Taylor S C, Little H J, Nutt D J, Sellars N
Neuropharmacology. 1985 Jan;24(1):69-73. doi: 10.1016/0028-3908(85)90097-8.
The effects on body temperature of the benzodiazepine contragonists FG 7142 (N-methyl-beta-carboline-3-carboxamide) and DMCM (methyl-6,7-dimethoxy-4-ethyl-beta-carboline-3-carboxylate), the benzodiazepine antagonist Ro 15-1788 (ethyl-8-fluoro-5,6-dihydro-5-methyl-7-oxo-4H-imidazo-(1,5-a)(1,4)benzod iazepin e -3-carboxylate) and the benzodiazepine agonist, flurazepam, were investigated in mice. Both of the contragonists and flurazepam reduced the body temperature. The antagonist Ro 15-1788 did not alter body temperature alone but significantly antagonised the effects of FG 7142 and of flurazepam. The effects of the latter two drugs on locomotor activity in animals in a familiar environment were also investigated. Flurazepam reduced the activity counts in these circumstances but FG 7142 did not cause a significant change, at doses which considerably reduced body temperature. The drug FG 7142 also reduced the body temperature in rats. The effects on body temperature of the benzodiazepine contragonists and flurazepam were unusual in that they were changes in the same direction, both antagonised by Ro 15-1788. However, they differed in that while the effects of flurazepam on locomotor activity might contribute to its hypothermic effect this did not appear to be the case for FG 7142.
研究了苯二氮䓬类对抗剂FG 7142(N-甲基-β-咔啉-3-甲酰胺)和DMCM(甲基-6,7-二甲氧基-4-乙基-β-咔啉-3-羧酸酯)、苯二氮䓬类拮抗剂Ro 15-1788(乙基-8-氟-5,6-二氢-5-甲基-7-氧代-4H-咪唑并-(1,5-a)(1,4)苯并二氮䓬-3-羧酸酯)以及苯二氮䓬类激动剂氟西泮对小鼠体温的影响。两种对抗剂和氟西泮均降低了体温。拮抗剂Ro 15-1788单独使用时不改变体温,但能显著拮抗FG 7142和氟西泮的作用。还研究了后两种药物对处于熟悉环境中的动物运动活性的影响。在这些情况下,氟西泮降低了活动计数,但在能显著降低体温的剂量下,FG 7142未引起显著变化。药物FG 7142也降低了大鼠的体温。苯二氮䓬类对抗剂和氟西泮对体温的影响不同寻常,因为它们的变化方向相同,且均被Ro 15-1788拮抗。然而,它们的不同之处在于,虽然氟西泮对运动活性的影响可能有助于其降温作用,但FG 7142似乎并非如此。