Sinapic acid is one of the most common hydroxycinnamic acids and is widespread in the plant kingdom. It has been identified in various fruits, vegetables, cereal grains, oilseed crops, some spices, and medicinal plants. Sinapic acid and its derivatives possess antimicrobial, antioxidant, anti-inflammatory, anticancer and anti-anxiety activities.

Myosmine (3-(1-pyrrolin-2-yl)pyridine) is a minor tobacco alkaloid widely occurring in food products of plant and animal origin. Myosmine expresses significant genotoxic effects in human target cells of carcinogenesis. After nitrosation and/or peroxidation, myosmine gives rise to reactive pyridyloxobutylating species which are capable of forming pyridyloxobutylated DNA adducts.

Paraherquamide (PHQ), a potent and broad-spectrum anthelminthic. Paraherquamide (PHQ), 2-deoxoparaherquamide (2DPHQ), and close structural analogs of these compounds rapidly induce flaccid paralysis in parasitic nematodes in vitro, without affecting adenosine triphosphate (ATP) levels. Paraherquamide anthelmintics are nicotinic cholinergic antagonists in both nematodes and mammals, and this mechanism appears to underlie both their efficacy and toxicity. Paraherquamide A is a natural product produced by Penicillium paraherquei which was discovered in 1981. It was evaluated by Merck in the late 1980’s and a small chemistry effort was conducted to produce analogs. Paraherquamide A was found to have outstanding broad spectrum nematocidal activity against various sheep gastro-intestinal nematodes. It is a nicotinic antagonist that blocks depolarization in muscles and induces a rapid paralysis of the mid-body of the parasite. However, it was severely toxic in mice and dogs, which prevented its development, as these species are the standard models for safety studies.

Du-24565 is a potent and selective inhibitor of the synaptosomal uptake of serotonin. At higher concentration, it affects the uptake of norepinephrine and dopamine. It is a potential antidepressant and can be useful as a pharmacological tool to study the role of 5-HT in the central nervous system. DU-24565 had little effect on serotonin or tyrosine accumulation in human melanoma cells but suppressed the uptake of extracellular Dopa. In vitro, DU-24565 inhibited the proliferation of PC-3, DU-145 and LNCaP human prostate carcinoma cells in a dose-dependent manner.

Norlidocaine (monoethylglycinexylidide, MEGX) is the major metabolite of lidocaine. The lidocaine metabolites formed on the first pass, which include MEGX and GX, have additive central nervous system (CNS) toxicity to lidocaine itself, making oral administration unacceptable. Monoethylglycinexylidide (MEGX) also has local anesthetic activity. It contributes to central nervous system (CNS) toxicity in some patients treated with lidocaine. Lidocaine is eliminated mainly by biotransfomation to monoethylglycinexylidide. MEGX has pharmacologic activity. MEGX has an antiarrhythmic potency of the same order as lidocaine in vitro in a guinea pig atrium model and is about half as potent in vivo in dogs.

SCH-23390 is a potent and selective antagonist of the D1A and D1B dopamine receptors having Ki of 0.2 and 0.3 nM respectively. The C11 radiolabeled version has proven to be useful as a PET imaging probe in humans for the investigation of a number of neurological conditions including Schizophrenia, Parkinson's Disease, and Huntington's Disease. It should be noted that the non-radiolabeled compound did receive preclinical interest as a potential therapeutic (annotated separately), although such efforts have been discontinued due to side-effects and a lack of therapeutic efficacy.

Sulforaphane is a naturally-occurring phytochemical belonging to the class of isothiocyanates. As the aglycone metabolite of glucosinolate glucoraphanin (sulforaphane glucosinolate), sulforaphane acts as an antioxidant and potent stimulator of endogenous detoxifying enzymes. This agent displays anticarcinogenic properties due to its ability to induce phase II detoxification enzymes, such as glutathione S-transferase and quinone reductase, thereby providing protection against certain carcinogens and toxic, reactive oxygen species. Broccoli sprouts contain large amounts of sulforaphane, which is also found in other cruciferous vegetables including cabbage and kale. Sulforaphane is under investigation for the treatment of Autism Spectrum Disorder and Schizophrenia.

Erucamide is a fatty acid amide, which is similar to the classical endocannabinoid analog oleoylethanolamide. It was discovered in mice, that erucamide may regulate the central nervous system and may have the potential to antagonize depression and anxiety and these effects of the compound may be related to the regulation of the hypothalamus-pituitary-adrenal axis (HPA).

Theaflavin is a black tea polyphenol, which possesses a wide variety of pharmacological properties including potent antioxidative, anti-apoptotic, anti-cancer and anti-inflammatory effects. Theaflavin (TF-1) can bind to, and inhibit the purified 20S proteasome, accompanied by suppression of tumour cell proliferation, suggesting that the tumour proteasome is an important target whose inhibition is at least partially responsible for the anticancer effects of black tea. Theaflavin is a potent inhibitor of interleukin-8 gene expression in vitro. The proximal mechanism of this effect involves, in part, inhibition of IkappaB kinase activation and activator protein-1 pathway. Theaflavin has been known to possess neuroprotective effects against ischemia, Alzheimer's disease and other neurodegenerative disorders.

Salsolinol (1-methyl-6,7-dihydroxy-1,2,3,4-tetrahydroisoquinoline, SAL) is a tetrahydroisoquinoline derivative, detected in humans. Salsolinol can be formed in the mammalian brain by three different mechanisms: (1) via the nonenzymatic Pictet–Spengler condensation of dopamine and aldehydes producing salsolinol as two racemic isomers (R or S). (2) By the nonenzymatic condensation of dopamine and pyruvate yielding 1-carboxyl-tetrahydroisoquinoline, followed by decarboxylation and reduction, which produces (R)-salsolinol. (3) By selective synthesis of (R)-salsolinol from dopamine and acetaldehyde, the level of which is increased after ethanol intake. Apart from that salsolinol has also been detected in certain beverages and foodstuff, including soy sauce, cheese. Only the (R) enantiomer of Salsolinol and occur in the human brain, cerebrospinal fluid (CSF) and intraventricular fluid (IVF), and the (S) enantiomer was not detected. Salsolinol was also found to be involved in neurotoxicity processes altering the normal function and survival of dopamine neurons. It has been proposed, that salsolinol participated in the etiopathogenesis of Parkinson’s disease. Salsolinol could inhibit various enzymes, for example, monoamine oxidase and tyrosine hydroxylase and recently was revealed, that (R)-SAL and (S)-SAL were agonists of the μ-opioid receptor. (S)-SAL is a more potent agonist than the (R)-SAL stereoisomer, it was suggested that an opioid action of SAL or its enantiomers is involved in the rewarding effects of ethanol.