anxiogenic

Phenibut (Aminophenylbutyric acid) is a central depressant and derivative of the naturally occurring inhibitory neurotransmitter γ-aminobutyric acid (GABA).

FKBP51F67V-selective antagonist Ligand2 (example 3-3), a potent ligand, selectively binds to the FKBP51 F67V variant, with no affinity for wild-type FKBP51 or FKBP52 [1]. It effectively reverses the anxiogenic phenotype resulting from FKBP51 F67V overexpression in the amygdala.

[DPro5] Corticotropin Releasing Factor, human, rat, a selective R2 agonist of corticotropin-releasing factor/hormone (CRF), is a hypothalamic hormone that prompts the release of adrenocorticotropic hormone (ACTH) and β-endorphin. Unlike typical agents, it does not induce anxiogenic effects but instead influences learning and memory processes in rats [1].

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

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.

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

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.

Phenibut hydrochloride (3-Amino-4-phenylbutyric acid hydrochloride) is a GABA mimetic that acts as an agonist at GABAB receptors, blocks α2δ subunit-containing voltage-gated calcium channels, stimulates dopamine receptors, and inhibits the actions of β-phenethylamine