Bolger G T, Weissman B A, Lueddens H, Barrett J E, Witkin J, Paul S M, Skolnick P
Brain Res. 1986 Mar 19;368(2):351-6. doi: 10.1016/0006-8993(86)90580-9.
The densities of dihydropyridine calcium antagonist binding sites were examined in brains and cardiac issues of representative species from 4 classes of non-mammalian vertebrates (aves, pigeon; amphibia, frog; reptilia, chameleon; and osteichthyes, trout) previously shown to have low or undetectable levels of 'peripheral-type' binding sites for benzodiazepines. Dihydropyridine binding sites were present in brain and cardiac tissue of these 4 classes of non-mammalian vertebrates. The apparent dissociation constants for [3H]nitrendipine in non-mammalian vertebrates were comparable to those found in mammalian (rat) tissues. The densities of [3H]nitrendipine binding sites in brain and cardiac tissues were highest in the pigeon, with lower densities in tissues from chameleon, frog and trout. The densities of dihydropyridine binding sites in the latter tissues were comparable to those observed in the rat. Thus, dihydropyridine binding sites are phylogenetically diverse yet have similar kinetic characteristics in mammals and non-mammalian vertebrates. Despite the pharmacologic evidence that links dihydropyridine binding sites and peripheral binding sites for benzodiazepines in mammals, the earlier evolutionary appearance of the former sites suggest that even though they may share one or more common effector mechanisms, they are discrete entities.
在4类非哺乳动物脊椎动物(鸟类,鸽子;两栖类,青蛙;爬行类,变色龙;硬骨鱼类,鳟鱼)的大脑和心脏组织中检测了二氢吡啶钙拮抗剂结合位点的密度,这些动物先前已被证明苯二氮䓬类“外周型”结合位点水平较低或无法检测到。这4类非哺乳动物脊椎动物的大脑和心脏组织中存在二氢吡啶结合位点。非哺乳动物脊椎动物中[3H]尼群地平的表观解离常数与在哺乳动物(大鼠)组织中发现的解离常数相当。鸽子大脑和心脏组织中[3H]尼群地平结合位点的密度最高,变色龙、青蛙和鳟鱼组织中的密度较低。后几种组织中二氢吡啶结合位点的密度与在大鼠中观察到的密度相当。因此,二氢吡啶结合位点在系统发育上具有多样性,但在哺乳动物和非哺乳动物脊椎动物中具有相似的动力学特征。尽管有药理学证据表明哺乳动物中二氢吡啶结合位点与苯二氮䓬类外周结合位点有关,但前者位点在进化上更早出现,这表明尽管它们可能共享一种或多种共同的效应机制,但它们是独立的实体。