anxiolytic activity

Tiapride is a selective blocker of D2/3 dopamine receptors in the brain. It is used in the therapy of various psychiatric and neurological disorders containing dyskinesia, negative symptoms of psychosis, alcohol withdrawal syndrome, and aggression and agitation in the elderly.

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.

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

Amibegron hydrochloride is a selective β3-adrenergic receptor (β3AR) agonist that increases energy expenditure and fat oxidation by activating β3ARs in brown adipose tissue; Amibegron hydrochloride is commonly used in research on metabolic disorders. Amibegron hydrochloride exhibits anxiolytic and antidepressant activity.

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

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

Naluzotan(PRX 00023) is a novel and potent 5-HT1A agonist with IC50 and Ki values of approximately 20 nM and 5.1 nM, respectively.Naluzotan is a potent hERG K+ channel blocker with an IC50 value of 3800 nM.Naluzotan exhibits anxiolytic activity and can be used to study depression.

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.

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.

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.

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.

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

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

Opipramol (Ensidon) is a compound with antidepressant activity that attenuates cocaine-seeking behavior in a rat model of self-administration.Opipramol is a sigma (σ) receptor agonist with anxiolytic activity and may be used in the study of neurological disorders.

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

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

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

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.

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

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

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.