ML398 is a potent and selective dopamine D4 receptor antagonist which has been used in scientific research.[1][2][3] It shows high affinity for the dopamine D4 receptor (Ki = 36 nM) and negligible affinity for other four dopamine receptors (>20,000 nM).[2][3] As such, the drug shows more than 100-fold selectivity for the dopamine D4 receptor over the other dopamine receptors.[2][3] It has been found to reverse cocaine-induced hyperlocomotion.[2] The chemical synthesis of ML398 has been described.[2][4] ML398 was first described in the scientific literature by 2014.[2]
References
- ↑ "Delving into the Latest Updates on ML-398 with Synapse". Synapse. 23 May 2026. Retrieved 7 July 2026.
- 1 2 3 4 5 6 Berry CB, Bubser M, Jones CK, Hayes JP, Wepy JA, Locuson CW, et al. (September 2014). "Discovery and Characterization of ML398, a Potent and Selective Antagonist of the D4 Receptor with in Vivo Activity". ACS Medicinal Chemistry Letters. 5 (9): 1060–1064. doi:10.1021/ml500267c. PMC 4160761. PMID 25221667.
- 1 2 3 Berry CB, Locuson CW, Daniels JS, Lindsley CW, Hopkins CR (2015). "Discovery and characterization of ML398, a potent and selective chiral morpholine based antagonist of the dopamine 4 (D4) receptor". Probe Reports from the NIH Molecular Libraries Program. PMID 25834901.
- ↑ Torres S, Velasco M, Gallegos-Rojas JÁ, Bernès S, Orea ML, Terán JL, et al. (2019). "A Concise Stereoselective Synthesis of ( R )-2-Benzylmorpholine and ML398 from ( R )-(−)-2-Phenylglycinol". Journal of Heterocyclic Chemistry. 56 (9): 2677–2682. doi:10.1002/jhet.3657. ISSN 0022-152X.