Besipirdine is a potential novel first-in-class oral treatment for over active bladder currently in Phase II development, with a mechanism of action clearly different from that of antimuscarinics. It was under evaluation by Aventis up to phase III for Alzheimer’s disease, involving the administration of the compound to over 1500 patients. However, this research has been discontinued. Besipirdine antagonizes alpha-2 and alpha-1 adrenoceptors and inhibits both norepinephrine and serotonin uptake. The most common adverse events were asymptomatic postural hypotension and asymptomatic bradycardia.

Thozalinone (Stimsen) has been used as an antidepressant in Europe and has also been trialed as an anorectic. It acts via inducing the release of norepinephrine and dopamine as with its analogues pemoline and aminorex. Thozalinone has been shown to possess some pharmacologic actions similar to those of amphetamine and imipramine, but with important differences. It is less toxic than amphetamine, and its margin of safety in mice is greater. The stimulant action does not progress to tremors or convulsions as the dosage is increased. The anorexigenic activity of thozalinone is more pronounced and longer lasting than that of amphetamine. There is no evidence of the development of tolerance. The cardiovascular side effects of thozalinone are minimal, and analeptic actions are absent.

Benzodiazepines represent a group of two-ring heterocyclic compounds consisting of a benzene ring fused to a diazepine ring. Benzodiazepines (BZDs) are one of the most widely prescribed pharmacologic agents in the United States (more than 112 million prescriptions in 2007). BZDs are used for numerous indications, including anxiety, insomnia, muscle relaxation, relief from spasticity caused by central nervous system pathology, and epilepsy. BZDs are also used intraoperatively because of their amnesic and anxiolytic properties. However, these properties become undesired side effects in nearly all other clinical instances. BZDs act as positive allosteric modulators on the gamma amino butyric acid (GABA)-A receptor. The GABA-A receptor is a ligand-gated chloride-selective ion channel. Benzodiazepines are a large drug class and have a long history of development, starting with the first FDA-approvals in the 1960s. All benzodiazepines are listed as DEA schedule IV controlled substances. As controlled substances, all benzodiazepines have the potential for abuse, addiction and diversion.

Gidazepam (also known as hydazepam or hidazepam) is an anxiolytic and atypical benzodiazepine derivative, developed in the Soviet Union and used to treat the nervous system diseases. Interacts with benzodiazepine receptors, increases the sensitivity of GABA receptors to the mediator, increases the inhibitory effect of GABA in the central nervous system. Reduces the excitability of the subcortical structures of the brain, inhibits polysynaptic spinal reflexes. Reduces emotional tension, fear, anxiety. It has an activating effect, vegetostabilizing properties, mildly relaxed and relaxing substance. Virtually does not affect the productive symptoms of psychotic genesis (acute delusional, hallucinatory, affective disorders), there is rarely a decrease in affective tension. There is evidence of a positive effect on the cardiovascular system of patients with a neurological condition and in healthy people in stressful situations.

Piroheptine is an antagonist of muscarinic acetylcholine receptors. The drug was used for the treatment of Parkinson's disease, however, it is no longer marketed.

PHENYLACETYLGLYCINE DIMETHYLAMIDE is a analgesic and antipyretic. Known as Ralgin in Japan. Has being shown to have neurological activity.

Methylbenactyzium bromide has been used as a spasmolytic for the treatment of gastrointestinal ulcer and gastrointestinal spasms.

Fenproporex is a central and indirect-acting sympathomimetic. It was developed as an anorectic drug. Their anorectic effects are believed to be a result of adrenergic activation. Fenproporex has never been approved by the US Food and Drug Administration (FDA) for sale in the US due to lack of efficacy and safety data. There is a paucity of randomized, placebo-controlled trials on Fenproporex. These studies suggest that Fenproporex is modestly effective in promoting weight loss. Data from these studies are insufficient to determine the risk-benefit profile of Fenproporex. Abuse potential and amphetamine-like adverse effects are causes for concern. Adverse effect most frequently reported are: insomnia, anxiety, depression, irritability, dry mouth.

4-Amino-3-hydroxybutanoic acid (GABOB) is an endogenous ligand found in the central nervous system in mammals. γ-Amino-β-hydroxybutyric acid is a derivative of the neurotransmitter GABA. It has been claimed to be of value in neurological disorders and to have an antihypertensive effect. γ-Amino-β-hydroxybutyric acid can help overcome stress and anxiety, improve learning and boost memory function. It is also known to increase growth hormone levels, which help the body heal and rejuvenate itself. There are no reported side effects of γ-Amino-β-hydroxybutyric acid when taken at therapeutic dosages. At high dosages, some slight drowsiness may occur. Adverse effects have included dizziness and anorexia also.

Prednisolone farnesylate, a synthetic glucocorticoid, is a terpene-modified compound of prednisolone with an antiinflammatory and antirheumatic action. Glucocorticoid receptor agonists. Farnerate Gel (trade name from Dainippon Pharmaceuticals) and Farnezone Gel (Taiho Pharmaceuticalshave) were launched in Japan in 1998 as topical rheumatoid arthritis (RA) product to treat symptoms associated with RA such as finger, hand and elbow swelling and pain.