Tofisopam (marketed under brand names Emandaxin and Grandaxin) is a 2,3-benzodiazepine derivative that is marketed in several European countries as the anxiolytic drug. Tofisopam does not bind to the benzodiazepine binding site of the gamma-aminobutyric acid receptor. One study has shown that tofisopam acts as an isoenzyme-selective inhibitor of phosphodiesterases (PDEs) with the highest affinity to PDE-4A1 followed by PDE-10A1, PDE-3, and PDE-2A3. Like other benzodiazepines, tofisopam possesses anxiolytic properties but unlike other benzodiazepines, it does not have anticonvulsant, sedative, skeletal muscle relaxant, motor skill-impairing or amnestic properties. While it may not be an anticonvulsant in and of itself, it has been shown to enhance the anticonvulsant action of classical 1,4-benzodiazepines such as diazepam (but not sodium valproate, carbamazepine, phenobarbital, or phenytoin). Tofisopam is not approved for sale in the United States or Canada. However, Vela Pharmaceuticals of New Jersey is developing the D-enantiomer (dextofisopam) as a treatment for irritable bowel syndrome, with moderate efficacy demonstrated in clinical trials so far.

Camazepam is a benzodiazepine psychoactive drug, marketed under the brand names Albego, Limpidon and Paxor. It is the dimethyl carbamate ester of temazepam, a metabolite of diazepam. While it possesses anxiolytic, anticonvulsant, skeletal muscle relaxant and hypnotic properties it differs from other benzodiazepines in that its anxiolytic properties are particularly prominent but has comparatively limited anticonvulsant, hypnotic and skeletal muscle relaxant properties. Changes in sleep with camazepam were minimal. However, non-anxious subjects reported being more relaxed the next day. Camazepam may cause skin disorders.

Ethyl loflazepate (Lof) has been used widely as a sedative and anxiolytic agent for nearly 20 years. Ethyl loflazepate was designed to be a prodrug for descarboxyloflazepate, its active metabolite. It is the active metabolite which is responsible for most of the pharmacological effects rather than ethyl loflazepate. The main metabolites of ethyl loflazepate are descarbethoxyloflazepate, loflazepate and 3-ydroxydescarbethoxyloflazepate which are the benzodiazepine receptor agonists. Ethyl loflazeplate is commercialized in Mexico, under the trade name Victan. It is officially approved for the following conditions Anxiety: Post-trauma anxiety; Anxiety associated with severe neuropathic pain; Generalized anxiety disorder (GAD); Panic attack; Delirium tremens. It possesses anxiolytic, anticonvulsant, sedative and skeletal muscle relaxant properties. Accumulation of the active metabolites of ethyl loflazepate are not affected by those with renal failure or impairment. The symptoms of an overdose of ethyl loflazepate include sleepiness, agitation and ataxia. Hypotonia may also occur in severe cases. These symptoms occur much more frequently and severely in children. High doses of the antidepressant fluvoxamine may potentiate the adverse effects of ethyl loflazepate.

Etizolam is an analogue of benzodiazepine that contains thienotriazolodiazepine group. The drug was developed and approved in Japan and now is used in Japan, Italy and India for the treatment of anxiety disorders. Etizolam exerts its action through activation of GABA A receptors, moreover, the agonistic behavior was shown on isolated neurons. There are several cases when etizolam dependence was reported. In many countries the drug is recognized as a psychoactive substance and its distribution is illegal there.

Fludiazepam is a potent benzodiazepine and 2ʹ-fluoro derivative of diazepam,[3] originally developed by Hoffman-La Roche in the 1960s. Fludiazepam is marketed in Japan and Taiwan under the brand name Erispan. Fludiazepam exerts its pharmacological properties via enhancement of GABAergic inhibition. Fludiazepam has 4 times more binding affinity for benzodiazepine receptors than diazepam. Fludiazepam possesses anxiolytic, anticonvulsant, sedative, hypnotic and skeletal muscle relaxant properties.

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.

Cloxazolam is an agonist of GABA-A receptor that was developed in Japan for the treatment of anxiety-disorders. The drug was marketed in Europe under the names Sepazon, Olcadil, Akton and Lubalix.

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.

Pinazepam, a benzodiazepine derivative, differs from other drugs of its class by the presence of an unsaturated bond, the propargyl group, at the N-1 position. In animals, pinazepam controls anxiety and aggressiveness and exerts anticonvulsant activity. In clinical trials with open or controlled design, pinazepam, compared with diazepam, showed significant and purely anxiolytic action in patients suffering from anxiety with or without somatic manifestations, particularly in gastrointestinal disorders. Even though it is not a specific hypnotic drug, it seems to help patients in whom the physiological course of the sleep is disturbed. Pinazepam is used in the treatment of anxiety and insomnia associated with anxiety.

KETAZOLAM, a benzodiazepine with an additional d-face-fused heterocyclic ring, possesses anxiolytic, anticonvulsant, sedative and skeletal muscle relaxant properties. It is used for the treatment of anxiety and spasticity.