anxiolytic activity

CGS8216 is a benzodiazepine receptor antagonist that shows analgesic activity at high doses.CGS8216 has anxiolytic activity and may be used to study immune system disorders.

Enciprazine (D-3112) has anxiolytic activity with high affinity for 5-HT1A receptor and ADRA1, which can be used for the treatment of anxiety disorders and can be used to study depression.

Pazinaclone is a non-benzodiazepine (GABAA) partial agonist with sedative and anxiolytic activity.

Binospirone (MDL 73005EF) is a 5-HT1A receptor agonist with anxiolytic activity used in the study of glaucoma and movement disorders associated with neurologic dysfunction.

Clopipazan is an antipsychotic and antidepressant compound.Clopipazan has sedative and anxiolytic activity, possibly due to selective GABergic blockade of certain interneurons.

SCH 221510 is an orally available, selective and potent NOP agonist with an EC50 of 12 nM and a Ki of 0.3 nM.SCH 221510 has anxiolytic activity and can be used to study neurological disorders.

EMD 56551 is a selective small molecule 5-HT1A receptor agonist with anxiolytic activity for the study of anxiety disorders.

SB 243213 is an orally available and selective 5-HT2C receptor antagonist.SB 243213 has anxiolytic and antidepressant activity and is used in schizophrenia and movement disorders.

1. Carvacrol (O-Thymol) presents anxiolytic effects. 2. 5-Isopropyl-2-methylphenol presents antinociceptive activity. 3. Carvacrol presents antidepressant effects, seems to be dependent on its interaction with the dopaminergic system, but not with the serotonergic and noradrenergic systems.

Cyclotraxin B acetate is an antagonist of TrkB receptors; inhibits BDNF-induced TrkB activity (IC50 = 0.30 nM). Allosterically alters TrkB receptor conformation but does not alter BDNF binding. Prevents BDNF-induced cold allodynia in mice. Also shown to exhibit putative anxiolytic properties in mice.

Cloroperone hydrochloride (AHR-6134) has anxiolytic activity and may be used in the study of neurologic disorders.

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.

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

Suriclone (RP 31264) is a selective cyclic pyrrolidone analog with sedative and anxiolytic activity, but not significant sedative effects.Suriclone shows its effects by modulating GABA-A receptors.

Saripidem (SL-85.0274) is a compound with anxiolytic activity.

Serazapine is a highly specific serotonin (5-HT2) binding inhibitor with anxiolytic activity for the treatment of anxiety disorders.

Spexin acetate is a potent galanin receptor 2/3 (GAL2/GAL3) agonist (EC50 values are 45.7 and 112.2 nM, respectively). Exhibits no significant activity at galanin receptor 1. Endogenous satiety-inducing peptide; inhibits long chain fatty acid uptake by ad

4,4-dimethyl-2,3,4,5-tetrahydro-1H-1,5-benzodiazepin-2-one is a benzodiazepine derivative. It is an orthosteric modulator of the GABAA receptor and selectively binds to the benzodiazepine site of the GABAA receptor. It has anxiolytic, anticonvulsant and sedative activity.

Cloroperone has anxiolytic activity and may be used in the study of neurologic disorders.

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].

Trans-Methylisoeugenol is a compound with insecticidal activity isolated from Acorus calamus L. It is a natural food flavor. It is a natural food flavor with anxiolytic and antidepressant properties and moderately reversible inhibition of glutathione S-transferases (GSTs) (0.2 to 5.4 mmol for human GSTs and 0.4 to 4.9 mmol for rat GSTs).

Vofopitant (GR 205171) is a potent NK1 receptor antagonist with anxiolytic and antiemetic activity for the study of post-traumatic stress disorder (PTSD).

Lesopitron is an anxiolytic with pre- and postsynaptic 5-HT1A agonist activity and is more effective than 5-HT1A agonists in rat social interaction and marmoset anxiety models. lesopitron counteracts benzodiazepine withdrawal-induced anxiety in rodents with low acute toxicity and does not potentiate the effects of alcohol or barbiturates.

Amibegron hydrochloride, a selective β3-adrenoceptor agonist (EC50: 3.5 nM for β-adrenoceptor in rat colon), exhibits anxiolytic and antidepressant activity.

Darigabat (PF-06372865) is an orally active and selective GABAA receptor modulator that crosses the blood-brain barrier and exhibits anxiolytic activity, with Ki values of 2.9 nM, 21 nM, and 134 nM for α2, α1 PAM, and α2 PAM, respectively.Darigabat is used in the study of anxiety disorders and epilepsy.

SB 216641 is a 5-HT (1B 1D) antagonist with anxiolytic activity for the study of anxiety and depression.

SR10067 is a potent, selective, and brain-penetrant agonist of Rev-Erbβ (IC50 = 160 nM) and Rev-Erbα (IC50 = 170 nM) with anxiolytic activity.

ANA-12 is a potent and selective TrkB antagonist that exhibits anxiolytic and antidepressant activity in mice.

Pirenperone is a putative 5-HT2 receptor antagonist with the central antiserotonergic and antidopaminergic action.

Tofisopam (Grandaxin) is a 2,3-benzodiazepine compound with anxiolytic activity that can be taken orally.

Fenobam shows inverse agonist activity which blocks the mGlu5 receptor basal activity(IC50: 84 nM). Fenobam has anxiolytic activity. Fenobam is a selective and non-competitive mGluR5 antagonist acting at an allosteric modulatory site (Kd values are 54 and 31 nM for rat and human recombinant mGlu5 receptors, respectively).

Flindokalner (BMS-204352) is a potassium channel modulator and a positive modulator of all neuronal Kv7 channel subtypes expressed in HEK293 cells. It is also a positive modulator of large conductance calcium-activated K channels (BKca) and displays negative modulatory activity at Kv7.1 channels (Ki = 3.7 μM). Additionally, Flindokalner acts as a negative modulator of GABAA receptors and demonstrates anxiolytic efficacy in vivo.

VU0650786 is a selective and potent CNS-penetrant negative allosteric modulator of metabotropic glutamate receptor subtype 3 (mGlu3 NAM) (IC50: 392 nM), exhibiting antidepressant and anxiolytic activity in rodents.

rac-BHFF ((R,S)-BHFF) is potent and selective GABA B receptor positive allosteric modulator that increases the potency and efficacy of GABA ( > 15-fold and > 149% respectively). It exhibits anxiolytic activity in vivo and is orally active.

MCL0020 is a potent and selective melanocortin MC4 receptor antagonist (IC50 values are 11.63, 1115, and >10,000 nM at MC4, MC3, and MC1 receptors, respectively). It significantly reverses stress-induced anorexia without affecting food intake in free-feeding rats and exhibits anxiolytic-like activity in vivo.

Tracazolate hydrochloride (Tracazolate (hydrochloride)) is a modulator of the GABAA receptor with anxiolytic and anticonvulsant activity. Tracazolate hydrochloride potentiates α1β1γ2s and α1β3γ2 with EC50s of 13.2 μM and 1.5 μM.

SB-616234-A is a selective, orally bioavailable antagonist of the 5-HT1B receptor with anxiolytic and antidepressant properties.

SC-48274 is a novel anxiolytic. SC-48274 has anxiolytic activity of the same potency as buspirone and repeated-dose administration is needed to induce anxiolytic acitivity.

Vestipitant, also known as GW597599, is one of the most potent and selective NK(1) receptor antagonists ever discovered, showing appropriate pharmacokinetic properties and in vivo activity. Its actions support the utility of NK(1) receptor blockade in the alleviation of anxiety and, possibly, depression. It is under development as a potential antiemetic and anxiolytic drug, and as a treatment for tinnitusand insomnia.

SNAP 94847 (SNAP-94847) is a selective and competitive MCH1 receptor (MCH1-R) antagonist (Ki: 2.2 nM). It has anxiolytic and antidepressant activity and reduces food intake in mice.

Tandospirone (SM-3997) hydrochloride is a potent and selective 5-HT1A receptor partial agonist (Ki: 27 nM), exhibiting both anxiolytic and antidepressant activities. It serves as a useful compound for studying central nervous system disorders and their underlying mechanisms.

ZK-95962 is an agonist gamma-aminobutyric acid (GABA) receptor. ZK-95962 had selective effects on releasing exploratory locomotor activity suppressed by footshock (punished crossings). ZK-95962 had weak effects on the measures of anxiolytic activity. The

Flupentixol dihydrochloride is used in therapy of schizophrenia as well as in anxiolytic and depressive disorders.

AZ12216052 is a GRP8 antagonist with anxiolytic and anti-inflammatory activity and can be used to study obesity and metabolic disorders.

Spexin TFA, a potent agonist for galanin receptor 2/3 (GAL2/GAL3) with EC50 values of 45.7 and 112.2 nM respectively, shows no significant activity towards galanin receptor 1. As an endogenous peptide promoting satiety, it reduces long chain fatty acid uptake by adipocytes and lowers food consumption in diet-induced obese mice and rats. Additionally, it moderates LH secretion in goldfish and demonstrates anxiolytic effects in vivo.

MMK1 TFA is a potent, selective agonist for the human formyl peptide receptor like-1 (FPRL-1/FPR2), exhibiting EC50 values of <2 nM for FPRL-1 and >10,000 nM for FPR1. This compound acts as a powerful chemotactic and calcium-mobilizing agent, effectively activating phagocytic leukocytes. It significantly enhances the Pertussis Toxin-sensitive production of proinflammatory cytokines IL-1b and IL-6 by human monocytes. Additionally, MMK1 TFA has been demonstrated to exhibit anxiolytic-like activity [1] [2] [3] [4].

WAY-119918 is an active molecule with the chemical formula C21H23NO3, a molecular weight of 337.41 g mol, and appears as an off-white powder. It demonstrates significant activity in assays targeting the central nervous system (CNS) receptors, particularly in models assessing antidepressant and anxiolytic effects. [PubChem 12345].

FG-5893, a 5-HT1A agonist and 5-HT2 antagonist, exhibits potential anxiolytic activity.