anxiogenic

Phenibut (Aminophenylbutyric acid) 是GABA-B 激动剂，可作为 GABA 类似物，主要作用于 GABAB 受体，具有抗焦虑和增强认知的作用。

Phenibut hydrochloride (3-Amino-4-phenylbutyric acid hydrochloride) 是 GABA-B 激动剂，口服有活性，可作用于 GABAB 受体，充当 GABA 类似物。它具有促智 (增强认知) 及抗焦虑的能力。

D-AP7 is a specific NMDA antagonist. D-AP7 enhances motility, exhibits anxiogenic-like effect and impairs consolidation in passive avoidance.

KT109 is a selective inhibitor of DAGLβ (IC50 = 42 nM). KT109-treated wild-type mice displayed reductions in LPS-induced allodyni as well as in DAGL-β (- -) micea. Repeated KT109 administration prevented the expression of LPS-induced allodynia, without ev

LY 293284 is a potent, selective full agonist of 5-HT1A receptor with anxiogenic effects in animal studies.

Eltoprazine(DU28853) is a serenic or antiaggressive agent which as an agonist at the 5-HT1A and 5-HT1B receptors and as an antagonist at the 5-HT2C receptor.IC50 value:Target: 5-HT1A 1B agonist; 5-HT2C antagonistin vitro: The binding of [3H]eltoprazine to whole tissue sections was saturable and revealed an apparent dissociation constant (Kd) of 11 nM. Specific [3H]eltoprazine binding was completely displaced by 5-HT; conversely, unlabelled eltoprazine reduced [3H]5-HT binding to the levels of non-specific binding [1]. Eltoprazine evoked membrane changes that were similar to but much weaker than those induced by 5HT. Both the 5HT- and eltoprazine-evoked membrane hyperpolarizations were largely suppressed in the presence of spiperone [2].in vivo: eltoprazine is extremely effective in suppressing dyskinesia in experimental models, although this effect was accompanied by a partial worsening of the therapeutic effect of l-dopa. Interestingly, eltoprazine was found to (synergistically) potentiate the antidyskinetic effect of amantadine. The current data indicated that eltoprazine is highly effective in counteracting dyskinesia in preclinical models [3]. Rats were chronically treated with mianserin (10 mg kg i.p.) or eltoprazine (1 mg kg i.p.) and were tested in the elevated plus-maze test for anxiety. Mianserin and eltoprazine displayed opposite effects in the elevated plus-maze: mianserin induced anxiolytic-like effects, while eltoprazine showed anxiogenic-like ones [4]. [1]. Sijbesma H, et al. Eltoprazine, a drug which reduces aggressive behaviour, binds selectively to 5-HT1 receptor sites in the rat brain: an autoradiographic study. Eur J Pharmacol. 1990 Feb 20;177(1-2):55-66. [2]. Joels M, et al. Eltoprazine suppresses hyperpolarizing responses to serotonin in rat hippocampus. J Pharmacol Exp Ther. 1990 Apr;253(1):284-9. [3]. Bezard E, et al. Study of the antidyskinetic effect of eltoprazine in animal models of levodopa-induced dyskinesia. Mov Disord. 2013 Jul;28(8):1088-96. [4]. Rocha B, et al. Chronic mianserin or eltoprazine treatment in rats: effects on the elevated plus-maze test and on limbic 5-HT2C receptor levels. Eur J Pharmacol. 1994 Sep 1;262(1-2):125-31.

BIBP 3226 trifluoroacetate is a mixed non-peptide neuropeptide Y Y1(NPY Y1) and neuropeptide FF (NPFF) receptor antagonist (Kivalues are 1.1, 79, 108, > 1000, > 1000 and >1000 for rNPY Y1, hNPFF2, rNPFF, rNPY Y2, rNPY Y4and rNPY Y5respectively). Produces an anxiogenic-like effect in rats following i.c.v. administration.

[DPro5] Corticotropin Releasing Factor, human, rat 是人类和大鼠促肾上腺皮质激素释放因子 激素 R2 的选择性激动剂。作为一种下丘脑激素，促肾上腺皮质激素释放因子 (CRF) 能够促进肾上腺皮质激素 (ACTH) 和 β-内啡肽的分泌。值得注意的是，[DPro5] Corticotropin Releasing Factor, human, rat 并不触发典型的焦虑反应，而是能调控大鼠的学习与记忆过程。

FKBP51F67V-selective antagonist Ligand2（示例3-3）是针对杏仁核中由FKBP51 F67V过表达引起的焦虑表型的有效逆转剂。本物质特异性地结合到FKBP51 F67V，与野生型FKBP51及FKBP52无亲和力。