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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- CAS No.: 143691-37-6
- 화학식: C19H19N3O3
- 분자량:337.38
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보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Protocol
- 순도&문서
- References
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Help & FAQs
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Biological Activity
제품 설명
IC50 & Target
[2]|
AMPA Receptor |
In Vitro
GYKI 53405 inhibits kainate-induced whole-cell currents in primary cultured embryonic telencephalic cells of Sprague-Dawley rats, with an IC50 of 7.4 μM[2].
GYKI 53405 inhibits the amplitude of AMPA receptor-mediated population spike potentials in CA1 pyramidal cells of hippocampal slices from male Wistar rats, with an IC50 of 17.8 μM[2].
GYKI 53405 (10-7 M) exhibits no significant binding affinity for GABAA, GABAB or benzodiazepine receptors at a concentration of 10-7 M[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
GYKI 53405 (3 mg/kg; p.o.; single dose) induces anxiolytic-like behavior in male Sprague-Dawley rats in the elevated plus maze test[2].
GYKI 53405 (3 mg/kg; i.p.; single administration) reverses mCPP-induced anxiety-like behavior in male Wistar rats in the light-dark box test[2].
Oral administration of GYKI 53405 produces sedative effects in male NMRI mice, with an ID50 of 9.8 mg/kg[2].
GYKI 53405 (i.p.; single administration) exhibits potent anticonvulsant activity in audiogenic seizure-susceptible DBA/2j mice, with an ED50 value of 1.1 mg/kg for inhibiting tonic extension seizures and an ED50 value of 3.1 mg/kg for inhibiting clonic seizures[3].
GYKI 53405 (i.p.; single dose; 30 min prior to electroshock) inhibits maximal electroshock-induced tonic hindlimb extension seizures in NMRI mice, with an i.p. ED50 of 2.6 mg/kg[3].
GYKI 53405 (3.75-30 mg/kg; i.p.; single administration; 30 minutes prior to MgCl2 injection) exerts dose-dependent neuroprotective activity in the MgCl2-induced global cerebral ischemia model of NMRI mice, with a PD50 of 8.3 mg/kg via intraperitoneal injection, and significantly prolongs the survival time of mice starting from the dose of 7.5 mg/kg[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:WAG/Rij (male, 7-8 months old, 320-420 g, genetic absence epilepsy model)[1]
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Dosage:16 mg/kg
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Administration:i.p.; single dose
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Result:Failed to significantly alter cumulative duration, number, or proportional occurrence of spike-wave discharges during light slow wave sleep compared to vehicle-treated controls.
Failed to significantly alter vigilance states (wakefulness, light slow wave sleep, deep slow wave sleep) compared to vehicle-treated controls.
Failed to significantly alter average paroxysm duration compared to vehicle-treated controls.
Increased frequency of self-grooming compared to vehicle-treated controls.
Induced wet dog shakes in 3 of 8 animals.
Slightly reduced locomotor activity compared to vehicle-treated controls.
Did not induce abnormal behavior or ataxia.
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Animal Model:Sprague-Dawley (male, 220-250 g)[2]
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Dosage:3 mg/kg
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Administration:p.o.; single dose
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Result:Significantly increased the time rats spent in the open arms of the elevated plus-maze.
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Animal Model:Wistar (male, 180-220 g)[2]
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Dosage:3 mg/kg
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Administration:i.p.; single dose
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Result:Significantly reversed the mCPP-induced reduction in movement time in the lit area of the light-dark box.
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Animal Model:NMRI (male, 20-25 g)[2]
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Dosage:1 mg/kg; 9.8 mg/kg
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Administration:p.o.; single dose
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Result:Defined the maximal non-sedating dose as 1 mg/kg p.o.
Produced sedative inhibition of spontaneous motor activity at doses above 1 mg/kg p.o., with an ID50 of 9.8 mg/kg p.o.
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Animal Model:DBA/2j (male, 7-11 g, audiogenic seizure model)[3]
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Dosage:1.1 mg/kg (tonic extensor seizure inhibition); 3.1 mg/kg (clonic seizure inhibition); 5 mg/kg (time-course assessment); over 2.5 mg/kg (tonic fits and death prevention)
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Administration:i.p.; single dose; 15 minutes prior to seizure challenge (for dose-response); single dose (for time-course assessment)
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Result:Achieved an ED50 of 1.1 mg/kg for inhibition of tonic extensor seizures.
Achieved an ED50 of 3.1 mg/kg for inhibition of clonic seizures.
Completely prevented tonic fits and death at doses over 2.5 mg/kg.
Showed more than 80% seizure suppression 3 hours after treatment at 5 mg/kg.
Exhibited strong anticonvulsive effect that gradually disappeared between 3 and 8 hours at 5 mg/kg.
Sustained maximal exit inhibition effect for 4 hours, then gradually decreased to zero between 4 and 8 hours at 5 mg/kg.
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Animal Model:NMRI (Crl: NMRI BR-outbread, male, 20-25 g, maximal electroshock seizure model)[3]
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Dosage:2.6 mg/kg
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Administration:i.p.; single dose; 30 minutes prior to electroshock
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Result:Achieved an ED50 of 2.6 mg/kg for inhibition of tonic hind limb extensor seizures.
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Animal Model:NMRI (Crl: NMRI BR-outbread, male, 20-25 g, MgCl2-induced global cerebral ischaemia model)[3]
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Dosage:3.75 mg/kg; 7.5 mg/kg; 15 mg/kg; 30 mg/kg; 8.3 mg/kg (PD50 dose)
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Administration:i.p.; single dose; 30 minutes prior to MgCl2 injection
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Result:Prolonged survival time in a dose-dependent manner, with a PD50 of 8.3 mg/kg.
Produced significant increases in survival time at doses of 7.5 mg/kg and above.
Chemical Information
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CAS No. 143691-37-6
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분자량 337.38
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화학식 C19H19N3O3
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SMILES
O=C(N1N=C(C=2C=CC(N)=CC2)C=3C=C4OCOC4=CC3CC1C)C
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Synonyms
LY 293606
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
[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]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
GYKI 53405 Related Classifications
HY-15080 Related Classifications
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