Br-PBTC is a potent, 2/4 subtype-selective positive allosteric modulator ofnAChRs(nicotinic acetylcholine receptors) with α2β2，α2β4，α4β2，α4β4，(α4β2)₂α4 and (α4β2)₂β2EC₅₀ranges from 0.1~0.6 μM. Br-PBTC acts from the c-tail of an α subunit^[1].

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].

339.25

C₁₄H₁₅BrN₂OS

1839519-57-1

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