Type II positive allosteric modulator of α7 nACh receptors (pEC50 = 5.5). Displays no agonist activity at α7 receptors at concentrations up to 0.1 mM; potentiates agonist-evoked responses and reduces rate of desensitization of α7 nAChRs. Exhibits potency and efficacy similar to PNU 120596 (Cat. No. 2498).
|Storage||Store at +4°C|
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions
The following data is based on the product molecular weight 376.47. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||2.66 mL||13.28 mL||26.56 mL|
|5 mM||0.53 mL||2.66 mL||5.31 mL|
|10 mM||0.27 mL||1.33 mL||2.66 mL|
|50 mM||0.05 mL||0.27 mL||0.53 mL|
References are publications that support the biological activity of the product.
Gronlien et al (2007) Distinct profiles of α7 nAChR positive allosteric modulation revealed by structurally diverse chemotypes. Mol.Pharmacol. 72 715 PMID: 17565004
Gill et al (2011) Agonist activation of α7 nicotinic acetylcholine receptors via an allosteric transmembrane site. Proc.Natl.Acad.Sci. 108 5867
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Keywords: TQS, TQS supplier, positive, allosteric, modulators, pam, alpha, α, a7, nicotinic, receptors, nachr, type, II, Nicotinic, (a7), Receptors, 4233, Tocris Bioscience
1 Citation for TQS
Citations are publications that use Tocris products. Selected citations for TQS include:
Abbas (2017) The α7 nicotinic acetylcholine receptor positive allosteric modulator attenuates lipopolysaccharide-induced activation of hippocampal IκB and CD11b gene expression in mice. Drug Discov Ther 11 206 PMID: 28867753
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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* or download your copy today!
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Alzheimer's disease (AD) is a degenerative brain disease and the most common cause of dementia, affecting approximately 47 million people worldwide. Updated in 2015, this poster summarizes the structural and functional changes observed in the progression of this neurodegenerative disease, as well as classic AD drug targets.
Learning & Memory Poster
Recognition memory enables us to make judgements about whether or not we have encountered a particular stimulus before. This poster outlines the cellular mechanisms underlying recognition memory and its links to long-term depression, as well as the use of pharmacological intervention to assess the role of neurotransmitters in recognition memory.
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.