Jackson H C, Nutt D J
Reckitt & Colman Psychopharmacology Unit, Department of Pharmacology, School of Medical Sciences, Bristol, U.K.
Eur J Pharmacol. 1991 Nov 26;205(2):213-6. doi: 10.1016/0014-2999(91)90823-9.
The effect of benzodiazepine and beta-carboline inverse agonists on body temperature in mice was investigated using doses shown to be pro-convulsant in other studies. The benzodiazepine partial inverse agonists Ro 15-3505 (0.1-30 mg/kg i.p.), Ro 15-4513 (0.1-10 mg/kg i.p.) and the fuller benzodiazepine inverse agonist Ro 19-4603 (0.03-0.3 mg/kg i.p.) had no effect on rectal temperature. Ro 19-4603 (1 mg/kg i.p.) produced a small hypothermic response. In contrast, the beta-carboline partial and full inverse agonists, FG 7142 (30, 60 mg/kg i.p.) and methyl-6,7-dimethoxy-4-ethyl-beta-carboline-3-carboxylate (3, 10 mg/kg i.p.), produced large decreases in body temperature. These differential effects of benzodiazepine and beta-carboline inverse agonists on body temperature may provide further evidence for the existence of benzodiazepine receptor subtypes.
使用在其他研究中显示具有促惊厥作用的剂量,研究了苯二氮䓬类和β-咔啉反向激动剂对小鼠体温的影响。苯二氮䓬类部分反向激动剂Ro 15-3505(腹腔注射0.1 - 30毫克/千克)、Ro 15-4513(腹腔注射0.1 - 10毫克/千克)和更完全的苯二氮䓬类反向激动剂Ro 19-4603(腹腔注射0.03 - 0.3毫克/千克)对直肠温度没有影响。Ro 19-4603(腹腔注射1毫克/千克)产生了轻微的体温过低反应。相比之下,β-咔啉部分和完全反向激动剂FG 7142(腹腔注射30、60毫克/千克)和甲基-6,7-二甲氧基-4-乙基-β-咔啉-3-羧酸盐(腹腔注射3、10毫克/千克)使体温大幅下降。苯二氮䓬类和β-咔啉反向激动剂对体温的这些差异效应可能为苯二氮䓬受体亚型的存在提供进一步证据。