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B 973B New
Positive allosteric modulator of α7 nAChRs (EC50 ~0.3 μM); active enantiomer. Increases potency of acetylcholine (EC50 values are 0.007 mM and 0.3 mM in the presence and absence of B 937B, respectively). Potentiates peak acetylcholine-induced currents 6-fold relative to maximal acetylcholine, and slows channel desensitization, resulting in a 6900-fold increase in charge transfer. Decreases paw edema in vivo. Analgesic.
|Storage||Store 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.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions
The following data is based on the product molecular weight 452.5. 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|
|1 mM||2.21 mL||11.05 mL||22.1 mL|
|5 mM||0.44 mL||2.21 mL||4.42 mL|
|10 mM||0.22 mL||1.1 mL||2.21 mL|
|50 mM||0.04 mL||0.22 mL||0.44 mL|
References are publications that support the biological activity of the product.
Garai et al (2018) B-973, a novel α7 nAChR Ago-PAM: racemic and asymmetric synthesis, electrophysiological studies, and in vivo evaluation. ACS Med.Chem.Lett. 9 1144 PMID: 30429960
Post-Munson et al (2017) B-973, a novel piperazine positive allosteric modulator of the α7 nicotinic acetylcholine receptor. Eur.J.Pharmacol. 15 799 PMID: 28132910
Quadri et al (2019) Macroscopic and microscopic activation of a7 nicotinic acetylcholine receptors by the structurally unrelated allosteric agonist-positive allosteric modulators (ago-PAMs) B-973B and GAT107. Mol.Pharmacol. 95 43 PMID: 30348894
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Literature in this Area
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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.