B 973B

Biological Activity

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.

Technical Data

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.

Background References

1. B-973, a novel α7 nAChR Ago-PAM: racemic and asymmetric synthesis, electrophysiological studies, and in vivo evaluation.
   Garai et al.
   ACS Med.Chem.Lett., 2018;9:1144
2. B-973, a novel piperazine positive allosteric modulator of the α7 nicotinic acetylcholine receptor.
   Post-Munson et al.
   Eur.J.Pharmacol., 2017;15:799
3. Macroscopic and microscopic activation of a7 nicotinic acetylcholine receptors by the structurally unrelated allosteric agonist-positive allosteric modulators (ago-PAMs) B-973B and GAT107.
   Quadri et al.
   Mol.Pharmacol., 2019;95:43

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