cis-Dosulepin is a stereoisomer of Dothiepin (trade name Prothiaden, Dothep, Thaden, and Dopress; Dosulepin (INN, BAN) a tricyclic antidepressant that is used in several European and South Asian countries, as well as Australia, South Africa, and New Zealand. Dosulepin is used for the treatment of the major depressive disorder and neuropathic pain. Dosulepin is only Therapeutic Goods Administration and Medicines and Healthcare products Regulatory Agency approved for the treatment of the major depressive disorder. Dothiepin is not used in the United States. The central action of cis-dosulepin was compared with that of its antidepressant stereoisomer trans-dosulepin, cis-dosulepin exerted weaker anti-reserpine, anti-tetrabenazine, and 3H-5-HT (serotonin) uptake inhibiting actions than trans-dosulepin, but cis-dosulepin's inhibition of 3H-dopamine and 3H-norepinephrine uptake was slightly more potent than that of trans-dosulepin. On the other hand, cis-dosulepin exhibited extremely potent anticholinergic action in oxotremorine induced tremor, isolated ileum and the 3H-quinuclidinyl benzilate binding test. It also showed potent apomorphine enhancing the action and shortened the period of immobility in the forced swimming test in animals.

Abecarnil (isopropyl 6-benzyloxy-4-methoxymethyl-beta-carboline-3-carboxylate) is a nonselective mixed full agonist/partial agonist at GABA(A) receptor subtypes. Abecarnil possesses anxiolytic and anticonvulsant properties. Abecarnil has been studied in the treatment of anxiety disorders however its development has been discontinued.

Spiperone (Spiroperidol; brand name: Spiropitan (JP)) is a typical antipsychotic and research chemical belonging to the butyrophenone chemical class. Spiperone is selective D2 dopamine receptor antagonist; α1B-adrenoceptor antagonist; mixed 5-HT2A/5-HT1 serotonin receptor antagonist. Additionally, spiperone was identified by compound screening to be an activator of Ca2+ activated Cl− channels (CaCCs), thus a potential target for therapy of cystic fibrosis. Spiperone is widely used as a pharmacological tool for studying neurotransmitter receptors.

Zomebazam is is a pyrazolodiazepinone derivative drug. It is anxiolytic, nootropic drug. Zomebazam is the mother compound of razobazam. It is structurally related to zometapine.

Flutazolam is a benzodiazepine derivative developed in Japan by Mitsui. The drug is marketed under the name Coreminal and used for the treatment of gastrointestinal disorders. The mechanism of flutazolam action is due to activation of GABA-A receptors as it has affinity to the benzodiazepine binding sites.

Flutoprazepam is a benzodiazepine derivative that reduce anxiety, stress, depression, fatigability and sleep disorders in patients with neurosis and psychosomatic disorders by binding to GABA-A receptor and modulating its activity.

Loprazolam is a hypnotic drug which stimulates GABA-A receptors. Due to its hypnotic activity the drug is used to treat short-term sleep disordes.

Anxiolytic drug, Gedocarnil [SH 530, ZK 113315], was undergoing phase I clinical trials with Schering AG in Germany as a potential nootropic agent. However it`s development for the treatment of cognition disorders was discontinued.

Perospirone (Lullan®) is an atypical antipsychotic of the azapirone family. It is used in Japan for the treatment of schizophrenia and acute cases of bipolar mania. Its primary mode of action is through antagonism of serotonin 5-HT2A and dopamine D2 receptors.

Avizafone is a water-soluble peptide prodrug of diazepam that is hydrolyzed by an aminopeptidase to liberate lysine and diazepam Avizafone was developed by the French military to terminate seizures caused by battlefield nerve agents. Diazepam has a faster entry to the general circulation and achieved higher maximum concentration after injection of prodrug than after the parent drug and this is extremely valuable in nerve agents poisoning conditions.