Chweh A Y, Swinyard E A, Wolf H H
Can J Physiol Pharmacol. 1984 Jan;62(1):132-5. doi: 10.1139/y84-021.
The potencies of seven benzodiazepines (BDZs) were established by three tests: inhibition of [3H]flunitrazepam receptor binding, inhibition of [3H]adenosine uptake, and prevention of pentylenetetrazol-induced seizures in mice. There is a high correlation between the potency for inhibition of [3H]flunitrazepam receptor binding and the antipentylenetetrazol potencies of benzodiazepines (r = 0.941; p less than 0.01). The antipentylenetetrazol potencies of benzodiazepines correlate well with their ability to inhibit [3H]adenosine uptake (r = 0.860; p less than 0.05 and greater than 0.01). However, there is no significant correlation between the potency for the inhibition of [3H]flunitrazepam receptor binding and the potency for inhibition of [3H]adenosine uptake (r = 0.751; p greater than 0.05). In addition, there is a marked difference in BDZ potency as measured by these two tests in vitro. The ratios of the Ki values (Ki2/Ki1) range from 98 for BDZ I to 64615 for clonazepam. The data presented indicate that antipentylenetetrazol activity of benzodiazepines results from an interaction between BDZ and nanomolar affinity BDZ receptors.
通过三项试验确定了七种苯二氮䓬类药物（BDZs）的效价：抑制[³H]氟硝西泮受体结合、抑制[³H]腺苷摄取以及预防小鼠戊四氮诱发的惊厥。苯二氮䓬类药物抑制[³H]氟硝西泮受体结合的效价与其抗戊四氮效价之间存在高度相关性（r = 0.941；p < 0.01）。苯二氮䓬类药物的抗戊四氮效价与其抑制[³H]腺苷摄取的能力密切相关（r = 0.860；p < 0.05且> 0.01）。然而，抑制[³H]氟硝西泮受体结合的效价与抑制[³H]腺苷摄取的效价之间无显著相关性（r = 0.751；p > 0.05）。此外，通过这两项体外试验测定的BDZ效价存在显著差异。Ki值的比值（Ki2/Ki1）范围从BDZ I的98到氯硝西泮的64615。所呈现的数据表明，苯二氮䓬类药物的抗戊四氮活性源于BDZ与纳摩尔亲和力BDZ受体之间的相互作用。
