Antiseizure Properties of Histamine H₃ Receptor Antagonists Belonging 3,4-Dihydroquinolin-2(1H)-Ones.

ABSTRACT: H₃R is becoming an attractive and promising target for epilepsy treatment as well as the discovery of antiepileptics. In this work, a series of 6-aminoalkoxy-3,4-dihydroquinolin-2(1H)-ones was prepared to screen their H₃R antagonistic activities and antiseizure effects. The majority of the target compounds displayed a potent H₃R antagonistic activity. Among them, compounds 2a, 2c, 2h, and 4a showed submicromolar H₃R antagonistic activity with an IC₅₀ of 0.52, 0.47, 0.12, and 0.37 μM, respectively. The maximal electroshock seizure (MES) model screened out three compounds (2h, 4a, and 4b) with antiseizure activity. Meanwhile, the pentylenetetrazole (PTZ)-induced seizure test gave a

SUBMITTER: Hua Y 

PROVIDER: S-EPMC10144301 | biostudies-literature | 2023 Apr

REPOSITORIES: biostudies-literature