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Biological Activity for Loreclezole hydrochloride
Loreclezole 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.
Technical Data for Loreclezole hydrochloride
|Storage||Desiccate at -20°C|
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for Loreclezole hydrochloride
|Solvent||Max Conc. mg/mL||Max Conc. mM|
|DMSO||1.37||5 with gentle warming|
|ethanol||1.37||5 with gentle warming|
Preparing Stock Solutions for Loreclezole hydrochloride
The following data is based on the product molecular weight 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.
|Concentration / Solvent Volume / Mass||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|
Product Datasheets for Loreclezole hydrochloride
References for Loreclezole hydrochloride
References are publications that support the biological activity of the product.
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.
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Keywords: Loreclezole hydrochloride, Loreclezole hydrochloride supplier, Subtype-selective, GABAA, receptor, modulators, Receptors, positive, allosteric, PAM, 117857-45-1, 1295, Tocris Bioscience
2 Citations for Loreclezole hydrochloride
Citations are publications that use Tocris products. Selected citations for Loreclezole hydrochloride include:
Kotak et al (2008) Hearing loss prevents the maturation of GABAergic transmission in the auditory cortex. Mol Med 18 2098 PMID: 18222937
Lemos et al (2011) Stress-hyperresponsive WKY rats demonstrate depressed dorsal raphe neuronal excitability and dysregulated CRF-mediated responses. Neuropsychopharmacology 36 721 PMID: 21160465
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Literature in this Area
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*Please note that Tocris will only send literature to established scientific business / institute addresses.
GABA Receptors Scientific Review
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.
Epilepsy is a brain disease that affects 60 million people globally. More than 20 anti-seizure drugs are currently available, but these do not address the underlying causes of the condition. This poster summarizes current knowledge about the development of the condition and highlights some approaches that have disease-modifying effects in proof-of-concept studies.
Peripheral sensitization is the reduction in the threshold of excitability of sensory neurons that results in an augmented response to a given external stimulus. This poster outlines the excitatory and inhibitory signaling pathways involved in modulation of peripheral sensitization. The role of ion channels, GPCRs, neurotrophins, and cytokines in sensory neurons are also described.
Schizophrenia is a debilitating psychiatric disorder that affects 1% of the worldwide population. This poster describes the neurobiology of Schizophrenia, as well as highlighting the genetic and environmental factors that play a fundamental role in the etiology of the disease. The current and emerging drug targets are also discussed.