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CAS No. : 161605-73-8
MCE 国际站:Fanapanel
产品活性:Fanapanel (ZK200775) 是高选择性AMPA拮抗剂。
研究领域:Membrane Transporter/Ion Channel | Neuronal Signaling
作用靶点:iGluR
In Vitro: In the cortical slice preparation assay, ZK200775 gave Ki values of 3.2 nM, 100 nM, and 8.5 μM against quisqualate, kainate, and NMDA, respectively. In the spreading depression assay, it gave IC50 values of 200 nM, 76 nM, 13 μM, and 18 μM against quisqualate, kainate, NMDA, and glycine [1].
In Vivo: ZK200775 elevated the threshold for AMPA- and kainate-induced clonic seizures in mice with a THRD50 (threshold dose) of 2.9 (1.7–4.6) and 1.6 (1.3–2.0) mg/kg i.v., whereas the threshold for NMDA-induced seizures was elevated only in doses, THRD50 of 24.1 (21.9–26.5) mg/kg i.v., which affected motor coordination in the rotating rod, ED50 14.6 (12.1–17.6) mg/kg. ZK200775 in doses of 10 and 30 mg/kg i.v. reduced muscle tone in genetically spastic rats [1]. ZK200775 (3.0 but not 1.5 or 6.0 mg/kg) significantly decreased the nicotine-induced (0.6 mg/kg) DA release in the NAcc and nicotine-stimulated LMA. ZK200775 (1.5, 3.0, 6.0 mg/kg) alone influenced neither DA release nor LMA. ZK200775 showed 34-fold selectivity for AMPA receptors compared to NMDA receptors and no affinity to nicotine receptors
相关产品:Clinical Compound Library Plus | Bioactive Compound Library Plus | Membrane Transporter/Ion Channel Compound Library | Neuronal Signaling Compound Library | Clinical Compound Library | Neurotransmitter Receptor Compound Library | Anti-Alzheimer's Disease Compound Library | Neuroprotective Compound Library | Anti-Parkinson's Disease Compound Library | Neurodegenerative Disease-related Compound Library | Antidepressant Compound Library | Membrane Protein-targeted Compound Library | Membrane Receptor-targeted Compound Library | Highly Selective Inhibitors Library | 6-Methoxy-2-naphthoic acid | NMDA receptor modulator 4 | CIQ | Budipine | Glycine-15N,d2 | AMPA receptor modulator-3 | ZL006 | GluN2B-NMDAR antagonist-1 | Orphenadrine hydrochloride | AMPA receptor modulator-2 | (S)-Willardiine | Kynurenic acid-d5 | N20C hydrochloride | Ifenprodil tartrate | GluN2B receptor modulator-1 | Decanoic acid-d2 | Coluracetam | Caroverine hydrochloride | L-Phenylalanine-d | Dynorphin A (1-10) (TFA) | L-Glutamic acid-d5 | JAMI1001A | Sepimostat | NMDA | CFM-2 | Cyclothiazide | JNJ-61432059 | DQP-1105 | L-Glutamic acid-13C5,15N,d5
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货号: HY-15069
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