Eszopiclone is a nonbenzodiazepine hypnotic, pyrrolopyrazine derivative of the cyclopyrrolone class and is indicated for the short-term treatment of insomnia. While Eszopiclone is a hypnotic agent with a chemical structure unrelated to benzodiazepines, barbiturates, or other drugs with known hypnotic properties, it interacts with the gamma-aminobutyric acid-benzodiazepine (GABABZ) receptor complex. Subunit modulation of the GABABZ receptor chloride channel macromolecular complex is hypothesized to be responsible for some of the pharmacological properties of benzodiazepines, which include sedative, anxiolytic, muscle relaxant, and anticonvulsive effects in animal models. Eszopiclone binds selectively to the brain alpha subunit of the GABA A omega-1 receptor. The mechanism of action of Eszopiclone is not completely understood. It is thought that Eszopiclone acts on the benzodiazepine receptors as an agonist and interacts with GABA-receptor complexes. Used for the treatment of insomnia.

Emapunil acts as a selective agonist at the peripheral benzodiazepine receptor (TSPO). At the cellular level, the selective TSPO ligand XBD173 potentiated the amplitude and duration of GABA-mediated inhibitory postsynaptic currents in mouse medial prefrontal cortical neurons, which was prevented by finasteride. In animal and human trials, XBD173 produced rapid anxiolytic and anti-panic effects probably via newly synthesized neurosteroids, without producing sedation or withdrawal symptoms, and may represent a promising target for the development of fast-acting anxiolytics with a more favourable side-effect profile than benzodiazepines.

PK-11195 was first discovered by Pharmuka Laboratories. It was found to be antagonist of the Translocator Protein (TSPO) with potential for development in a number of conditions including cancer models, cardiac ischemia, seizures, depression, and anxiety. PK-11195 has been studied extensively in vitro and in animal models. In phase I clinical trials no anti-inchemic effects were found after drug administration. A tritium [3H] labeled and a C-11 labeled version of PK-11195 are both used diagnostically as PET imaging compounds.

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.

PBR28 or PBR-28, a chemical substance that binds to translocator protein TSPO, also known as Peripheral-type benzodiazepine receptor (PBR). TSPO located within the cells such as macrophages reaches high levels of expression in inflammatory conditions and thus can be a biomarker of neuroinflammation. When radioactivity in the form of carbon-11 is tagged to PBR 28 and is administered, its uptake in the inflammatory body regions can be measured using positron emission tomography (PET). PBR28 now is involved in a clinical trial to evaluate the specificity of its binding in the joints of patients with inflammatory joint disease, like rheumatoid and psoriatic arthritis.

PK-11195 is a selective antagonist of the Translocator Protein (TSPO). The C11 radiolabeled isotope of PK-11195 ([11C]-(R)-PK-11195) has been used effectively for diagnostic PET imaging in a number of CNS conditions where imaging of TSPO is informative (the S- enantiomer is not used). Applicable conditions including Schizophrenia, Multiple Sclerosis, and Traumatic Brain Injuries where it has been particularly useful for detection of increased microglial activation. It has also been investigated as means to monitor the role of Toll-Like Receptor-4 (TLR-4) after cerebral ischemia in mice. It should be noted that the unlabeled PK-11195 had been investigated for a number of potential therapeutic uses but did not progress beyond animal and cell models.

Etifoxine (etafenoxine, StresamⓇ) is a non-benzodiazepine anxiolytic with an anticonvulsant effect. It was developed in the 1960s for anxiety disorders and is currently being studied for its ability to promote peripheral nerve healing and to treat chemotherapy-induced pain. In addition to being mediated by GABA-A2 receptors like benzodiazepines, etifoxine appears to produce anxiolytic effects directly by binding to 2 or 3 subunits of the GABAA receptor complex. It also modulates GABAA receptors indirectly via stimulation of neurosteroid production after etifoxine binds to the 18 kDa translocator protein (TSPO) of the outer mitochondrial membrane in the central and peripheral nervous systems, previously known as the peripheral benzodiazepine receptor (PBR). Therefore, the effects of etifoxine are not completely reversed by the benzodiazepine antagonist flumazenil. Etifoxine is used for various emotional and bodily reactions followed by anxiety. It is contraindicated in situations such as shock, severely impaired liver or kidney function, and severe respiratory failure. The average dosage is 150 mg per day for no more than 12 weeks. The most common adverse effect is drowsiness at the initial stage. It does not usually cause any withdrawal syndromes. In conclusion, etifoxine shows less adverse effects of anterograde amnesia, sedation, impaired psychomotor performance, and withdrawal syndromes than those of benzodiazepines.

Meticrane is a diuretic. Meticrane is used to treat essential hypertension.