Aptiganel (CNS 1102, Cerestat), a selective ligand with antagonized properties for the ion-channel site of the N-methyl-D-aspartate receptor-channel complex, was developed as a neuroprotective agent for focal brain ischemia. However, in the clinical trials in patients with acute ischemic stroke aptiganel was not efficacious at either of the tested doses and may be harmful. That is why its further study was discontinued.

Phenothrin, also called sumithrin and d-phenothrin, a synthetic pyrethroid compound, is widely used to control agricultural and household insects, as well as to eliminate human louse infestation, but studies conducted in Paris, France and the United Kingdom have shown widespread resistance to phenothrin. Synthetic pyrethroids, including phenothrin, have a similar mode of action as organochlorines. They act on the membrane of nerve cells of insects blocking the closure of the ion gates of the sodium channel during re-polarization. This strongly disrupts the transmission of nervous impulses. At low concentrations insects suffer from hyperactivity. At high concentrations they are paralyzed and die. The EPA has not assessed its effect on cancer in humans. However, one study performed by the Mt. Sinai School of Medicine links sumithrin with breast cancer; the link made by sumithrin's effect on increasing the expression of a gene responsible for mammary tissue proliferation.

Gepefrine (Pressionorm and Wintonin) is an antihypotensive agent. It was used for therapy of orthostatic dysregulation. One hour after oral administration of 30 mg or 45 mg gepefrine the blood pressure increased significantly at rest and more markedly on standing and during the step test. Gepefrine led to a reduction in pathological orthostatic regulation during the early phase as well as to the prevention of subjective and objective signs of orthostatic adjustment disorder during the late phase. Patients with insufficient rise in blood pressure during the step test (80 watts) showed after gepefrine a distinct tendency towards normalisation and the regression of subjective states of exhaustion. Gepefrine caused on average no substantive alternations in heart rate during all phases of the investigation. Complications or side-effects due to the method or the medicament were not observed.

Ketobemidone (Cliradon, Ketogan, Ketodur, Cymidon) is a strong opioid analgesic, structurally related to pethidine, which has been in clinical use for more than 50 years. In the Scandinavian countries ketobemidone is only available in combination with a spasmolytic substance N,N-dimethyl-3,3-diphenyl-I-methylallylamine (A29). Ketobemidone has been shown to be a non-competitive N-methyl-D-aspartate (NMDA) receptor antagonist. In spite of a relatively low mu-receptor affinity ketobemidone has a higher analgesic potency than morphine by systemic administration. It is probably due to its higher lipophilicity and consequently more easy penetration into the CNS. Ketobemidone is indicated for the treatment of all types of severe pain, such as postoperative, cancer, kidney stones and fractures.

Norfenefrine or meta-octopamine, also known as 3,β-dihydroxyphenethylamine, is an adrenergic agent used as a sympathomimetic drug which is marketed in Europe, Japan, and Mexico. Along with its structural isomer p-octopamine and the tyramines, norfenefrine is a naturally occurring, endogenous trace amine and plays a role as a minor neurotransmitter in the brain. Norfenefrine controls blood pressure in acute hypotensive states eg pheochromocytomectomy, sympathectomy, poliomyelitis, spinal anesth, MI, septicemia, blood transfusion and drug reactions. Adjunct in treatment of cardiac arrest and hypotension.

Croconazole is a antifungal drug developed for the treatment of dermatomycoses and candidiasis. It has a broad spectrum activity against many microorganisms such as T. mentagrophytes, T. rubrum, M. canis, Microsporum gypseum, and Epidermophyton floccosum. The drug was used as a topical 1% cream under the name Pilzcin. According to the information on the manufacturer (Merz pharma) website, Pilzcin is no longer marketed.

Iobenguane, mainly use as a radiopharmaceutical, used in a scintigraphy method called MIBG scan. Synthetic guanethidine derivative that locates phaeochromocytomas and neuroblastomas. The radioisotope used can either be iodine-123 for imaging or iodine-131 for destruction of tissues that metabolize noradrenaline. Iodine 123 is a cyclotron-produced radionuclide that decays to Te 123 by electron capture. Images are produced by a I123 MIBG scintigraphy. It localizes to adrenergic tissue and thus can be used to identify the location of tumors such as pheochromocytomas and neuroblastomas. With I-131 it can also be used to eradicate tumor cells that take up and metabolize norepinephrine. The radioactive iodine component is responsible for its imaging properties. Iobenguane and guanethidine are substrates for the norepinephrine transporter (NET) and accumulate by the uptake mechanism into presynaptic nerve endings. Unlike norepinephrine, these drugs are protonated under physiologic conditions; therefore, they do not cross the blood–brain barrier and in vivo uptake is limited primarily to systemic neuronal tissue. The accumulation of iobenguane in myocardial tissue is also dictated by the high fraction of aortic blood flow that enters the coronary arteries. This physiology constitutes an ideal molecular targeting mechanism for diagnosis of various cardiac diseases, including heart failure, heart transplant rejection, ischemic heart disease, dysautonomia, and drug-induced cardiotoxicity, as well as cardiac neuropathy related to diabetes mellitus and Parkinson disease

Dexfenfluramine, also marketed under the name Redux, is a serotoninergic anorectic drug. Dexfenfluramine, the dextrorotatory isomer of fenfluramine, is indicated for use in the management of obesity in patients with a body mass index of > or = 30 kg/m2, or > or = 27 kg/m2 in the presence of other risk factors. Unlike fenfluramine, dexfenfluramine is a pure serotonin agonist. Dexfenfluramine increases serotonergic activity by stimulating serotonin (5-hydroxytryptamine; 5-HT) release into brain synapses, inhibiting its reuptake into presynaptic neurons and by directly stimulating postsynaptic serotonin receptors. Dexfenfluramine reduces blood pressure, percent glycosylated hemoglobin, and concentrations of blood glucose and blood lipids, but these benefits may be indirect. Dexfenfluramine may also be of some value in controlling eating habits in diabetic patients, preventing weight gain after smoking cessation, and treating bulimia, seasonal affective disorder, neuroleptic-induced obesity, and premenstrual syndrome. Dexfenfluramine's most frequent adverse effects are insomnia, diarrhea, and headache; it has also been associated with primary pulmonary hypertension. The drug should not be combined with other serotonergic agonists because of the risk of serotonin syndrome. The recommended dosage is 15 mg twice daily. Dexfenfluramine is effective in the treatment of obesity in selected patients. Because its efficacy is lost after six months of continuous treatment, it should be viewed primarily as an adjunct to diet and exercise. Dexfenfluramine was approved by the FDA in 1996 and has been widely used for the treatment of obesity. However, Dexfenfluramine was removed from the U.S. market in 1997 following reports of valvular heart disease and pulmonary hypertension.

Oxaflumazine acid disuccinate, a neuroleptic drug, was studied in the treatment of psychotic children in a pedopsychiatric environment.

Ufenamate is a topical analgesic. It is indicated for pain and inflammation associated with musculoskeletal and joint disorders. It is a COX inhibitor. Ufenamate is freely soluble in oil and is poorly soluble in water. It is used in the form of ointments or creams. It is manufactured under the brand name Combec in Japan. It is also an ingredient of Fenazol Ointment 5%, used in Japan for the treatment of eczema, dermatitis and herpes zoster.