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Submit ReviewLoreclezole hydrochloride is a subtype-selective GABAA receptor modulator. Acts as a positive allosteric modulator of β2 or β3-subunit containing receptors. Also acts as a negative modulator at a novel regulatory site, enhancing GABAA receptor sensitization. Inhibits homomeric ρ1 GABAC receptors.
分子量 | 311 |
公式 | C10H6Cl3N3.HCl |
储存 | Desiccate at -20°C |
纯度 | ≥99% (HPLC) |
CAS Number | 2227372-56-5 |
PubChem ID | 45073437 |
InChI Key | AWKSVFLKVCVVFQ-MDZFRNKHSA-N |
Smiles | Cl[H].Cl\C(=C/N1C=NC=N1)C1=C(Cl)C=C(Cl)C=C1 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
DMSO | 1.37 | 5 温和加热 | |
ethanol | 1.37 | 5 温和加热 |
以下数据基于产品分子量 311。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
浓度/溶剂体积/质量 | 1 mg | 5 mg | 10 mg |
---|---|---|---|
0.05 mM | 64.31 mL | 321.54 mL | 643.09 mL |
0.25 mM | 12.86 mL | 64.31 mL | 128.62 mL |
0.5 mM | 6.43 mL | 32.15 mL | 64.31 mL |
2.5 mM | 1.29 mL | 6.43 mL | 12.86 mL |
参考文献是支持产品生物活性的出版物。
Donnelly and Macdonald (1996) Loreclezole enhances apparent desensitisation of recombinant GABAA receptor currents. Neuropharmacology 35 1233 PMID: 9014138
Fisher et al (2000) Loreclezole inhibition of recombinant α1β1γ2L GABAA receptor single channel currents. Neuropharmacology 39 235 PMID: 10670419
Smith et al (2004) Compounds exhibiting selective efficacy for different β subunits of human recombinant γ-aminobutyric acidA receptors. J.Pharmacol.Exp.Ther. 311 601 PMID: 15210837
Thomet et al (2000) Loreclezole as a simple functional marker for homomeric ρ type GABAC receptors. Eur.J.Pharmacol. 408 R1 PMID: 11080529
If you know of a relevant reference for Loreclezole hydrochloride, please let us know.
关键词: Loreclezole hydrochloride, Loreclezole hydrochloride supplier, Subtype-selective, GABAA, receptor, modulators, Receptors, positive, allosteric, PAM, 117857-45-1, 1295, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 Loreclezole hydrochloride 的部分引用包括:
Lemos et al (2011) Stress-hyperresponsive WKY rats demonstrate depressed dorsal raphe neuronal excitability and dysregulated CRF-mediated responses. Neuropsychopharmacology 36 721 PMID: 21160465
Kotak et al (2008) Hearing loss prevents the maturation of GABAergic transmission in the auditory cortex. Mol Med 18 2098 PMID: 18222937
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Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*请注意,Tocris 仅会向正规科研企业/机构地址发送文献。
Written by Ian Martin, Norman Bowery and Susan Dunn, this review provides a history of the GABA receptor, as well as discussing the structure and function of the various subtypes and the clinical potential of receptor modulators; compounds available from Tocris are listed.
The key feature of drug addiction is the inability to stop using a drug despite clear evidence of harm. This poster describes the brain circuits associated with addiction, and provides an overview of the main classes of addictive drugs and the neurotransmitter systems that they target.