Dimetofrine is a selective agonist of post-synaptic a1-adrenergic receptors. The drug was investigated as a cardiostimulant to treat orthostatic hypotension. Clinical investigation showed that dimetofrine relieves asthenia, paleness, drowsiness, fatigue, headache and other symptoms associated with hypotension. It was observed, that in acidic conditions similar to conditions in the stomach, dimetofrine is able to react with nitrites with the formation of highly mutagenic compound 2,6-dimethoxy-1,4-benzoquinone (DMBQ).

Oleoylethanolamide (oleic monoethanolamide, OEA), the naturally occurring amide of ethanolamine and oleic acid, is an endogenous lipid that modulates feeding, body weight, and lipid metabolism by binding with high affinity to the ligand-activated transcription factor, peroxisome proliferator-activated receptor-alpha (PPAR-alpha). OEA reveals the pharmacological properties in the treatment of obesity, atherosclerosis and other diseases. It was shown, that OEA can be used to control hunger in Prader-Willi syndrome, in addition, it exhibited neuroprotective properties in Parkinson's disease experiments. OEA is an endogenous ligand of the orphan receptor GPR119, a G protein-coupled receptor (GPCR) expressed predominantly in the human and rodent pancreas and gastrointestinal tract and in rodent brain, suggesting that the reported effects of OEA on food intake may be mediated, at least in part, via the GPR119 receptor. Recently was shown, that OEA was an effective inhibitor of hyperpigmentation through activation of ERK, Akt and p38 pathways, inhibition of the CREB pathway, and subsequent down-regulation of MITF, TRP-1 and tyrosinase production. Therefore, OEA could be a useful therapeutic agent for use in the treatment of hyperpigmentation and could be an effective component in whitening and lightening cosmetics.

Silymarin, a plant-derived flavonoid from the plant Silybum marianum, is considered the most potential drug to treat almost all kind of liver diseases, particularly alcoholic liver disease, acute and chronic viral hepatitis and toxins-mediated liver dysfunctions. The main component of the silymarin complex is silybin, synonymous with silibinin, sometimes incorrectly called silybinin, which is a mixture of two diastereomers A and B in approximately 1:1 proportion. The drug possess hepatoprotective and antioxidant activity. The hepatoprotective effect is due to stimulation of synthesis of structural and functional proteins and phospholipids, as well as acceleration of the regeneration of hepatocytes. Antioxidant effect is determined by interaction of bioflavones with free radicals in the liver and its detoxication. In such manner the process of peroxidation of the lipids is interrupted and further liver destruction is prevented. Side effect is a mild laxative effect has occasionally been observed.

Nandrolone cyclohexylpropionate (a derivative of Nandrolone, which is approved by FDA) is an anabolic steroid. Nandrolone cyclohexylpropionate is reported as an ingredient of Sanabolicum in Austria. Sanabolicum is a rarely found version of the anabolic androgenic steroid nandrolone, with a CycloHexylPropionate ester. This modification makes nandrolone more anabolic (muscle building) and less androgenic. Nandrolone cyclohexylpropionate is an androgen receptor agonist.

Reproterol is a short-acting β2 adrenoreceptor agonist used in the treatment of asthma. Reproterol increases the generation of cAMP in isolated peripheral blood monocytes in vitro more effectively than does orciprenaline. In the presence of the highly potent but nonselective ß-antagonist, propranolol, the cAMP-generating action of reproterol was inhibited only partially. Reproterol has gained wide use when it was licensed as a fixed combination therapy with cromoglycate. Until today, the bronchodilator effects of reproterol and the bronchoprotective and anti-inflammatory actions of cromoglycate combined in one inhaler remain the successful fixed combination of a disease-modifying and symptomatic drug for the treatment of asthma.

Resocortol butyrate is a corticosteroid which has a high intrinsic glucocorticoid activity. Its mineralocorticoid and progestational activity is very low. Resocortol butyrate has local and systemic glucocorticoid effects. The expression of these effects depends on the mode of application and the dosage applied. After topical application on the skin, a local anti-inflammatory effect is seen, which is accompanied by a moderate and reversible adrenal suppression at higher doses. After oral administration in dogs few systemic effects were observed. Resocortol butyrate was marketed under the brand name Pruban as the topical cream for the treatment of acute localised moist dermatitis in dogs. It was discontinued.

Urapidil is an anti-hypertensive agent approved in Europe for the treatment of the corresponding disease. The drug acts by activating 5HT1a receptor and inhibiting alpha1-adrenergic receptors.

Bephenium is an anthelmintic agent formerly used in the treatment of hookworm infections and ascariasis (as a hydroxynaphthoate salt). Bephenium exerts its anti-helminthic action by inducing muscle contraction in parasites. The contraction is suggested to be mediated by B-type AChR receptors, which are activated upon administration of bephenium.

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.