Sloan J W, Martin W R, Hernandez J, Hook R
Pharmacol Biochem Behav. 1985 Dec;23(6):987-93. doi: 10.1016/0091-3057(85)90105-4.
Saturation studies employing (-)- and (+)-[3H]nicotine indicate that the isomers bind to different very high and high affinity sites since the binding density for (-)-[3H]nicotine is 10 times that for (+)-[3H]nicotine. Both isomers also bind to a low affinity site (KDS = approximately 10(-5) to 10(-4) M). Competition studies employing unlabelled (-)- and (+)-nicotine reveal greater complexities. The isomers also appear to bind to a separate site which enhances binding at the (-)- and (+)-nicotine high affinity sites. (+)-Nicotine is more effective in increasing the binding of (-)-[3H]nicotine at its high affinity site than (-)-nicotine. Further, (+)-nicotine has a greater specificity for enhancing binding than (-)-nicotine in that it enhances (-)-[3H]nicotine binding at lower concentrations and inhibits binding at higher concentrations than (-)-nicotine.
使用（-）-和（+）-[³H]尼古丁进行的饱和度研究表明，这两种异构体与不同的极高亲和力和高亲和力位点结合，因为（-）-[³H]尼古丁的结合密度是（+）-[³H]尼古丁的10倍。两种异构体也都与一个低亲和力位点结合（解离常数约为10⁻⁵至10⁻⁴ M）。使用未标记的（-）-和（+）-尼古丁进行的竞争研究揭示了更大的复杂性。这些异构体似乎还与一个单独的位点结合，该位点增强了（-）-和（+）-尼古丁高亲和力位点的结合。（+）-尼古丁在增加（-）-[³H]尼古丁在其高亲和力位点的结合方面比（-）-尼古丁更有效。此外，（+）-尼古丁在增强结合方面比（-）-尼古丁具有更高的特异性，因为它在比（-）-尼古丁更低的浓度下增强（-）-[³H]尼古丁的结合，而在更高的浓度下抑制结合。
