gyki 52466

GYKI 52466 is a synthetic small molecule that acts as a **selective, non-competitive antagonist of the AMPA receptor (α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid receptor)**[1][5][6]. Its primary mechanism is **negative allosteric modulation of ionotropic AMPA receptors**, resulting in inhibition of glutamate-mediated excitatory neurotransmission. This leads to pronounced **anticonvulsant and neuroprotective effects** in multiple preclinical models, with particular utility in seizure prevention and attenuation of excitotoxic injury[1][3][5][6]. There is evidence for a secondary metabotropic action as an **inverse agonist at G-protein coupled receptors**, reducing basal GPCR activity and conferring prolonged neuroprotection after preconditioning, especially in hippocampal neurons[1][6]. GYKI 52466 has been studied mainly in animal models of seizures, spinal cord injury, and neuroprotection, but development has been limited by adverse motor and cognitive side effects at effective doses[1]. The drug is typically used in research and is not approved for clinical use. Chemical formula: C17H15N3O2[2][4][5]. CAS 102771-26-6[4].

Other names

1-(4-aminophenyl)-4-methyl-7,8-methylenedioxy-5H-2,3-benzodiazepine4-(8-methyl-9H-[1,3]dioxolo[4,5-h][2,3]benzodiazepin-5-yl)anilineGYKI 52466 hydrochlorideGYKI52466 hydrochlorideGYKI-52466 hydrochloride4-(8-Methyl-9H-1,3-dioxolo(4,5-h)(2,3)benzodiazepin-5-yl)benzenamine