A study of the structure-affinity relationship in SYA16263; is a D₂ receptor interaction essential for inhibition of apormorphine-induced climbing behavior in mice?

ABSTRACT: Dopamine (DA) and serotonin (5-HT) receptors are prime targets for the development of antipsychotics. The specific role of each receptor subtype to the pharmacological effects of antipsychotic drugs remains unclear. Understanding the relationship between antipsychotic drugs and their binding affinities at DA and 5-HT receptor subtypes is very important for antipsychotic drug discovery and could lead to new drugs with enhanced efficacies. We have previously disclosed SYA16263 (5) as an interesting compound with moderate radioligand binding affinity at the D₂ & D₃ receptors (Ki = 124 nM & 86 nM respectively) and high binding affinities towards D₄ and 5-HT_1A receptors (Ki = 3.5 nM & 1.1 nM respectively). Furthermore, we have demonstrated SYA16263 (5

SUBMITTER: Onyameh EK 

PROVIDER: S-EPMC8670397 | biostudies-literature | 2021 Jan

REPOSITORIES: biostudies-literature