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CAS No.: 78538-74-6

FG 7142 Catalog No. CSN27585

Synonyms: ZK 39106;LSU-65

FG 7142 (ZK 39106; LSU-65), a non-selectively benzodiazepine inverse agonist, has high affinity for the α1 subunit-containing GABAA receptor (Ki=91 nM). FG 7142 (ZK 39106; LSU-65) also modulates GABA-induced chloride flux at GABAA receptors expressing the α1 subunit (EC50= 137 nM). FG 7142 (ZK 39106; LSU-65) can increase tyrosine hydroxylation and cause upregulation of β-adrenoceptors in mouse cerebral cortex .

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技术信息

生物活性

描述FG 7142, a non-selectively benzodiazepine inverse agonist, has high affinity for the α1 subunit-containing GABAA receptor (Ki=91 nM). FG 7142 also modulates GABA-induced chloride flux at GABAA receptors expressing the α1 subunit (EC50= 137 nM). FG 7142 can increase tyrosine hydroxylation and cause upregulation of β-adrenoceptors in mouse cerebral cortex. FG-7142 has affinity for those expressing the α subunit, the Ki values are 91 nM; 330 nM; 492 nM and 2.150 μM for α1, α2, α3 and α5 subunits, respectively. FG-7142 (intraperitoneal injection; 15-30 mg/kg) activates mesolimbocortical dopaminergic projections, leading to increases in dopamine in the prefrontal cortex and the nucleus accumbens in rats. FG-7142 (intraperitoneal injection; 15 mg/kg) increases tyrosine hydroxylase activity and dopamine turnover in the medial prefrontal cortex and ventral tegmentum in vivo, but effects are not detected in mesolimbic or nigrostriatal areas^[2]. FG-7142 (7.5 mg/kg) increased l-tryptophan, serotonin, and 5-hydroxyindoleacetic acid concentrations in the prelimbic cortex but not in several other regions studied including subdivisions of the amygdala and bed nucleus of the stria terminalis^[3]. FG 7142 (25 mg/kg, i.p.) caused a time-dependent increase in dopamine release in prefrontal cortex which was statistically significantly greater than the response to vehicle administration. The anxiogenic benzodiazepine inverse agonist FG 7142 can selectively increase dopamine release in prefrontal cortex^[4].
参考文献

[1] Cottone P, et al. 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.Neuropsychopharmacology. 2007 May;32(5):1069-81. Epub 2006 Nov 1.
[2] Cottone P, Sabino V, Steardo L, Zorrilla EP. 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. Neuropsychopharmacology. 2007 May;32(5):1069-81
[3] Evans AK, Abrams JK, Bouwknecht JA, Knight DM, Shekhar A, Lowry CA. The anxiogenic drug FG-7142 increases serotonin metabolism in the rat medial prefrontal cortex. Pharmacol Biochem Behav. 2006 Jun;84(2):266-74
[4] Bradberry CW, Lory JD, Roth RH. The anxiogenic beta-carboline FG 7142 selectively increases dopamine release in rat prefrontal cortex as measured by microdialysis. J Neurochem. 1991 Mar;56(3):748-52

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 4.4396 mL
- 22.1980 mL
- 44.3959 mL
- 5 mM
- 0.8879 mL
- 4.4396 mL
- 8.8792 mL
- 10 mM
- 0.4440 mL
- 2.2198 mL
- 4.4396 mL

技术信息

CAS号	78538-74-6	储存条件	粉末 Sealed in dry,Room Temperature 液体 -20°C:3-6 月 -80°C:12月
分子式	C13H11N3O	运输	蓝冰
分子量	225.25	别名	ZK 39106;LSU-65

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