Chemistry:CTW0415

From HandWiki

CTW0415 is an experimental drug from the piperidine family, which acts as a selective positive allosteric modulator of the 5-HT2C receptor, with higher potency than older drugs such as VA012. Structure-activity relationship studies showed that small variations to chain length and side chain substitution could lead to preferential binding for either 5-HT2C or the related 5-HT2A receptor, which subsequently led to the discovery of the related 5-HT2A selective positive allosteric modulator CTW0404.[1][2][3]

References

  1. "Discovery of 4-Phenylpiperidine-2-Carboxamide Analogues as Serotonin 5-HT2C Receptor-Positive Allosteric Modulators with Enhanced Drug-like Properties". Journal of Medicinal Chemistry 63 (14): 7529–7544. July 2020. doi:10.1021/acs.jmedchem.9b01953. PMID 32567857. 
  2. "Serendipitous Discovery of Novel 5-HT2AR Positive Allosteric Modulators (PAMs) Derived From 5-HT2CR PAM Scaffolds". The Journal of Pharmacology and Experimental Therapeutics 389: 87. 2024. doi:10.1124/jpet.087.985400. 
  3. Zhou J, Cunningham KA, Bolinger AA, Anastasio NC, "Novel heterocyclic compounds as serotonin (5-ht) 5-ht2a and 5-ht2c receptor positive allosteric modulators.", WO patent 2023/023287, published 22 February 2024