Kovalev G I, Firstova Iu Iu, Abaimov D A, Starikova N A
Zh Nevrol Psikhiatr Im S S Korsakova. 2012;112(3 Pt 1):39-43.
We conducted a comparative study on the effect of active compounds of pantogam and pantogam active (calcium D(R)-homopantothenate and calcium DL(RS)-homopantothenate) and its L(S)-isomer on the receptors of main brain neuromediators in rats using in vitro radioligand binding analysis. All three compounds interact with binding sites of specific GABA-A and, in particular, GABA-B receptor ligands. Racemate and S-enantiomer, but not its R-form, competed to a moderate degree for D2-receptor binding sites. In all cases, degrees of interaction with receptors were ranged as follows: S-isomer>racemate>R-isomer. These qualitative and quantitative differences are assumed to contribute to pharmacological activity of both drugs.
我们使用体外放射性配体结合分析法，对泛硫乙胺及其活性成分（D（R）-泛解酸钙和DL（RS）-泛解酸钙）的活性化合物及其L（S）-异构体对大鼠主要脑内神经递质受体的作用进行了比较研究。所有这三种化合物均与特异性GABA-A，尤其是GABA-B受体配体的结合位点相互作用。外消旋体和S-对映体，而非其R-形式，对D2受体结合位点有中等程度的竞争。在所有情况下，与受体的相互作用程度如下：S-异构体>外消旋体>R-异构体。这些定性和定量差异被认为有助于两种药物的药理活性。
