Adiphenine (hydrochloride)

Adiphenine hydrochloride is a non-competitive inhibitor of nicotinic acetylcholine receptor (nAChR), with an IC₅₀s of 1.9, 1.8, 3.7, and 6.3 μM for α1, α3β4, α4β2, and α4β4, respectively. Adiphenine hydrochloride has anticonvulsant effects^[1][2][3]. IC50 & Target:IC50: 1.9 µM (α1 nAChR), 1.8 µM (α3β4 nAChR), 3.7 µM (α4β2 nAChR), 6.3 µM (α4β4 nAChR)^[1] In Vitro:Adiphenine (10 nM-1 mM; 3 min) blocks the function of α1*-nAChR in a dose-dependent manner in TE671/RD cells, with an IC₅₀ of 1.9 μM^[1].
Adiphenine (10 nM-1 mM; 3 min) blocks the function of α3α4*-nAChR in a dose-dependent manner in SH-SY5Y cells, with an IC₅₀ of 1.8 μM^[1].
Adiphenine (10 nM-1 mM; 3 min) blocks the function of α4β2- and α4β4-nAChR in a dose-dependent manner in SH-EP1 cells, with IC₅₀s of 3.7 and 6.3 μM, respectively^[1].
Adiphenine (50-200 μM; 30-60 s) decreases the frequency of ACh-induced single-channel currents in HEK 293 cells^[2]. In Vivo:Adiphenine (i.p.) prevents the hindleg tonic-extensor component of maximal electroshock seizures (MES), with an ED₅₀ of 62 mg/kg in mice^[3].