Kozlowski M R
Central Research Division, Pfizer Inc., Groton, CT 06340.
Pharmacol Biochem Behav. 1988 May;30(1):73-5. doi: 10.1016/0091-3057(88)90426-1.
The abilities of 4 triazolobenzodiazepines, adinazolam, alprazolam, estazolam and triazolam, to inhibit thyrotropin-releasing hormone (TRH) receptor binding and to antagonize the narcoleptic effects of TRH were examined. The IC50 values for inhibition of 3H-3-methyl-His-2-TRH (MeTRH) binding ranged from 19 microM to 477 microM, and the Hill coefficient from 0.53 to 0.98. Similar ranges of values were obtained from benzodiazepines of other structural classes. Thus, the inhibition of TRH receptor binding by the triazolobenzodiazepines is similar to that produced by other types of benzodiazepines. Furthermore, the triazolobenzodiazepine, alprazolam, antagonized the narcoleptic effect of TRH. However, this action is not necessarily linked to its inhibition of TRH receptor binding since alprazolam also inhibited the narcoleptic effect of amphetamine.
研究了4种三唑并苯二氮䓬类药物，即阿地唑仑、阿普唑仑、艾司唑仑和三唑仑，抑制促甲状腺激素释放激素（TRH）受体结合以及拮抗TRH致发作性睡病作用的能力。抑制3H-3-甲基组氨酸-2-TRH（MeTRH）结合的IC50值范围为19微摩尔至477微摩尔，希尔系数范围为0.53至0.98。从其他结构类别的苯二氮䓬类药物也获得了类似的值范围。因此，三唑并苯二氮䓬类药物对TRH受体结合的抑制作用与其他类型苯二氮䓬类药物产生的抑制作用相似。此外，三唑并苯二氮䓬类药物阿普唑仑拮抗了TRH的发作性睡病作用。然而，这种作用不一定与其对TRH受体结合的抑制有关，因为阿普唑仑也抑制了苯丙胺的发作性睡病作用。
