Chemical Name: 3,4-Difluoro-N-[(1S)-1-[6-[4-(2-pyridinyl)-1-piperazinyl]-2-pyrazinyl]ethyl]benzenepropanamide
Biological ActivityB 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.
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Tocris products are intended for laboratory research use only, unless stated otherwise.
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
B-973, a novel piperazine positive allosteric modulator of the α7 nicotinic acetylcholine receptor.
Post-Munson et al.
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.
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