K-134, a 2(1H)-quinolinone derivative, is a phosphodiesterase 3 inhibitor. It has both anti-thrombotic and anti-hyperplastic activities. It was evaluated in a phase II trial in patients with peripheral artery disease and claudication.

Brolamfetamine (also known as DOB, bromo-DMA, and 4-bromo-2,5-dimethoxyphenylisopropylamine) is one of a vast number of compounds used recreationally to achieve hallucinogenic effects. Brolamfetamine is one of the most potent hallucinogens, with its hallucinogenic potency directly linked to its abuse potential. Brolamfetamine acts as a partial agonist of 5HT2A, 5HT2B, 5HT2C, and TAAR1 receptors, but it’s psychedelic effects are mainly mediated by its agonistic properties at the 5-HT2A receptor. Animal studies have shown physiologic effects including hypertension, tachycardia, hyperpyrexia, pupillary dilatation, and peripheral vasoconstriction. In general, Brolamfetamine having a similar effect to LSD, with slower onset (up to 3–4 h to peak intoxication) and longer duration of effect (up to 36 h). Brolamfetamine is not commonly available, through periods of higher circulation were reported in Australia in 1983, Ireland in 2003, and in Italy in 2015. Brolamphetamine, as well as many other synthetic hallucinogens, are increasingly being sold as LSD. Internationally Brolamfetamine is a Schedule I drug under the Convention on Psychotropic Substances. Due to its selectivity, Brolamfetamine is often used in scientific research when studying the 5-HT2 receptor subfamily.

Vinconate possesses both encephalotropic and psychotropic properties. Animal experiments have shown that this compound could induce the facilitation of phosphatidylinositide (PI) turnover via the stimulation of muscarinic acetylcholine receptors. In addition, vinconate could lead to the direct activations of PIP2-specific and cytosolic phospholipase C. The drug was on the stage of preregistration for the treatment of cognition disorders in Japan. However, information about the further fate of this drug is not available.

Tolufazepam is a 1-alkylsulfonylaryl-1,4-benzodiazepine derivative. It exhibited a competitive antagonism of 3H-diazepam binding in the cerebellum, cerebrum and submaxillary gland. Tolufazepam showed anticonvulsant and anxiolytic activity in animal models – it was very potent in preventing convulsions elicited by pentylenetetrazol. This anticonvulsant action was suppressed by previous administration of Ro 15-1788. Tolufazepam was also active in inhibiting suppressive behavior in the test of Vogel.

Penclomedine, a synthetic pyridine derivative that has made its way to clinical trials because of the antitumor activity seen using the NCI screening program. Its mechanism of action is unknown although exists assumption that it can be metabolized to a free radical, DNA-reactive species. Penclomedine was involved in phase I clinical trial in treating patients with solid tumors or lymphoma. In this trial oral penclomedine was conducted to potentially alter the toxicity profile and to avoid the neurological side effects seen with i.v. penclomedine. The more favorable toxicity profile of penclomedine was obtained. It would seem reasonable to pursue a Phase II evaluation of p.o. penclomedine in patients with intracranial neoplasms, because central nervous system penetration appears unusually good. However, information about the further development of this drug is not available.

Stibamine Glucoside is a nitrogen glucoside of p-aminophenylstibinate of sodium useful for the treatment of leishmaniasis and visceral leishmaniasis also known as kala-azar black fever Stibamine Glucoside is administered by slow i.v or deep i.m. injection. Some 80% of a dose is recov¬ered in the urine on 24 h. Elimination from the plasma is biphasic, the half-life of the initial phase being 2 h and that of the subsequent phase 76 h. In high dose car¬diac, renal or hepatic toxicity may occur. Stibamine Glucoside is no longer marketed due to safety reason.

Stirimazole is an imidazole derivative patented by Lilly Industries Ltd. as an antiparasitic agent effective against Trypanosoma congolense, T. gambiense, T. rhodesiense, and T. cruzi. Stirimazole inhibited Trichomonas vaginalis in vitro at 0.225 μg/ml and eliminated infected lesions in mice at 20 mg/kg orally. Stirimazole eliminated intestinal amebiasis in rats at 50 mg/kg orally and hepatic amebiasis in hamsters at 100 mg/kg i.p. Stirimazole was curative against Trypanosoma rhodesiense, Trypanosoma cruzi, Trypanosoma gambiense, and Trypanosoma congolense in mice at 25, 100, 12.5, and 25 mg/kg (4 times, i.p.), respectively, and against Trypanosoma vivax in calves at 25 mg/kg i.v.

Flamenol (3,5-Dihydroxyanisole) is organic compound used in synthesis of isorobustin and substituted linear and angular benzofurocoumarins

Vercirnon (GSK-1605786, CCX-282, nTraficet-EN) is a selective, and potent antagonist of human CCR9. Vercirnon binds to the intracellular side of the receptor, exerting allosteric antagonism and preventing G-protein coupling. CCR9 is a tissue-specific lymphocyte trafficking molecule that selectively attracts both B- and T-cells to the small gut. Inhibition of CCR9 by GSK-1605786 may inhibit B- and T-cell entry to the small gut and ameliorate inflammation while leaving immune function at other anatomical sites unaffected. Vercirnon is an orally bioavailable, anti-inflammatory agent that is being developed by ChemoCentryx for treatment of inflammatory bowel disease with an initial focus in Crohn's disease. A pivotal phase III programme of vercirnon was initiated in patients with moderate-to-severe Crohn's disease, however, the programme was suspended when the first pivotal trial failed to meet its primary endpoint. Phase II trials for ulcerative colitis and celiac disease were conducted, however investigations for ulcerative colitis were suspended while no further development has been reported for celiac disease.