143691-37-6
Chemical Structure
GYKI 53405
Synonym(s): LY 293606
- CAS No.: 143691-37-6
- Formula:C19H19N3O3
- Molecular Weight:337.38
IUPAC Name: 1-(5-(4-aminophenyl)-8-methyl-8,9-dihydro-7H-[1,3]dioxolo[4',5':4,5]benzo[1,2-d][1,2]diazepin-7-yl)ethan-1-one
InChIKey: JACAAXNEHGBPOQ-UHFFFAOYSA-N
SMILES: O=C(N1N=C(C=2C=CC(N)=CC2)C=3C=C4OCOC4=CC3CC1C)C
Biological Activity: GYKI 53405 (LY 293606) is a non-competitive, orally active AMPA receptor antagonist. GYKI 53405 shows no significant binding affinity for GABAA, GABAB or benzodiazepine receptors. GYKI 53405 increases self-grooming behavior, induces wet dog-like shakes, reduces spontaneous activity, produces anxiolytic-like behavior, reverses the anxiogenic effect induced by mCPP, inhibits locomotor activity, suppresses sound-induced and maximal electroshock-induced seizures, prolongs survival in global cerebral ischemia models, and exhibits sustained anticonvulsant effects at doses below the sedation threshold. GYKI 53405 can be used in research related to absence epilepsy, anxiety disorders and global cerebral ischemia[1][2][3].
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GYKI 53405 | GYKI 53405 (LY 293606) is a non-competitive, orally active AMPA receptor antagonist. GYKI 53405 shows no significant binding affinity for GABAA, GABAB or benzodiazepine receptors. GYKI 53405 increases self-grooming behavior, induces wet dog-like shakes, reduces spontaneous activity, produces anxiolytic-like behavior, reverses the anxiogenic effect induced by mCPP, inhibits locomotor activity, suppresses sound-induced and maximal electroshock-induced seizures, prolongs survival in global cerebral ischemia models, and exhibits sustained anticonvulsant effects at doses below the sedation threshold. GYKI 53405 can be used in research related to absence epilepsy, anxiety disorders and global cerebral ischemia. | |||||||||||||||||||||
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- [1]. Jakus R, et al. Effect of two noncompetitive AMPA receptor antagonists GYKI 52466 and GYKI 53405 on vigilance, behavior and spike-wave discharges in a genetic rat model of absence epilepsy. Brain Res. 2004;1008(2):236-244. [Content Brief]
- [2]. Kapus GL, et al. Antagonism of AMPA receptors produces anxiolytic-like behavior in rodents: effects of GYKI 52466 and its novel analogues. Psychopharmacology (Berl). 2008;198(2):231-241. [Content Brief]
- [3]. Szabados T, et al. Comparison of anticonvulsive and acute neuroprotective activity of three 2,3-benzodiazepine compounds, GYKI 52466, GYKI 53405, and GYKI 53655. Brain Res Bull. 2001;55(3):387-391. [Content Brief]
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