Rilapine is a member of the atypical antipsychotics (also known as second-generation antipsychotics) with high affinity for the 5-HT6 receptor. This compound also has some affinity for the 5-HT1C receptor and 5-HT7 receptor (in rats).

Eclazolast (REV 2871 or CHBZ) is a non-disodium cromoglycate (DSCG)-like, antiallergic drug. Eclazolast is taken up by rat mast cells and human leukocytes in a specific and saturable manner. The compound can be hydrolyzed by a granule-associated enzyme in the mast cell to an ionic metabolite (REV 3579) whose in vitro profile is identical to that of DSCG. Eclazolast is a potent inhibitor of both immunologic and non-immunologic histamine release. It inhibits exocytosis by intracellularly affecting only direct Fc(epsilon)RI linked processes and not through inhibition of Ca2+ influx channels.

Bavisant (also known as JNJ-31001074 or BEN-2001), a highly selective, active antagonist of the human H3 receptor that was invented by Johnson & Johnson for the treatment of attention-deficit hyperactivity disorder (ADHD). However, the result of clinical trials did not display significant clinical effectiveness in the treatment of adults with ADHD. BenevolentAI has started phase II clinical trials where investigated bavisant for ameliorating the excessive daytime sleepiness in patients with Parkinson’s disease, using one of the drug side effects is dose-dependent insomnia.

Piberaline (EGYT-475) is the antidepressant drug. Piberaline antagonized the reserpine-induced dopamine depletion in the olfactory tubercle of rats. Piberaline in contrast to tricyclic antidepressants does not impair the acquisition of avoidance conditioning but rather improves it while it does not facilitate the extinction of learned behavior but considerably delays it. EGYT-2760, an active metabolite of EGYT-475, has a central serotoninomimetic action which involves 5-HT uptake-inhibition and 5-HT1 receptor agonistic effect.

Molinazone is a benzotriazinone derivative patented by chemical and pharmaceutical companies Farbenfabriken Bayer A.-G. and Bristol-Myers Co. as an analgesic and muscle relaxant

Denzimol is a new imidazole derivative with anticonvulsant properties. Denzimol suppressed electrically and chemically induced tonic seizures but did not prevent the clonic ones. Denzimol prolongs pentobarbitone sleeping times indicating that drug binds to rat liver microsomes and are potent inhibitors in the rat of mixed function monooxygense activities both in‐vitro and in‐vivo. The antiepileptic activity of the denzimol has been evaluated in patients with poorly controlled partial epilepsy by adding on the drug to the current therapy. Although denzimol increased blood concentrations of carbamazepine, correlation analysis indicated that the improvement was more likely due to intrinsic properties of denzimol. No severe side effects were reported, although several patients experienced nausea and vomiting, which caused 2 patients to drop out. The drug did not show any mutagenic activity when compared with mutagenic standards.

Dianicline binds with high affinity to the rat and human alpha4beta2 nicotinic acetylcholine receptor (nAChR) subtypes and displays selectivity for the alpha4beta2 nAChR. Electrophysiological experiments indicate that dianicline is a partial agonist at the human alpha4beta2 nAChR subtype. Pretreatment with dianicline reduces the dopamine-releasing and discriminative effects of nicotine. Dianicline shows activity in animal models of nicotine dependence at doses devoid of unwanted side effects typically observed with nicotine. Dianicline did not increase cigarette smoking abstinence rates beyond the initial phase of treatment. However, self-reported craving and nicotine withdrawal symptoms were reduced. The most common adverse event for subjects receiving dianicline was nausea. Other gastrointestinal disorders also tended to be more frequent in the dianicline group, including diarrhea.

Ciprokinen is a renin inhibitor discovered by Roche. Ciprokinen inhibited human renin in a buffer and human plasma with an IC50 of 0.07 and 0.65 nmol/L, respectively. In animal models, acute and chronic administration of ciprokinen lead to a reduction in arterial blood pressure. Development of ciprokinen was discontinued at a preclinical stage.

Lerisetron is a 5-hydroxytryptamine3 receptor antagonist. It was under development by FAES Farma for the potential treatment of emesis resulting from chemotherapy. Lerisetron specifically binds to 5-HT3 receptors, located peripherally on vagus nerve terminals and centrally in the chemoreceptor trigger zone (CTZ) of the area postrema, which may result in suppression of chemotherapy-induced nausea and vomiting. Lerisetron had been in phase III clinical trials for the treatment of emesis. However, this study was discontinued.