Hill H F, Watanabe Y, Shibuya T
Jpn J Pharmacol. 1984 Sep;36(1):15-21. doi: 10.1254/jjp.36.15.
The postnatal development of 3[H] ethylketocyclazocine (EKC) binding characteristics was examined using membranes from the cerebral cortex of rats at various ages. Binding site affinity did not vary significantly between postnatal days 1 and 90. However, the apparent density of cortical binding sites increased fivefold between birth and adulthood. These results were similar to another ontogenic study of brain opiate receptor binding. Whereas EKC was equally potent as a competitor for 3[H] EKC binding in cortex from neonatal and adult rats, tifluadom was three times more potent in neonatal cortex than in adult cortex as a displacer of specific EKC binding. Brotizolam, a new thienodiazepine and a potent sedative hypnotic, also was distinctly more potent as an inhibitor of 3H-diazepam binding in neonatal rat brain cortex than in adult rat brain cortex. These results suggest that subtypes of benzodiazepine receptors, as well as some opiate receptor subtypes, exhibit different rates of postnatal development.
利用不同年龄段大鼠大脑皮层的膜片，研究了[³H]乙基酮环唑辛（EKC）结合特性的产后发育情况。出生后第1天至第90天之间，结合位点亲和力无显著变化。然而，从出生到成年，皮层结合位点的表观密度增加了五倍。这些结果与另一项关于脑阿片受体结合的个体发育研究相似。虽然EKC作为新生儿和成年大鼠皮层中[³H]EKC结合的竞争剂效力相同，但替氟朵在新生儿皮层中作为特异性EKC结合的置换剂，其效力是成年皮层中的三倍。新型噻吩二氮䓬类强效镇静催眠药布罗替唑仑，作为新生大鼠脑皮层中³H-地西泮结合的抑制剂，其效力也明显高于成年大鼠脑皮层。这些结果表明，苯二氮䓬受体亚型以及一些阿片受体亚型在产后发育过程中表现出不同的速率。
