GYKI 53655 hydrochloride (Synonyms: LY300168 hydrochloride) |
| Catalog No.GC14842 |
AMPA and kainate receptor antagonist
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 143692-48-2
Sample solution is provided at 25 µL, 10mM.
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GYKI53655 hydrochloride is an α-amino-3-hydroxy-5-methylisoxazole-4-propionic acid (AMPA) antagonist.
GYKI53655 hydrochloride (LY300168) inhibits α-amino-3-hydroxy-5-methylisoxazole-4-propionic acid (AMPA) (10 μM)-induced responses with IC50 value of 5.9±0.1 μM. GYKI53655 hydrochloride inhibits AMPA (10 μM) responses inrecombinant G1uR4 expressing HEK293 cells with IC50 value of 4.6±0.4 μM. Using 3 μM cyclothiazide the inhibition produced by GYKI53655 hydrochloride is 79±2% (n=4 cells). GYKI53655 hydrochloride produces only small inhibitions of kainate-induced currents at 30 μM and inhibits kainate-induced currents at a concentration of 100 μM by 12±2 (n=4) and 18±4 (n=4), respectively. GYKI53655 hydrochloride inhibits AMPA receptor-mediated responses in cerebella Purkinje neurons with an IC50 value of 1.5±0.1 μM[1].
GYKI53655 hydrochloride (4 mg/kg) is found to have a short-lasting depressant effect on neuronal responses to iontophoreticα-amino-3-hydroxy-5-methylisoxazole-4-propionic acid (AMPA), with a half-recovery time of approximately 7 min. GYKI53655 hydrochloride (4 and 8 mg/kg) substantially depresses or completely abolishes AMPA responses. Results demonstrate the dose-dependence of GYKI53655 hydrochloride (2 to 8 mg/kg) in depressing responses to AMPA. At the highest doses tested, GYKI53655 hydrochloride reduces AMPA responses to a comparable degree[2]. Tonic fit and death are completely prevented by GYKI53655 hydrochloride at dose over 5.0 mg/kg. The ED50 value of GYKI53655 hydrochloride is 2.2 mg/kg i.p. The maximal effects of GYKI53655 hydrochloride lasts 3 h then the exit inhibition effect of GYKI53655 hydrochloride falls to 20% 1 h later[3].
References:
[1]. Bleakman D, et al. Activity of 2,3-benzodiazepines at native rat and recombinant human glutamate receptors in vitro: stereospecificity and selectivity profiles. Neuropharmacology. 1996;35(12):1689-702.
[2]. Chizh BA, et al. A comparison of intravenous NBQX and GYKI 53655 as AMPA antagonists in the rat spinal cord. Br J Pharmacol. 1994 Jul;112(3):843-6.
[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 Jun;55(3):387-91.
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Cell experiment: |
Whole-cell voltage clamp recordings are made from single cells with use of the tight seal whole cell configuration of the patch-clamp technique. Experiments are performed at room temperature (20 to 22°C) and recorded on an amplifier. GYKI53655 hydrochloride application is via a series of perfusion lines to a multi-barrelled applicator and exchange of solutions under the present recording conditions is approximately 100 msec. For the acutely isolated cerebella Purkinje neurons, GYKI53655 hydrochloride application is by bath perfusion and occurs within approximately 15 sec. Curve fitting to data points is based upon the equationy=100(Dn/(Dn+IC50n)), where the slope of the line n is fixed to a value of 1 and D is the antagonist concentration. Statistical significance is determined by one-way ANOVA followed by Student- Newman-Keulstest[1]. |
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Animal experiment: |
Experiments are performed on 27 male Wistar rats (260 to 350 g). Briefly, rats are anaesthetized with halothane in O2 and tracheal, carotid and jugular cannulae are inserted. The lumbo-thoracic spinal cord is exposed and cut at T9-T11 and the animal is prepared for extracellular recordings of single dorsal horn neurone action potentials. Anaesthesia after surgery is maintained with α-chloralose. Jugular cannulae are inserted. GYKI53655 hydrochloride is administered intravenously. The effect of GYKI53655 hydrochloride is expressed quantitatively as percentages of control excitatory amino acids (EAA) responses, where control is taken as the mean of the last 3 pre-drug counts; mean values±s.e.mean are indicated. No corrections for spontaneous activity are made[2]. |
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References: [1]. Bleakman D, et al. Activity of 2,3-benzodiazepines at native rat and recombinant human glutamate receptors in vitro: stereospecificity and selectivity profiles. Neuropharmacology. 1996;35(12):1689-702. |
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| Cas No. | 143692-48-2 | SDF | |
| Synonyms | LY300168 hydrochloride | ||
| Chemical Name | (S)-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 hydrochloride | ||
| Canonical SMILES | O=C(NC)N([C@@H](C)CC1=C2)N=C(C(C=C3)=CC=C3N)C1=CC4=C2OCO4.Cl | ||
| Formula | C19H20N4O3.HCl | M.Wt | 388.85 |
| Solubility | DMSO : ≥ 160 mg/mL (411.47 mM); H2O : 8 mg/mL (20.57 mM; Need ultrasonic and warming) | Storage | 4°C, sealed storage, away from moisture |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.5717 mL | 12.8584 mL | 25.7169 mL |
| 5 mM | 0.5143 mL | 2.5717 mL | 5.1434 mL |
| 10 mM | 0.2572 mL | 1.2858 mL | 2.5717 mL |
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
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Average Rating: 5 (Based on Reviews and 29 reference(s) in Google Scholar.)
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