161832-71-9
Chemical Structure
GYKI 53784
Synonym(s): LY303070
- CAS No.: 161832-71-9
- Formula:C19H20N4O3
- Molecular Weight:352.39
IUPAC Name: (R)-5-(4-aminophenyl)-N,8-dimethyl-8,9-dihydro-7H-[1,3]dioxolo[4',5':4,5]benzo[1,2-d][1,2]diazepine-7-carboxamide
InChIKey: SMGACXZFVXKEAX-LLVKDONJSA-N
SMILES: CNC(N1N=C(C2=CC=C(C=C2)N)C3=C(C[C@H]1C)C=C4C(OCO4)=C3)=O
Biological Activity: GYKI 53784 (LY303070) is an orally active, blood-brain penetrant, selective, non-competitive AMPA receptor antagonist (IC50 = 0.32 μM). GYKI 53784 completely blocks AMPA-mediated synaptic transmission, protects against excitotoxicity, and partially inhibits Kainite (Kainic acid) (HY-N2309) responses, revealing both AMPA and kainate receptors. GYKI 53784 selectively blocks synaptic transmission (IC50 = 365.3 nM) without affecting neuronal excitability, and exhibits potent stereoselective antinociceptive effects via an opioid-independent mechanism. GYKI 53784 is a versatile tool for studying AMPA receptor function in synaptic transmission, excitotoxicity, neuroprotection, pain, and inflammation, with potential relevance to hearing loss, neonatal ischemia, neurodegenerative disorders, schizophrenia, and Alzheimer's disease[1][2][3][4][5][6][7][8][9][10].
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GYKI 53784 | GYKI 53784 (LY303070) is an orally active, blood-brain penetrant, selective, non-competitive AMPA receptor antagonist (IC50 = 0.32 μM). GYKI 53784 completely blocks AMPA-mediated synaptic transmission, protects against excitotoxicity, and partially inhibits Kainite (Kainic acid) (HY-N2309) responses, revealing both AMPA and kainate receptors. GYKI 53784 selectively blocks synaptic transmission (IC50 = 365.3 nM) without affecting neuronal excitability, and exhibits potent stereoselective antinociceptive effects via an opioid-independent mechanism. GYKI 53784 is a versatile tool for studying AMPA receptor function in synaptic transmission, excitotoxicity, neuroprotection, pain, and inflammation, with potential relevance to hearing loss, neonatal ischemia, neurodegenerative disorders, schizophrenia, and Alzheimer's disease. | |||||||||||||||||||||
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- [1]. Ruiz A, et al. Modulation of kainate-induced responses by pentobarbitone and GYKI 53784 in rat abducens motoneurons in vivo. Brain Res. 1999 Feb 13;818(2):421-30. [Content Brief]
- [2]. Ruel J, et al. The selective AMPA receptor antagonist GYKI 53784 blocks action potential generation and excitotoxicity in the guinea pig cochlea. Neuropharmacology. 2000 Aug 23;39(11):1959-73. [Content Brief]
- [3]. Ruel J, et al. Dopamine inhibition of auditory nerve activity in the adult mammalian cochlea. Eur J Neurosci. 2001 Sep;14(6):977-86. [Content Brief]
- [4]. Virdee JK, et al. A high-throughput model for investigating neuronal function and synaptic transmission in cultured neuronal networks. Sci Rep. 2017 Nov 3;7(1):14498. [Content Brief]
- [5]. Valenzuela CF, et al. Acute effects of ethanol on pharmacologically isolated kainate receptors in cerebellar granule neurons: comparison with NMDA and AMPA receptors. J Neurochem. 1998 Oct;71(4):1777-80. [Content Brief]
- [6]. Kapus G, et al. Differential modulation of the GYKI 53784-induced inhibition of AMPA currents by various AMPA-positive modulators in cerebellar Purkinje cells. Eur J Pharmacol. 2000 May 26;397(1):43-7. [Content Brief]
- [7]. Harsing LG Jr, et al. Negative allosteric modulators of AMPA-preferring receptors inhibit [(3)H]GABA release in rat striatum. Neurochem Int. 2000 Jul;37(1):33-45. [Content Brief]
- [8]. Világi I, et al. Protective effect of the antiepileptic drug candidate talampanel against AMPA-induced striatal neurotoxicity in neonatal rats. Brain Res Bull. 2002 Oct 15;59(1):35-40. [Content Brief]
- [9]. Launey T, et al. Excitatory amino acids and synaptic transmission in embryonic rat brainstem motoneurons in organotypic culture. Eur J Neurosci. 1999 Apr;11(4):1324-34. [Content Brief]
- [10]. Székely JI, et al. Apparent antinociceptive and anti-inflammatory effects of GYKI 52466. Eur J Pharmacol. 1997 Oct 8;336(2-3):143-54. [Content Brief]
Keywords
