Alpidem is an imidazopyridine anxiolytic acting as a partial agonist at γ-aminobutyric acid A (GABA(A)) receptor. Alpidem is selective for GABAA receptors bearing α1 subunits. Alpidem was briefly marketed for the treatment of anxiety, but was withdrawn because of liver toxicity.

Doxifluridine is a 5-fluorouracil prodrug that is being tested for the treatment of cancer. The cleavage into 5-fluorouracil occurs enzymatically via a nucleoside phosphorylase. Thus, doxifluridine is not active by itself and its antitumor activity is related to its metabolic conversion into 5-fluorouracil. Doxifluridine has neurotoxic adverse effects.

Zetidoline (DL-308) is an antipsychotic drug with antidopaminergic properties. It is a dopamine D2 receptor antagonist. DL-308 displayed sedative properties, as indicated by the sedated appearance of the subjects, by a decrease in subjectively rated alertness and by an impairment of performance on psychomotor tests. DL-308 appeared to be a more potent sedative than thioridazine. DL-308 (10 mg) caused an increase in subjectivey rated sweating and objectively measured heart rate, suggesting a sympathomimetic property for the drug. DL-308 had effects consistent with an alpha-adrenolytic action; it caused miosis, hypotension and a decrease in salivation. DL-308 had little effect on the motor system, as indicated by conventional clinical neurological examination.

Phosmet is a non-systemic, organophosphate insecticide used on both plants and animals. Phosmet is mainly used on apple trees for control of coddling moth, though it is used on a wide range of fruit crops, ornamentals and vines for the control of aphids, suckers, mites and fruit flies. Phosmet is a moderately potent cholinesterase inhibitor.

Naftopidil (INN, marketed under the brand name Flivas) is a drug used in benign prostatic hypertrophy which acts as a selective alpha1-adrenergic receptor antagonist, has been used for the treatment of benign prostatic obstruction and benign prostatic hyperplasia (BPH) associated lower urinary tract symptoms (LUTS). The Japanese Ministry of Health, Labor and Welfare approved naftopidil for treating men with BPH in 1996. Although well-designed, randomized studies are warranted to confirm the long-term outcomes and effector/target of naftopidil, the α1A-antagonist naftopidil, which also blocks α1D-adrenoceptor, improves voiding symptoms, and may also be useful for the management of men with storage symptoms represented by nocturia, retrieving their quality of life impaired by BPH-associated LUTS. The selective alpha1D-blocker naftopidil can significantly facilitate spontaneous passage of distal ureteral stones with few side effects, providing a new choice for medical expulsive therapy.

Amygdalin is a naturally occurring cyanogenic glycoside derived from nuts, plants, and the pits of certain fruits, primarily apricots. Bitter almonds containing amygdalin are used in Traditional Chinese Medicine to remove “blood stasis” and to treat abscesses. Amygdalin was first used as a cancer treatment in Russia in 1845, and in the United States in the 1920s. Laetrile is another name for the natural product amygdalin. Hydrogen cyanide is thought to be the main anticancer compound formed from laetrile (Amygdalin) via in situ release. Cyanide from the hydrolysis of amygdalin is believed to be cytotoxic with actions selective against cancerous cells, but results from animal studies were mostly negative. Other animal studies suggest it may help to relieve pain due to its anti-inflammatory and analgesic effects. One study suggested amygdalin can inhibit tumor growth, but subsequent tests were unable to confirm this observation. Laetrile (Amygdalin) has shown little anticancer activity in animal studies and no anticancer activity in human clinical trials. In 1970, an IND application to study laetrile was filed by the McNaughton Foundation (San Ysidro, California). This request was initially approved but later rejected because preclinical evidence in animals showed that laetrile was not likely to be effective as an anticancer agent. The side effects associated with laetrile toxicity mirror the symptoms of cyanide poisoning, including liver damage, difficulty walking (caused by damaged nerves), fever, coma, and death. Laetrile (Amygdalin) is not approved for use in the United States.

Spiperone (Spiroperidol; brand name: Spiropitan (JP)) is a typical antipsychotic and research chemical belonging to the butyrophenone chemical class. Spiperone is selective D2 dopamine receptor antagonist; α1B-adrenoceptor antagonist; mixed 5-HT2A/5-HT1 serotonin receptor antagonist. Additionally, spiperone was identified by compound screening to be an activator of Ca2+ activated Cl− channels (CaCCs), thus a potential target for therapy of cystic fibrosis. Spiperone is widely used as a pharmacological tool for studying neurotransmitter receptors.

Zinterol (MJ-9184-1) is an beta-adregenrgic agonist demostrated activity toward beta1-3 receptors. Oral zinterol caused a fast-appearing and long-lasting bronchodilator effect in patients with with stable chronic obstructive lung disease, however it seems development of zinterol was discontitued.

Zylofuramine is a psychomotor stimulant. It intended for use as an appetite suppressant and for the treatment of senile dementia in the elderly, but there is little information about it and it does not appear to have ever been marketed.

Tolycaine hydrochloride is an amide local anaesthetic included in some preparations to reduce the pain of injection. It can be used for dental injection.