Br-PBTC

Br-PBTC is a potent, 2/4 subtype-selective positive allosteric modulator of nAChRs (nicotinic acetylcholine receptors) with α2β2，α2β4，α4β2，α4β4，(α4β2)2α4 and (α4β2)2β2 EC50 ranges from 0.1~0.6 μM. Br-PBTC acts from the c-tail of an α subunit[1].

Signaling Pathways >> Membrane Transporter/Ion Channel >> nAChR

Signaling Pathways >> Neuronal Signaling >> nAChR

Research Areas >> Neurological Disease

nAChRs[1]

Br-PBTC (0.01~10 μM; HEK cells) selectively affects 2 and 4 subunits. Br-PBTC (3 μM; oocytes) has greater effects on nAChRs with 2 subunits over those with 4 subunits. Br-PBTC (0.01~10 μM; 15 minutes; HEK cells) can increase channel activation by a maximal concentration of ACh. Br-PBTC (3 μM; 50 seconds; oocytes) increased ACh activation of α4β2 nAChRs by 385± 61 %. Br-PBTC (3 μM；oocytes) reactivates short term desensitized nAChRs expressed. Br-PBTC (3 μM; 500 seconds; HEK cells) reactivates short term desensitized (α4β2)2α4 and(α4β2)2β2 nAChRs expressed. Br-PBTC (0.1~100 μM；0~140 seconds; HEK cells) reactivates long term desensitized nAChRs[1].

[1]. Wang J, et al. A Novel α2/α4 Subtype-selective Positive Allosteric Modulator of Nicotinic Acetylcholine Receptors Acting from the C-tail of an α Subunit. J Biol Chem. 2015;290(48):28834-28846.