Lappaconitine is an alkaloid isolated from the root of Aconltitum sinomantanum Nakai. It has a strong analgesic activity that does not involve the opioid receptor. It was shown to have class-I antiarrhythmic action and irreversibly blocks cloned human heart (hH1) channels by binding to the site 2 receptor.

Raclopride is a salicylamide neuroleptic, that acts as a selective antagonist of D2 dopamine receptors both in vitro and in vivo. Tritium-labelled raclopride has properties that demonstrate its usefulness as a radioligand for the labelling of dopamine-D2 receptors : 3H-Raclopride has a high affinity for the rat and human dopamine-D2 receptors, the non-specific binding of 3H-raclopride is very low, not exceeding 5% of the total binding and the distribution of the 3H-raclopride binding sites in the brain closely correlates with the dopaminergic innervation. The binding of 3H-raclopride is blocked by dopamine-D2 agonists and antagonists, while the D1 agonist SKF 38393 and the Dl antagonist SCH 23390 have much less potency. The interaction of dopamine with 3H-raclopride binding results in a shallow competition curve, which suggests that 3H-raclopride, similar to other dopamine-D2 radioligands, labels both high and low agonist affinity states of the dopamine-D2 receptor. The in vivo receptor binding studies performed with 3H-raclopride also demonstrate its favorable properties as a dopamine-D2 receptor marker in vivo In contrast to some other compounds used as radioligands, raclopride enters the brain readily and binds with a low component of non-specific binding in all dopamine-rich brain areas. A saturation curve may be achieved in vivo binding studies since injections of increasing concentrations of 3H-raclopride appears to be saturated at concentrations above 25 mkCi (corresponding to approximately 5 nmol/kg). Raclopride antagonizes apomorphine-induced hyperactivity in the rat at low doses (ED50 = 130 nM/kg i.p.) but induces catalepsy only at much higher doses (ED50 = 27 mkM/kg i.p.). Radiolabelled raclopride has been used as a ligand for in vitro and in vivo autoradiography in rat and primate brains. Raclopride C 11 is used with positron emission tomography (PET) as a clinical research tool to determine dopamine type 2 (D 2) receptor density in the human brain under normal and pathological conditions. For example, raclopride C 11 used in PET studies has served to confirm the age-related decrease in striatal dopamine D2 receptor density, which may be associated with a decline in the motor as well as cognitive functions. In patients with Alzheimer's disease, raclopride C 11 may be used to examine neuroreceptor distribution and quantities, which may help in the analysis of degenerative alterations of neuron populations and neuroreceptor systems in patients with this disease. In Huntington's disease, in which degeneration of neostriatal interneurons occurs (postsynaptic to the dopaminergic input), specific binding of raclopride C 11 to D 2 receptors may serve as one of the parameters in predicting performance in cognitive tasks.

Bicyclol, also known as SY 801, is a hepatoprotective agent. Bicyclol upregulates transcription factor Nrf2, HO-1 expression and protects rat brains against focal ischemia. Bicyclol induces cell cycle arrest and autophagy in HepG2 human hepatocellular carcinoma cells through the PI3K/AKT and Ras/Raf/MEK/ERK pathways. Bicyclol attenuates tetracycline-induced fatty liver associated with inhibition of hepatic ER stress and apoptosis in mice. Bicyclol promotes toll-like 2 receptor recruiting inosine 5'-monophosphate dehydrogenase II to exert its anti-inflammatory effect. Phase Ⅰ~Ⅳ clinical trials and extensive application after market launch prove that, Bicyclol is suitable for the treatment of chronic viral and non-viral liver disease with elevated serum aminotransferase abnormalities, and is excellent in safety. This drug is recommended for liver protection and anti-inflammatory medication by Chinese Medical Association in Guidelines for Management of Alcoholic Fatty Liver Disease, Guidelines for Management of Non-alcoholic Fatty Liver Disease, The Guideline of Prevention and Treatment for Chronic Hepatitis B, Expert Consensus On Hepatic Inflammation and Its Prevention and other professional guidelines and consensus.

Cupric salicylate is an anti-inflammatory agent which was used as pain relief for patients with osteoarthritis, rheumatoid and other degenerative diseases (as a copper-salicylate complex). The preparation seem to be discontinued for now.

9-Hydroxy chrysarobin or 3-methylanthralin is a pure product of chrysophanic acid reduction. The compound 3-methylanthralin is listed in the Merck Index as an antipsoriatic. Chrysarobin is a mixture of compounds derived from Goa powder, and includes 3-methylanthralin. Goa powder (Araboba) is derived from the wood and bark of Andria Araroba Aguiar (Leguminosae). Literature references describing the isolation of chrysarobin date back to the second part of 1800s. A method of reducing chrysarobin to obtain 3-methylanthralin was known as early as 1931. At present chrysarobin is used in the topical antipsoriatic compositions with natural plant extracts and as a homeopatic product. Pure 3-methylanthralin when tested on mice in vivo was found to play an important role in skin hyperplasia and promotion of skin carcinogenesis by effecting the expression of several gap-junctional proteins connexins (Cxs) and inhibiting glucocorticoid receptor expression in mouse epidermis specifically in keranocytes. Chrysarobin is approved by FDA as an over-the-counter drug. ProZ92 is a trade name a patented botanical formula, topical marketed in Israel which primary anti-psoriatic agents are: 3-methylanthralin, chrysophanol, aloe-emodin and aloe-emodin acetate.

Phenocoll is an antineuralgic, analgesic and antipyretic drug. It is a derivative of phenacetin and thus has the same mechanism of action (COX-2 inhibition). Hydrochloride and salicylate salts of phenocoll were used to control inflammation in such diseases as gout, influenza, malaria, rheumatism and pleuritis. The drug is no longer available for marketing.

Levormeloxifene (INN) is an experimental selective estrogen receptor modulator (SERM) that was being developed as an alternative to estrogen replacement therapy for the treatment and prevention of postmenopausal bone loss. Levormeloxifene is the levorotatory enantiomer of non-hormonal, non-steroidal oral contraceptive -- ormeloxifene (trade names Novex-DS, Centron, and Sevista). The development of Levormeloxifene was stopped because of a high incidence of gynecologic adverse events during clinical trials.

Zyrconium cyclosilicate (ZS-9) is a selective oral sorbent that traps potassium ions throughout the gastrointestinal tract. ZS-9 is not systemically absorbed; accordingly, the risk of systemic toxicity may be minimized. ZS-9 was originally developed by ZS Pharma, and later licensed to AstraZeneca. In 2018 the FDA has approved ZS-9 for treatment of hyperkalemia.

N-hydroxymethylsuccinimide is used for ester prodrugs synthesis and as proallergen in epicutaneous patch test, indicated for use as an aid in the diagnosis of allergic contact dermatitis.

Zinc Difumarate Hydrate is one of the sources of zinc and fumarate, which play an important role in energy metabolism. Zinc ions are essential for the formation of ferments with active zinc centers, which are involved in important processes of synthesis occurring in the body. Sufficient amounts of zinc enhance the metabolism of beta cells in the pancreatic islets of Langerhans and promote insulin synthesis and deposition. This in turn contributes to the normalization of fat and carbohydrate metabolism.