Background:

Adiphenine hydrochloride is a nicotinic receptor inhibitor, used as an antispasmodic drug.Target: nAChRAdiphenine hydrochloride decreased the frequency of ACh-induced single-channel currents. adiphenine decreased cluster duration (36-fold at 100 micromolxL(-1)). Adiphenine hydrochloride did not change amplitude but increased the decay rate (IC(50)= 15 micromolxL(-1)) [1]. Adiphenine hydrochloride was administered in3H-labelled form in doses of 15 u.mole/kg intravenously to male Wistar rats. Plasma and brain levels of the unchanged drug were measured [1]. The elimination of the3H -labelled compound from the plasma was monophasic with a half-life of 13 minutes. The unchanged drug was detectable in the plasma for 30 minutes after the injection. The time course of brain levels of unchanged drug paralleled that found in the plasma with a half-life of 9 to 12 minutes. In all experiments, brain and plasma levels of unchanged Adiphenine hydrochloride correlate highly [2].

参考文献:
[1]. 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.
[2]. 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.