Adafenoxate exerts nootropic and anxiolytic properties in rodents. Adafenoxate inhibits monoamine oxidase and cAMP phosphodiesterase activity. Adafenoxate inhibits monoamine uptake and regulates the density of the 5-HT1 sites in the brain.

Eprazinone has been variously described as having mucolytic or expectorant properties as well as a direct relaxant action on bronchial smooth muscle and it suppress the excitation of cough center to stop coughing. It is usually used to treat symptoms of cough and phlegm caused by respiratory diseases such as cold, upper respiratory infection, bronchitis, and pneumonia The most commonly reported adverse reactions include loss of appetite, nausea/vomiting, stomach discomfort, diarrhea (including loose stool) and symptom of irritation.

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.

Fenaclon is an anticonvulsant. It was developed in the former USSR. It is indicated for the treatment of epilepsy.

Acefylline is a stimulant drug of the xanthine chemical class. It acts as an adenosine receptor antagonist. Acephylline piperazine is a theophylline derivative with a direct bronchodilator action. It has the advantages over theophylline in being far less toxic and producing minimal gastric irritation. It is indicated for the treatment of asthma, emphysema, acute and chronic bronchitis associated with bronchospasm.Acefylline relaxes smooth muscles, relieves bronchospasm & has a stimulant effect on respiration. It stimulates the myocardium & central nervous system, decreases peripheral resistance & venous pressure & causes diuresis. The mechanism of action is still not clear, inhibition of phosphodiesterase with a resulting increase in intracellular cyclic AMP does occur, but not apparently at concentrations normally used for clinical effect. Other proposed mechanisms of action include adenosine receptor antagonism, prostaglandin antagonism & effects on intracellular calcium. Sodium phenobarbital is a non-selective central nervous system depressant that is primarily used as sedative-hypnotic.

Pivagabine [4-(2,2-dimethyl-1-oxopropylamino) butanoic acid] is a hydrophobic 4-aminobutyric acid derivative with neuromodulatory activity. Pharmacokinetic and toxicological evaluations showed that pivagabine penetrates the blood-brain barrier in rats, does not undergo metabolic transformation and exhibits a low toxicity after either single or repeated administration. Moreover, behavioral studies demonstrated that this compound prevented pentylenetetrazol- and bicuculline-induced convulsions in rats. Pivagabine was shown to improve performance on stress-related tests by reducing the anxiety-producing reactions to the various experimental settings. The marked antistress action of Pivagabine is mediated by antagonizing the effects of stress on GABA(A) receptor function and corticotropin-releasing factor concentrations in the brain, but not by altering the stress-induced increase in neurosteroid concentrations. Pivagabine treatment reduced the physical and mental fatigability of neurasthenia patients and increased their sense of well-being.

Ibudilast (KETAS®) is a non-selective cyclic nucleotide phosphodiesterase (PDE) inhibitor. It is an antithrombotic, antiasthmatic drug that is used for improving prognosis and relieving symptoms in patients suffering from ischemic stroke and for the treatment of bronchial asthma. A definitive mechanism of its action is yet to be established. However, inhibition of the release of inflammatory cytokines, inhibition of leukocyte activation, and inhibition of the expression of cell adhesion molecules have been proposed as likely mechanisms of action of ibudilast (KETAS®). It is currently in development in the US (for instance as a potential therapy for multiple sclerosis), but is approved for use in Japan.

Cotinine is a product formed after the chemical nicotine enters the body. Measuring cotinine in people’s blood is the most reliable way to determine exposure to nicotine for both smokers and nonsmokers exposed to environmental tobacco smoke. Cotinine is safe, non-addictive and has pharmacokinetic properties adequate for therapeutic use. Research has shown that cotinine has antipsychotic, anxiolytic, and antidepressant properties and modulates the serotonergic, cholinergic and dopaminergic systems. Cotinine behaves as a positive allosteric modulator of the nicotinic acetylcholine receptors and has anti-inflammatory effects. Cotinine is under investigation as an agent for the treatment of depression, PTSD, schizophrenia, Alzheimer's disease and Parkinson's disease.

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.

Trifluomeprazine is a sedative and hypnotic, it was used in veterinary medicine under the brand name Nortran. Withdrawn from the market.