Phenibut (beta-phenyl-gamma-aminobutyric acid or 4-amino-3-phenylbutyric acid) is a neuropsychotropic drug that was discovered and introduced into clinical practice in Russia in the 1960s. It has anxiolytic and nootropic (cognition enhancing) effects. It acts as a GABA-mimetic, primarily at GABA(B) receptors. Pharmacological activity of racemic phenibut relies on R-phenibut and this correlates to the binding affinity of enantiomers of phenibut to the GABAB receptor. In addition R-phenibut binds to the α2-δ subunit of voltage-dependent calcium channels. It is highly effective in treating anxiety, post-traumatic stress disorder, depression, asthenia, insomnia, alcoholism, stuttering, and vestibular disorders. It also improves mental performance (attention, memory, speed and accuracy of sensory-motor reactions), physical performance, reduces sleep disorders as well as movement and speech disorders.

Phenazepam belongs to the 1,4-benzodiazepines, the same family of medicines to which diazepam, oxazepam and temazepam belong. Phenazepam was first synthesized and developed in 1975 in the former Soviet Union where it became one of the most prescribed benzodiazepines since 1978 to treat sleep disorder, anxiety, alcohol use disorder and epilepsy. Phenazepam has not been licensed elsewhere in the world. The actions of phenazepam are mediated by the GABAA-receptor and reversed by the selective benzodiazepine antagonist flumazenil. In vitro, phenazepam and its metabolite 3-hydroxyphenazepam potentiate GABA responses with EC50-values of 6.1 nM and 10.3 nM, respectively, comparable to the value of 13.5 nM for diazepam. In vivo, phenazepam induces pronounced myorelaxation in the rotarod test with an ED50-value of 2.48 (1.65-3.72) mg/kg, and at 10 mg/kg it decreases punished responding in the conflict test (conflict between drinking motivation and painful electrical stimuli). Phenazepam increases the duration of sleep induced by hexanal several fold and is in this respect superior to diazepam. Both phenazepam and 3-hydroxyphenazepam are full GABAA receptor agonists.

Nimetazepam (Erimin) is an intermediate-acting hypnotic drug which is a benzodiazepine derivative. It was first synthesized in 1962 in Japan. It does possess hypnotic, anxiolytic, sedative, and skeletal muscle relaxant properties. Nimetazepam is also an anticonvulsant. It is sold in 5 mg tablets known as Erimin. It is generally prescribed for the treatment of short-term severe insomnia in patients who have difficulty falling asleep or maintaining sleep. Nimetazepam is currently a Schedule IV drug under the international Convention on Psychotropic Substances of 1971. In Singapore, nimetazepam is a class C drug under the Misuse of Drugs Act. In Hong Kong, nimetazepam is regulated under Schedule 1 of Hong Kong's Chapter 134 Dangerous Drugs Ordinance. Nimetazepam can only be used legally by health professionals and for university research purposes.

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.