B 973B

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Description: Positive allosteric modulator of α7 nAChRs; analgesic
Alternative Names: (-)-(S)-B 973B
Chemical Name: 3,4-Difluoro-N-[(1S)-1-[6-[4-(2-pyridinyl)-1-piperazinyl]-2-pyrazinyl]ethyl]benzenepropanamide
Purity: ≥98% (HPLC)
Literature (2)

Biological Activity for B 973B

B 973B is a 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.

Compound Libraries for B 973B

B 973B is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.

Technical Data for B 973B

M. Wt 452.5
Formula C24H26F2N6O
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 2244989-34-0
PubChem ID 137319851
Smiles C[C@@H](C1=CN=CC(N2CCN(C3=CC=CC=N3)CC2)=N1)NC(CCC4=CC(F)=C(C=C4)F)=O

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 B 973B

Solvent Max Conc. mg/mL Max Conc. mM
DMSO 45.25 100
ethanol 22.62 50

Preparing Stock Solutions for B 973B

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.

Select a batch to recalculate based on the batch molecular weight:
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

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References for B 973B

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

If you know of a relevant reference for B 973B, please let us know.

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Citations for B 973B

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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.

Nicotinic ACh Receptors Scientific Review

Nicotinic ACh Receptors Scientific Review

Updated in 2014, this review by Sue Wonnacott summarizes the diverse structure and function of nicotinic acetylcholine receptors and gives an in-depth review of the ligands available for nAChR research. Compounds available from Tocris are listed.

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