| Bioactivity | 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]. |
| Target | IC50: 1.9 µM (α1 nAChR), 1.8 µM (α3β4 nAChR), 3.7 µM (α4β2 nAChR), 6.3 µM (α4β4 nAChR) |
| Invitro | 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]. |
| Name | Adiphenine hydrochloride |
| CAS | 50-42-0 |
| Formula | C20H26ClNO2 |
| Molar Mass | 347.88 |
| Appearance | Solid |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | 4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) |
| Reference | [1]. Gentry CL, et, al. Local anesthetics noncompetitively inhibit function of four distinct nicotinic acetylcholine receptor subtypes. J Pharmacol Exp Ther. 2001 Dec;299(3):1038-48. [2]. Spitzmaul, G., et al., The local anaesthetics proadifen and adiphenine inhibit nicotinic receptors by different molecular mechanisms. Br J Pharmacol, 2009. 157(5): p. 804-17. [3]. TANAKA K, et, al. Anticonvulsant properties of procaine, cocaine, adiphenine and related structures. Proc Soc Exp Biol Med. 1955 Oct;90(1):192-5. [4]. Michelot, J., et al., Adiphenine plasma levels and blood-brain barrier crossing in the rat. Eur J Drug Metab Pharmacokinet, 1985. 10(4): p. 273-8. |
Adiphenine hydrochloride
CAS: 50-42-0 F: C20H26ClNO2 W: 347.88
Adiphenine hydrochloride is a non-competitive inhibitor of nicotinic acetylcholine receptor (nAChR), with an IC50s of 1.
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