
| UNII | |
| Chemical and physical data | |
| Formula | C13H15N3O3 |
| Molar mass | 261.281 g·mol−1 |
| 3D model (JSmol) | |
| |
| |
CX1739 is an investigational new drug developed by Cortex Pharmaceuticals that is being evaluated for the treatment of a wide range of conditions such ADHD,[1] autism,[2] opioid-induced respiratory depression,[3] [4] and central sleep apnea.[5] It is a positive allosteric modulator of the AMPA receptor (ampakine).
CX1739 has similar pharmacological effects and favorable safety profile to older "Type II" ampakines such as CX516 and CX717, but with higher potency and improved bioavailability, unlike "Type I" ampakines such as CX614 which have been found to produce neurotoxicity at high doses.[6]
As with related ampakine compounds CX1739 has nootropic (memory enhancment) effects,[1] and was originally investigated for applications such as treatment of ADHD and dementia, but in the course of testing it was found to be effective as a respiratory stimulant and for facilitating nerve repair, so recent research has focused on potential use for conditions such as sleep apnoea and recovery from spinal cord injury.[7][8]
See also
[edit]References
[edit]- ^ a b Radin DP, Lippa A, Rana S, Fuller DD, Smith JL, Cerne R, et al. (2025). "Amplification of the therapeutic potential of AMPA receptor potentiators from the nootropic era to today". Pharmacology, Biochemistry, and Behavior. 248: 173967. doi:10.1016/j.pbb.2025.173967. PMC 11849398. PMID 39894310.
- ^ Silverman J, Oliver C, Karras M, Gastrell P, Crawley J (2013). "AMPAKINE enhancement of social interaction in the BTBR mouse model of autism". Neuropharmacology. 64 (1): 268–282. doi:10.1016/j.neuropharm.2012.07.013. PMC 3445667. PMID 22801296.
- ^ Radin DP, Zhong S, Cerne R, Shoaib M, Witkin JM, Lippa A (2024). "Low-Impact Ampakine CX1739 Exerts Pro-Cognitive Effects and Reverses Opiate-Induced Respiratory Depression in Rodents". Future Pharmacology. 4: 173–187. doi:10.3390/futurepharmacol4010012.
- ^ Xiao D, Xie F, Xu X, Zhou X (2020). "The Impact and Mechanism of Ampakine CX1739 on Protection Against Respiratory Depression in Rats". Future Medicinal Chemistry. 12 (23): 2093–2104. doi:10.4155/fmc-2020-0256. PMID 33030058.
- ^ Ren J, Ding X, Greer JJ (2015). "Ampakines Enhance Weak Endogenous Respiratory Drive and Alleviate Apnea in Perinatal Rats". American Journal of Respiratory and Critical Care Medicine. 191 (6): 704–710. doi:10.1164/rccm.201410-1898OC. PMID 25594679.
- ^ Radin DP, Zhong S, Cerne R, Witkin JM, Lippa A (2024). "High Impact AMPAkines Induce a Gq-Protein Coupled Endoplasmic Calcium Release in Cortical Neurons: A Possible Mechanism for Explaining the Toxicity of High Impact AMPAkines". Synapse. 78 (5). New York, N.Y.: e22310. doi:10.1002/syn.22310. PMID 39304968.
- ^ Rana S, Sunshine MD, Greer JJ, Fuller DD (2021). "Ampakines Stimulate Diaphragm Activity after Spinal Cord Injury". Journal of Neurotrauma. 38 (24): 3467–3482. doi:10.1089/neu.2021.0301. PMC 8713281. PMID 34806433.
- ^ Witkin JM, Radin DP, Rana S, Fuller DD, Fusco AF, Demers JC, et al. (2024). "AMPA receptors play an important role in the biological consequences of spinal cord injury: Implications for AMPA receptor modulators for therapeutic benefit". Biochemical Pharmacology. 228: 116302. doi:10.1016/j.bcp.2024.116302. PMC 12132907. PMID 38763261.
Further reading
[edit]- Radin DP, Cerne R, Witkin JM, Lippa A (2025). "Safety, Tolerability, and Pharmacokinetic Profile of the Low-Impact Ampakine CX1739 in Young Healthy Volunteers". Clinical Pharmacology in Drug Development. 14 (1): 50–58. doi:10.1002/cpdd.1475. PMID 39302241.