m-Chlorophenylpiperazine (meta-chlorophenylpiperazine or mCPP) is a psychoactive substance, which is illegal in many countries but can be found on the black market. It induces endocrine, neurological and psychiatric effects. mCPP is a partial agonist at the 5-HT2C receptor but antagonized the 5-HT2B and 5-HT3 receptors. mCPP is also an active metabolite of the drug trazodone, which is used as an effective antidepressant drug with a broad therapeutic spectrum, including anxiolytic efficacy. It is known, that mCPP induces migraine attacks and that the decrease of food intake induced by the mCPP depends on its ability to act as a serotonin agonist is a brain.

(R)-(+)-Propranolol (also known as DEXPROPRANOLOL) is the less active enantiomer of propranolol and is an antagonist of the beta-adrenergic receptor. It is known, that propranolol had been used for myocardial infarction; arrhythmia, anxiety and some other disease, but adverse effects instigated the replacement by newer drugs.

Ralimetinib (LY2228820), a trisubstituted imidazole derivative, is a potent and selective, ATP-competitive inhibitor of the α- and β-isoforms of p38 mitogen-activated protein kinase. LY2228820 produced significant tumor growth delay in multiple in vivo cancer models (melanoma, non-small cell lung cancer, ovarian, glioma, myeloma, breast). Eli Lilly is developing ralimetinib for the treatment of cancer.

Dazadrol is an antidepressant compound, developed by Schering Corp in the late 1960s. Dazadrol blocks uptake of noradrenaline and inhibits both basal and induced gastric acid secretion in the rat.

Fenobam is a selective and potent metabotropic glutamate (mGlu)5 receptor antagonist with inverse agonist activity. Fenobam was previously investigated as an anxiolytic in a number of phase II studies in the early 1980s. These studies revealed a mixed picture of anxiolytic efficacy, with double blind, placebo controlled trials variously reporting the compound as active or inactive. This discrepancy was not easily reconciled based on patient numbers, dose level, duration of treatment, or outcome measures. The positive effects seen in animal models of fragile X syndrome (FXS) treated with fenobam or other mGluR5 antagonists, the apparent lack of clinically significant adverse effects, and the potential beneficial clinical effects seen in this pilot trial support further study of the compound in adults with FXS.

Clofilium is a quaternary ammonium compound that acts as potassium channel blocker. Clofilium is a class III agent. Clofilium increases atrial and ventricular effective refractory period without changing conduction time and, despite no apparent change in premature ventricular complex frequency, it can abolish the ability to induce ventricular tachycardia by programmed stimulation and is also well tolerated.

Levonantradol is a synthetic cannabinoid analogue of delta (9)-tetrahydrocannabinol (delta(9)-THC) administered intramuscularly. It has antiemetic and anti-analgesic properties. Although its precise mechanism of action is unknown, levonantradol appears to bind and activate the cannabinoid receptors CB1 and/or CB2. Antiemetic effect of levonantradol significantly superior to chlorpromazine. However, its adverse central effects limit its utility. The main adverse events are drowsiness and dizziness. Levonantradol, administered intramuscularly to the patients suffering from postoperative pain, manifested significant analgesic efficacy. Analgesia persisted for more than 6 h with the 2.5 and 3 mg doses of levonantradol. Drowsiness was frequent but few other psychoactive effects were reported.

Medroxalol is a competitive antagonist at alpha1-adrenergic receptors and beta1-adrenergic receptors. Medroxalol also an agonist at beta2-adrenergic receptors. Medroxalol exerts antihypertensive and vasodilating effects. It was concluded that the principal action of medroxalol was to produce a fall in blood pressure by decreasing peripheral vascular resistance more than cardiac output.

Doxpicomine is the hydrochloride salt of l-3[(dimethylamino)-(m-dioxan-5-yl)methyl]pyridine, a derivative of substituted 1,3 dioxanes. Its analgesic effect appears to be mediated centrally through opiate-like receptors. Preclinical animal studies revealed analgesic activity and duration of action of the same order as that of meperidine and codeine when administered subcutaneously and of codeine but of shorter duration when administered orally. The analgesic effects were reversed by naloxone. The drug did not reduce or antagonize the analgesic effect of morphine. Drowsiness is an expected response to effective analgesics. It was the foremost side effect observed but was of short duration and minimal intensity and did not interfere with the postoperative regimen of coughing, deep breathing, and early ambulation. Nausea and vomiting were not reported after doxpicomine.

Vinzolidine (also known as LY104208), a semisynthetic vinblastine derivative that was developed as an antitumor agent. Vinzolidine participated in clinical trials phase II in the oral formulation in patients with lymphoma, particularly Hodgkin's disease. In addition, it was studied in patients with Kaposi's sarcoma, non-small cell lung cancer, colorectal cancer, and breast cancer. It was found significant side effects included neurotoxicity and dose-related myelosuppression. As a result, was suggested intravenous route of administration for vinzolidine could be more safely. However, the phase I trial of intravenous vinzolidine was shown no antitumor activity. The further development of this drug was discontinued.