anxiolytic-like

XAP044 is a mGlu7-selective antagonist which inhibits lateral amygdala long term potentiation (LTP) in brain slices from wild type mice with a half-maximal blockade at 88 nm[1].

Rosavin (Rosavidin) has antidepressant and anxiolytic actions, helps balance all the neurotransmitters.

SNAP 398299 is a Glycopeptide Receptor Type 3 (Gal3) antagonist with anxiolytic and antidepressant-like effects and is used in the study of mood disorders.

Epoxylinalool (2-(2-Hydroxy-2-Propyl)-5-Methyl-5-Vinyltetrahydrofuran) is a naturally occurring monoterpene alcohol widely used in the production of perfumes and flavors.

1. Pulegone ((+)-Pulegone) has cytotoxicity followed by regenerative cell proliferation is the MOA for Pulegone-induced urothelial tumors in female rats. 2. Pulegone induces a verapamil-sensitive psychostimulant effect that appears to independ on the opening of L-type calcium channels. 3. Pulegone has negative reinforcing properties and seems to possess anxiolytic-like actions unrelated to the benzodiazepine site of the γ-aminobutyric acid type A (GABAA) receptor.

ALPHA-PINENE ((-)-Alpha-Pinene) is a bicyclic monoterpene found in pine trees and other plants, including Cannabis with diverse biological activities [1]. It reduces the growth of a panel of seven Gram-positive bacteria, seven Gram-negative bacteria, and eight yeast strains with MIC values of 0.75-1.29, 1.05-1.59, and 0.7-1.17%, respectively [2]. It has insecticidal activity against C. molestus larvae with LC50 values ranging from 47 to 49 mg/L.3 ALPHA-PINENE (100 μg/ml) induces apoptosis, increases anion superoxide production and DNA fragmentation, and activates caspase-3 in B16/F10 melanoma cells [4]. In a B16/F10 mouse xenograft model, ALPHA-PINENE(100 ml of a 10 mg/ml solution) reduces the number of metastatic lung nodules by approximately 7-fold. ALPHA-PINENE(8.6 mg/L, aerosol) also increases the time spent in the open arms of the elevated plus maze by approximately 2-fold in mice, indicating anxiolytic-like activity [5].

Zapotin is a natural polyhydroxylated flavonoid that inhibits K562 cells, E. coli, and HIV-1 RT RNase H, exhibiting antioxidant, antiviral, antibacterial, anticonvulsant, anticancer, anxiolytic, antifungal, and antidepressant-like activities.

TPA-023B is an orally active and high-affinity agonist of the GABAA receptor α2/α3 subtype (Kis: 0.73 nM/2 nM) partial and an antagonist α1 subtype (Ki: 1.8 nM), has non-sedating anxiolytic-like properties.

Osanetant produces anxiolytic- and antidepressant-like effects. Osanetant is a selective NK3 receptor antagonist. It is researched for schizophrenia.

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

TRIM (1-(2-Trifluoromethylphenyl)imidazole) is an inhibitor of nNOS.

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.

Tracazolate (ICI 136,753) is a non-benzodiazepine compound that falls under the category of pyrazolo[1,6-a]pyridines and has demonstrated anxiolytic-like effects in animal models.

Dexmecamylamine ((+)-Mecamylamine) acts as an antagonist of nicotinic acetylcholine receptors (nAChR), effectively inhibiting α3β4, α4β2, α7, and α1β1γδ receptors, with an IC50 in the micromolar range. It also exhibits anxiolytic and antidepressant-like effects.

5-HT6R antagonist 3 (compound 15) is an effective and selective 5-HT6R antagonist capable of crossing the blood-brain barrier. It exhibits Ki values of 14 nM for 5-HT6, 3533 nM for 5-HT1A, 35 nM for 5-HT2A, and 1449 nM for 5-HT7. This compound demonstrates anxiolytic-like effects and possesses neuroprotective and cognitive-enhancing properties, indicating potential for Alzheimer's disease research.

MM 77 dihydrochloride is an effecitve 5-HT1A receptor postsynaptic antagonist with anxiolytic-like activity.

VU 0285683 is a specific negative allosteric modulator of mGluR5 with a high affinity for the MPEP binding site. VU 0285683 shows anxiolytic-like activity.

KRM-II-81 is a γ‑Aminobutyric Acid Type A (GABAA) Receptor Ligand. KRM-II-81 exhibits improved anxiolytic-like effects in a mouse marble burying assay and a rat Vogel conflict test.

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].

5α-Androst-16-en-3α-ol is a steroid pheromone that has been found in boar testes and human male axillary sweat and has diverse biological activities.1,2It enhances GABA-activated currents in primary mouse cerebellar granule cells (EC50= 0.4 μM).25α-Androst-16-en-3α-ol (0.1-1 μM) increases the amplitude of GABA-activated currents in HEK293 cells expressing human α1β2γ2and α2β2γ2subunit-containing GABAAreceptors.In vivo, 5α-androst-16-en-3α-ol (5-10 mg/kg) decreases immobility time in the forced swim test in mice. It increases time spent in the open arms of the elevated plus maze in mice, indicating anxiolytic-like activity, when administered at doses ranging from 30 to 50 mg/kg. 5α-Androst-16-en-3α-ol protects against seizures induced by pentylenetetrazole or electroshock in mice (ED50s = 48.9 and 21.9 mg/kg, respectively). 1.Brooksbank, B.W., Brown, R., and Gustafsson, J.A.The detection of 5α-androst-16-en-3α-ol in human male axillary sweatExperientia30(8)864-865(1974) 2.Kaminski, R.M., Marini, H., Ortinski, P.I., et al.The pheromone androstenol (5α-androst-16-en-3α-ol) is a neurosteroid positive modulator of GABAA receptorsJ. Pharmacol. Exp. Ther.317(2)694-703(2006)

TRPC4/5 channel blocker (IC50 values are 3.7-10.3 and 8.2 μM, respectively). Also weakly blocks TRPC3 channels. Exhibits rapid antidepressant and anxiolytic effects in vivo. Zhu et al (2015) Identification and optimization of 2-aminobenzimidazole derivatives as novel inhibitors of TRPC4 and TRPC5 channels. Br.J.Pharmacol. 172 3495 PMID:25816897 |Yang et al (2015) Acute treatment with a novel TRPC4/C5 channel inhibitor produces antidepressant and anxiolytic-like effects in mice. PLoS One 10 e0136255 PMID:26317356

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.

Posovolone (Co 134444), an orally active neuroactive steroid with sedative-hypnotic properties, exhibits anticonvulsant and anxiolytic-like activities, alongside ataxic effects.

Neophytadiene is a diterpene compound extracted from Turbinaria ornate, with anti-inflammatory, antidepressant, anxiolytic-like, anticonvulsant, antioxidant, and cardioprotective effects. It inhibits LPS-induced inflammation in RAW 264.7 macrophages and Sprague-Dawley rats and can be used in neurological disease research.