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苯二氮䓬反向激动剂FG-7142诱导小鼠出现延迟性行为抑郁。

Benzodiazepine inverse agonist FG-7142-induced delayed behavioral depression in mice.

作者信息

Chopra K, Kunchandy J, Kulkarni S K

机构信息

Department of Pharmaceutical Sciences, Panjab University, Chandigarh, India.

出版信息

Arch Int Pharmacodyn Ther. 1988 Jul-Aug;294:56-63.

PMID:2852932
Abstract

Effect of acute administration of a benzodiazepine-inverse agonist, FG-7142, on forced swimming-induced depression was investigated in mice. A single injection of FG-7142 (40 mg/kg) showed a delayed increase in behavioral despair, the peak effect being observed on the 5th and 6th day of FG-7142 administration. beta-Adrenoceptor agonist isoprenaline significantly potentiated FG-7142-induced behavioral despair. FG-7142-induced depression was sensitive to reversal by chronic treatment with propranolol or desipramine. These observations suggest that the inverse agonist FG-7142 upregulates beta-adrenoceptor population leading to behavioral despair in mice.

摘要

研究了苯二氮卓反向激动剂FG - 7142急性给药对小鼠强迫游泳诱导的抑郁的影响。单次注射FG - 7142(40毫克/千克)显示行为绝望延迟增加,在给予FG - 7142的第5天和第6天观察到峰值效应。β-肾上腺素能受体激动剂异丙肾上腺素显著增强了FG - 7142诱导的行为绝望。FG - 7142诱导的抑郁对普萘洛尔或地昔帕明的慢性治疗逆转敏感。这些观察结果表明,反向激动剂FG - 7142上调β-肾上腺素能受体数量,导致小鼠出现行为绝望。

相似文献

1
Benzodiazepine inverse agonist FG-7142-induced delayed behavioral depression in mice.苯二氮䓬反向激动剂FG-7142诱导小鼠出现延迟性行为抑郁。
Arch Int Pharmacodyn Ther. 1988 Jul-Aug;294:56-63.
2
Chronic benzodiazepine administration. VIII. Receptor upregulation produced by chronic exposure to the inverse agonist FG-7142.长期使用苯二氮䓬类药物。VIII. 长期暴露于反向激动剂FG - 7142所产生的受体上调。
J Pharmacol Exp Ther. 1991 Jul 1;258(1):280-5.
3
Are changes in glutamatergic mechanisms responsible for kindling to the benzodiazepine receptor inverse agonist, FG 7142?
Br J Pharmacol. 1989 Dec;98 Suppl:837P.
4
Strain differences in response to a benzodiazepine receptor inverse agonist (FG 7142) in mice.小鼠对苯二氮䓬受体反向激动剂(FG 7142)反应的品系差异。
Psychopharmacology (Berl). 1988;94(3):335-6. doi: 10.1007/BF00174705.
5
Inverse agonist properties of the FG 7142 discriminative stimulus.
Pharmacol Biochem Behav. 1991 Jan;38(1):99-104. doi: 10.1016/0091-3057(91)90595-s.
6
FG 7142 specifically reduces meal size and the rate and regularity of sustained feeding in female rats: evidence that benzodiazepine inverse agonists reduce food palatability.FG 7142 特别降低雌性大鼠的进食量以及持续进食的速率和规律性:有证据表明苯二氮䓬反向激动剂会降低食物的适口性。
Neuropsychopharmacology. 2007 May;32(5):1069-81. doi: 10.1038/sj.npp.1301229. Epub 2006 Nov 1.
7
Effect of baclofen, a GABAB-agonist, on forced swimming-induced immobility in mice.
Arch Int Pharmacodyn Ther. 1990 Sep-Oct;307:18-31.
8
Chronic desipramine treatment prevents the upregulation of cortical beta-receptors caused by a single dose of the benzodiazepine inverse agonist FG7142.慢性地昔帕明治疗可预防由单剂量苯二氮䓬反向激动剂FG7142引起的皮质β受体上调。
Eur J Pharmacol. 1987 Jul 9;139(2):225-32. doi: 10.1016/0014-2999(87)90255-x.
9
A single dose of FG 7142 causes long-term increases in mouse cortical beta-adrenoceptors.单次注射FG 7142可使小鼠皮质β-肾上腺素能受体长期增加。
Eur J Pharmacol. 1987 Feb 24;134(3):313-9. doi: 10.1016/0014-2999(87)90362-1.
10
Pharmacology of the beta-carboline FG-7,142, a partial inverse agonist at the benzodiazepine allosteric site of the GABA A receptor: neurochemical, neurophysiological, and behavioral effects.β-咔啉FG-7142的药理学研究,它是GABAA受体苯二氮䓬变构位点的部分反向激动剂:神经化学、神经生理学及行为学效应
CNS Drug Rev. 2007 Winter;13(4):475-501. doi: 10.1111/j.1527-3458.2007.00025.x.

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Are Noradrenergic Transmission Reducing Drugs Antidepressants?去甲肾上腺素能传递减少药物是抗抑郁药吗?
Front Behav Neurosci. 2021 Sep 30;15:673634. doi: 10.3389/fnbeh.2021.673634. eCollection 2021.
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Effects of a single or repeated administration of the benzodiazepine inverse agonist FG7142 on behaviour and cortical adrenoceptor binding in the rat.苯二氮䓬反向激动剂FG7142单次或重复给药对大鼠行为及皮质肾上腺素能受体结合的影响。
Psychopharmacology (Berl). 1989;98(3):417-24. doi: 10.1007/BF00451698.