MCE 的所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务。

S-8510 phosphate

CAS No. : 151466-23-8

MCE 站：S-8510 phosphate

产品活性：S-8510 (phosphate) 是苯二氮 (BDZ) 受体的逆向激动剂，其对 –GABA 和 +GABA 的 K_i 值分别为 34.6 nM 和 36.2 nM。

研究领域：Membrane Transporter/Ion Channel  |  Neuronal Signaling

作用靶点：GABA Receptor

In Vitro: S-8510 has a relatively high affinity to BDZ receptors. The ratio of Ki values for each ligand with and without GABA is defined as the GABA ratio, which is considered as a biochemical index for BDZ receptor ligands. The GABA ratio for S-8510 or CGS8216 is close to the value for flumazenil which is considered as an antagonist or a very weak agonist. S-8510 (10^-7 M) enhances LTP and this enhancement is antagonized by BDZ receptor antagonist, flumazenil. Flumazenil itself does not atfect LTP or evokes responses prior to tetanic stimulation. S-8510 has no effect on the field evoked potential up to 10^-5 M. However, S-8510 increases the amplitude of the population spike at a dose of 10^-4 M, and this effect is completely antagonized by concomitant application of flumazenil (10^-4 M) .

In Vivo: S-8510 or CGS8216 could cause lethal convulsion only in combination with more than 90 mg/kg of PTZ. The proconvulsant activity of S-8510 appears to be selective for PTZ-induced subconvulsive state. Scopolamine decreases the time spending in the area around the platform, indicating the amnesic action of scopolamine. S-8510 and CGS8216 reverses this scopolamine-induced amnesia. S-8510 improves the memory impairment induced by diazepam in the water maze and passive avoidance paradigms as well. S-8510 dose-dependently increases the ACh level up to 100 mg/kg. Both S-8510 and PTZ increases the extracellular level of NA in the hippocampus in a dose-dependent manner. Anxiogenic actions of S-8510, CGS8216 and FG7142 are examined in the water lick conflict paradigm of Wistar rats. S-8510 and CGS8216 fail to affect this behavioral paradigm up to 30 mg/kg. S-8510 significantly decreases the immobility time in the forced swimming test using ddY mice at 40 to 80 mg/kg in a dose-dependent manner. In the tetrabenazine-induced ptosis model, S-8510 significantly reduces the extent of ptosis induced by tetrabenazine at doses more than 10 mg/kg. Again, S-8510 reduces the extent of ptosis only by 39% even at the maximum dose, whereas imipramine exerts more pronounced effects (by about 80% at a dose of 20 mg/kg).

相关产品：(+)-Bicuculline  |  Aminooxyacetic acid hemihydrochloride  |  Gabazine  |  Riluzole  |  γ-Aminobutyric acid  |  Picrotoxin  |  Propofol  |  Vigabatrin  |  (R)-Baclofen  |  CGP52432  |  Furosemide  |  Etomidate  |  Flumazenil  |  Dihydroergotoxine mesylate  |  Ginkgolide A  |  Methionine  |  Emamectin Benzoate  |  Etifoxine  |  Isoguvacine hydrochloride  |  Jujuboside A  |  Topiramate  |  Lotilaner  |  (-)-Securinine  |  alpha-Asarone  |  Clomethiazole  |  Acamprosate calcium  |  DMCM hydrochloride

品牌介绍:
•   MCE (MedChemExpress) 拥有数百种全球独家化合物，我们致力于为全球科研客户提供*新*全的高品质小分子活性化合物；
•   10,000 多种高选择性抑制剂、激动剂涉及各热门信号通路及疾病领域；
•   设有专业的实验中心和严格的质控、验证体系；
•   提供 LC/MS、NMR、HPLC、手性分析、元素分析等各项质检报告，确保产品的高纯度、高品质；
•   产品的生物活性多经各国客户实验验证；
•   Nature, Cell, Science 等多种期刊及制药收录了MCE客户的科研成果；
•   专业团队跟踪*新的制药及生命科学研究进展，为您提供全球*新的活性化合物；
•   与世界各大制药公司及知名科研机构建立了长期的合作。