BIIE-0246 is a highly potent, high affinity antagonist selective for the Y2 receptor subtype. BIIE-0246 is a drug used in scientific research, it was one of the first non-peptide Y2-selective antagonists developed, and remains among the most widely used tools for studying this receptor. It has been used to demonstrate a role for the Y2 subtype as a presynaptic autoreceptor limiting further neuropeptide Y release, as well as modulating dopamine and acetylcholine release. Blockade of central neuropeptide Y (NPY) Y2 receptors by BIIE-0246 has being shown to reduce ethanol self-administration in rats.

6-Iodopravadoline (AM-630) is a cannabinoid receptor antagonist under development with the Univerisity of Wisconsin, USA, for potential use in the treatment of Anorexia nervosa. AM-630 is a selective CB2 receptor antagonist that binds to CB1 and CB2 receptors with Ki values of 5.2 μM and 31.2 nM, respectively. AM630 has been shown to display 165-fold selectivity over CB1 receptors and behave as a weak partial/inverse agonist at CB1 receptors. AM-630 acts as an inverse agonist on cloned human CB1 receptors. The efficacy of AM-630 in reducing the anxiety of the spontaneously anxious DBA/2 strain of mice strengthens the potential of the CB(2) receptor as a new target in the treatment of anxiety-related disorders.

8-Hyroxy-2-Dipropylaminotetralin Hydrobromide (8-OH-DPAT) is a chemical predominantly used in research settings. It is widely regarded as the first identified complete agonist of the 5-HT1a receptor, for which it has a Ki = 3.18 nM. 8-OH-DPAT also acts as an agonist of the 5-HT7 receptor, and as a substrate of the Sodium dependent serotonin transporter (SERT). Although it has never progressed to human clinical trials 8-OH-DPAT has been studied in animal models for a number of conditions both for its own potential and as a benchmark for other compounds.

Salidroside (Rhodioloside) is a glucoside which was isolated in 1926 from Salix triandra L. (Salicaceae). It is thought to be one of the compounds responsible for the antidepressant and anxiolytic actions of this plant, along with rosavin. Also was investigated that salidroside may be a promising candidate for the treatment of inflammatory liver injury and promotes skeletal regeneration in cell-autonomous and cell-non-autonomous ways and might be a potential therapy for accelerating fracture healing.

The radioligand N-(2,5-dimethoxybenzyl)-N-(5-fluoro- 2-phenoxyphenyl) acetamide labeled with carbon-11 (abbreviated as [11C]DAA1106) has emerged as a reliable radiotracer for examining neuroinflammation with positron emission tomography (PET) scanning in vivo. DAA-1106 is a selective agonist for the peripheral benzodiazepine receptor (also known as Translocator protein or TSPO). DAA-1106 exerts potent anxiolytic-like properties, in laboratory animals.

BRL-50481 is a selective inhibitor of phosphodiesterase 7 (PDE 7) that has acceptable selectivity for in vitro studies. Studies suggest that BRL-50481 is used to inhibit the activity of hrPDE7A1 which is usually expressed in baculovirus-infected Spodoptera frugiperda in a competitive manner. In osteoblasts, BRL-50481increases mineralization and bALP as a result of PDE7 silencing which upregulates several osteogenic genes. Further studies show that BRL-50481increases apoptosis in CLL cells via a mitochondrial-dependent process, and is associated with increased cAMP accumulation and down-regulation of the antiapoptotic protein survivin. BRL-50481 is a inhibitor of PDE7A.

DL-Tetrahydropalmatine (dl-THP), an active component isolated from Corydalis species (a Chinese herbal medicine). dl-THP has inhibitory effects on liver injury induced by carbon tetrachloride in mice. The drug demonstrated anxiolytic and anti-nociceptive effects in animal models. dl-THP may act through inhibition of amygdaloid dopamine release to inhibit an epileptic attack – it is a very effective anti-epileptogenic and anticonvulsant agent. dl-THP has been found to have antihypertensive effects. It acts through the 5-HT2 and/or D2-receptor antagonism in the hypothalamus to induce hypotension and bradycardia in rats.

L-838,417 is a subtype-selective GABAA modulator, acting as a partial agonist at alpha2, alpha3 and alpha5 subtypes and an antagonist at the alpha1 subtype. L-838,417 displays anxiolytic effects in vivo and is used as a tool compound to study roles of GABAA subunits.

S-14506 was originally identified and developed in France by Scientists at the Institut de Recherches Servier. S-14506 showed potent binding and antagonistic activity against the 5HT1-A receptor. It was found to work synergistically with D2 receptor antagonists and was therefore studied in animal models for depression, psychosis, and anxiety. A tritium labeled version was also studied as a potential 5HT1-A receptor PET imaging agent.

SB-228357 was originally developed by scientists at Smith Kline Beecham (now merged with Glaxo Welcome to form GlaxoSmithKline). SB-228357 was identified as an antagonist of the serotonin receptors 5-HT2a/b/c with the highest affinity exhibited towards the 5-HT2C receptor. SB-228357 was identified for preclinical development as a treatment for depression, anxiety, and cataplexy but has not progressed beyond animal trials.