New dual 5-HT1A and 5-HT7 receptor ligands derived from SYA16263.

ABSTRACT: We have previously reported that dual 5-HT_1A and 5-HT₇ receptor ligands might find utility as treatment options for various CNS related conditions including cognitive and anxiolytic impairments. We have also more recently reported that SYA16263 has antipsychotic-like properties with an absence of catalepsy in animal models ascribed to its ability to recruit β-arrestin to the D₂ receptor. However, SYA16263 also binds with very high affinity to 5-HT_1AR (Ki = 1.1 nM) and a moderate affinity at 5-HT₇R (Ki = 90 nM). Thus, it was of interest to exploit its pharmacophore elements in designing new dual receptor ligands. Using SYA16263 as the lead molecule, we have conducted a limited structure-affinity relationship (SAFIR) study by modifying v

SUBMITTER: Ofori E 

PROVIDER: S-EPMC7984856 | biostudies-literature | 2021 Mar

REPOSITORIES: biostudies-literature