Norbolethone is a 19-nor anabolic steroid first synthesized in 1966. During the 1960s it was administered to humans in efficacy studies concerned with short stature and underweight conditions. It has never been reported by doping control laboratories prior to 2001. Norbolethone matches the description for what is described as a "designer steroid. " In fact, Norbolethone was given in clinical trials over 30 years ago and never given the green light. No supply was ever manufactured, and no test was ever developed to detect this substance, yet ironically, it was suspected of being used in the 2000 Olympics based on blood and urine assays done by the IOC. Norbolethone was used in the treatment of idiopathic underweight, prevention of indomethacin-induced intestinal ulcers.

Meclonazepam (Ro11-3128 or 3-methylclonazepam) is a benzodiazepine derivative. It exerts anxiolytic activity. Meclonazepam demonstrated anti-schistosomal action, it causes spastic paralysis, calcium influx and tegumental disruption in the parasites. Contracturant effect of meclonazepam is not a result of its binding to the worm benzodiazepine binding sites.

Ibutamoren (L-163,191 MK-0677) is a spiropiperidine agonist of the ghrelin receptor and a growth hormone secretagogue. Ibutamoren mimics the actions of growth hormone releasing peptide-6 to increase serum levels of serum insulin-like growth factor-I (IGF-I). Orally active Ibutamoren was being developed by Merck & Co. for a variety of indications, including fibromyalgia, muscle wasting/weakness in patients with chronic kidney disease, Alzheimer's disease and fractures.However, there has been no recent development reported or development has been discontinued for these indications.

HU-308 ([(1R,2R,5R)-2-[2,6-dimethoxy-4-(2-methyloctan-2-yl)phenyl]-7,7-dimethyl-4-bicyclo[3.1.1]hept-3-enyl]methanol) is a potent, selective agonist for the CB2 receptor. The synthesis and characterization took place in the laboratory of Prof. Mechoulam at the Hebrew University of Jerusalem in the late 1990s. It has analgesic effects, promotes proliferation of neural stem cells,[3] and protects both liver and blood vessel tissues against oxidative stress via inhibition of TNF-α. In vivo, HU-308 has hypotensive, analgesic, and anti-inflammatory activities in mice that can be reversed by the CB2 receptor antagonist SR 144528 but not the CB1 receptor antagonist rimonabant. Pretreatment of mice with HU-308 decreases the I/R-induced tissue damage, inflammatory cell infiltration, tissue, and serum TNF-α, MIP-1, and MIP-2 levels, tissue lipid peroxidation, and apoptosis. HU-308 increases proliferation of HT29 colon cancer cells and growth of tumors in an HT29 mouse xenograft model. The physiological and toxicological properties of this compound have not been evaluated in humans.

Clonitazene is a synthetic opioid analgesic, structurally related to etonitazene. In the USA clonitazene is a schedule I narcotic controlled substance.

Ipamorelin is a new and potent synthetic pentapeptide which has distinct and specific growth hormone (GH)-releasing properties. Ipamorelin mimics ghrelin and binds to the ghrelin receptor (or GH secretagogue receptor, GHSR) in the brain, thereby selectively stimulating the release of GH from the pituitary gland. This results in increased plasma GH levels, which would affect many biological processes. Besides its presence in the brain, GHSR can also be found in the gastrointestinal tract, heart, lung, liver, kidney, pancreas, adipose tissue and immune cells. Unlike other GH releasing peptides, ipamorelin only stimulates GH release in a manner very similar to that of growth hormone releasing hormone.

Etaqualone (Aolan, Athinazone) is an analog of the hypnotic methaqualone, a non-barbiturate sedative it was developed and marked in France. Etaqualone possesses sedative and hypnotic properties and was used to treat insomnia resulting from its agonist activity at the β subtype of the GABAa receptor.

Diclofensine is an antidepressant with equipotent inhibitive effects on the neuronal uptake of norepinephrine (NE), serotonin, and dopamine. It is devoid of monoamine-releasing or monoaminoxidase-inhibiting properties. Diclofensine was found to be an effective antidepressant in human trials, with relatively few side effects, but was ultimately dropped from clinical development.

Mecloqualone is a quinazoline-class GABAergic and an analog of methaqualone. It acts as an agonist of the beta subtype of GABAa receptor and induces sedative, hypnotic and anxiolytic effects. Mecloqualone was marketed (mostly in france) under the names Nubrene and Casfen for the treatment of insomnia. Mecloqualone is no longer prescribed because of concerns about its potential for abuse and overdose. In the United States, it is registered as a Schedule-I non-narcotic controlled substance.

Eticyclidine (N-ethyl-1-phenylcyclohexylamine) is a phencyclidine derivative exerting nearly the same pharmacological profile as the parent compound. In rodents, it induces stereotypy, ataxia, interoceptive effect and hypothermia.