Binding of optically pure (−)-[3H]nicotine to rat brain membranes

AbstractWith the recent availability of (−)-[3H]nicotine of high specific activity, binding studies were performed on rat brain membranes in the presence of a variety of nicotine analogues and cholinergic drugs. Both a higher affinity (Kd = 2 × 10−10 M) and a lower affinity (2 × 10−9 M) site were observed; the stereoselectivity of both sites being similar. A good correlation was observed between IC50-values and psychotropic potency of a series of N′-alkyl substituted nicotine analogues