anxiety-like

DPN (Diarylpropionitrile) is an selective agonist of estrogen receptor β (ERβ) .

Apigenin (NSC 83244) is an aromatic oil extracted from the flowers or leaves of the daisy-like plants. Extracts, oils and teas made from chamomile are used for its soothing qualities as a sedative, mild analgesic and sleep medication. Apigenin has not been implicated in causing serum enzyme elevations or clinically apparent liver injury.

4-Ethylphenyl Sulfate is an intestinal microbial metabolite that reduces mature oligodendrocytes and myelin formation in the brain, affects PVT gene expression, and promotes anxiety-like behaviour in mice.

Org-12962 is an effective and selective 5-HT2C receptor agonist pEC50: 7.01). Org-12962 shows antiaversive effects in a rat model of panic-like anxiety. Org-12962 also shows high effacy for the 5-HT2A and 5-HT2B receptors (pEC50s: 6.38 and 6.28, respectively).

p-MPPI hydrochloride is a selective 5-HT1A receptor antagonist with antidepressant and anxiolytic-like effects.

Carpipramine (free base) is an atypical antipsychotic compound utilized in France and Japan to treat schizophrenia and anxiety. In addition to its neuroinhibitory and anxiolytic effects, it also possesses hypnotic properties. Structurally, carpipramine resembles tricyclic compounds like imipramine and is related to butyrophenones such as haloperidol.

RA-PR058 is an orally active Ramalin derivative capable of penetrating the blood-brain barrier, with multi-target regulatory functions. By reducing BACE1 expression, decreasing excessive tau protein phosphorylation, and mitigating anxiety-like behaviors, along with displaying favorable pharmacokinetic properties, RA-PR058 shows promise as a multi-target modulator for Alzheimer's disease.

TCS 1105 is a GABAA benzodiazepine receptor (BZR) ligand. TCS 1105 blocks Sema3A induced axonal growth cones collapse. TCS 1105 reduces anxiety-like behavior and enhances offensive behavior and social dominance in mice.

6-Hydroxyflavone (6-HF) is a noncompetitive inhibitors of cytochrome P450 2C9. It is a flavone, a type of chemical compound. It is reported in leaves of Barleria prionitis Linn. (a common Acanthaceae from India). 6-Hydroxyflavone may have a potential as a therapeutic drug capable for the treatment of anxiety-like disorders.

3'-Sialyllactose sodium is a prebiotic with anti-inflammatory activity that maintains immune homeostasis. 3'-Sialyllactose sodium reduces stressor-induced anxiety-like behaviors and can be used in studies of inflammation and arthritis.

SB 242084 hydrochloride is a 5-HT2C receptor antagonist(pKi=9.0) that displays 158- and 100-fold selectivity over 5-HT2A and 5-HT2B receptors respectively.IC50 value: 9.0(pKi) [1]Target: 5-HT2C antagonistin vitro: SB 242084 had over 100-fold selectivity over a range of other 5-HT, dopamine and adrenergic receptors. In studies of 5-HT-stimulated phosphatidylinositol hydrolysis using SH-SY5Y cells stably expressing the cloned human 5-HT2C receptor, SB 242084 acted as an antagonist with a pKb of 9.3, which closely resembled its corresponding receptor binding affinity [1].in vivo: SB 242084 potently inhibited m-chlorophenylpiperazine (mCPP, 7 mgkg i.p. 20 min pre-test)-induced hypolocomotion in rats, a model of in vivo central 5-HT2C receptor function, with an ID50 of 0.11 mg/kg i.p., and 2.0 mg/kg p.o. SB 242084 (0.1-1 mg/kg i.p.) exhibited an anxiolytic-like profile in the rat social interaction test, increasing time spent in social interaction, but having no effect on locomotion. SB 242084 (0.1-1 mg/kg i.p.) also markedly increased punished responding in a rat Geller-Seifter conflict test of anxiety, but had no consistent effect on unpunished responding [1].

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.

MS21570 as a GPR171 antagonist based on its ability to block,with an IC50 of 220 Nm,that reduces anxiety-like behavior and fear conditioning in mice.

Neuropeptide S(Mouse) TFA, an endogenous agonist for the neuropeptide S receptor (NPSR) with an EC50 value of 3 nM, plays a significant role in physiological processes by inducing the mobilization of intracellular Ca2+. This compound elevates locomotor activity and wakefulness, and simultaneously decreases anxiety-like behavior in mice.

Neuropeptide S(Rat) TFA, a robust endogenous agonist for the neuropeptide S receptor (NSPR) with an EC50 of 3.2 nM, enhances locomotor activity and promotes wakefulness while concurrently diminishing anxiety-like behavior in mice.

α-Helical CRF (9-41) is a synthetic peptide antagonist that targets corticotropin-releasing factor (CRF), effectively inhibiting CRF-induced adrenocorticotropic hormone (ACTH) release both in vitro, with isolated rat anterior pituitary cells at concentrations of 0.5 to 5 µM, and in vivo, in non-anesthetized, intact rats at doses ranging from 0.02 to 0.6 µmol/kg. Moreover, it prevents stress-induced ACTH release at a dose of 0.6 µmol/kg in rats and demonstrates the ability to enhance social interaction times in a rat model addressing nicotine-induced conditioned anxiety, in addition to decreasing binge-like ethanol consumption in mice.

Potent endogenous neuropeptide S receptor (NPSR) agonist (EC50 = 3 nM). Induces mobilization of intracellular Ca2+. Increases locomotor activity and wakefulness in mice. Also reduces anxiety-like behavior in mice.

Potent endogenous neuropeptide S receptor (NSPR) agonist (EC50 = 3.2 nM). Increases locomotor activity and wakefulness in mice. Also reduces anxiety-like behavior in mice.

Potent endogenous neuropeptide S receptor agonist (EC50 = 9.4 nM). Increases locomotor activity and wakefulness in mice. Also reduces anxiety-like behavior in mice.

Corticotropin-releasing hormone (CRH) is a peptide hormone involved in the stress response. It is the primary regulatory peptide of the hypothalamic-pituitary-adrenal (HPA) axis under stress conditions. CRH can be utilized for research in neuroendocrine activities and anxiety-like behaviors.

TAT-D1 peptide is a selective D1-D2 heteromer antagonist. It disrupts D1-D2 receptor heterodimers by interacting with specific domains of the D2 receptor through its unique amino acid sequence, especially the two glutamic acid residues at the C-terminus of the D1 receptor. TAT-D1 peptide is used for studying the role of D1-D2 receptor heterodimers in regulating depression and anxiety-like behaviors.