Securinine is a plant-derived alkaloid from the Securinega plant that has been used clinically as a therapeutic for primarily neurological related diseases. Securinine is well-known GABAA antagonist and recently it was found that Securinine is able to up-regulate p53 protein and to modulate the related family member p73 protein in a p53-dependent fashion, inducing p73 in the HCT116 p53(-) cells and down-regulating it in the p53(+) cells. Securinine induces G1 phase cell cycle arrest, upregulates expression of p53 and Bax, and downregulates expression of Bcl-2, PI3K, mTOR, and p70s6k in breast cancer cells and promyelocytic leukemia cells. Securinine activates p38 MAPK, enhancing monocyte antibacterial activity in vitro as well. This compound also exhibits antimicrobial activity against Alternaria, Curvularia, and Helminthosporum. Additionally, securinine decreases AChE activity and suppresses amyloid-β (Aβ)-induced glial inflammatory responses in animal models of Alzheimer’s disease, improving cognitive deficits. Securinine’s activity as a GABA antagonist, likely explains its reported clinical success in limited studies for the treatment of neurological conditions such as amyotrophic lateral sclerosis (ALS), poliomyelitis and multiple sclerosis. Securinine has not been utilized in the United States, it has been used clinically in several other countries particularly China and Russia. In China, it is considered one of the 50 fundamental Chinese herbs and is used in Chinese herbal medicine.

Enpiprazole is a heterocyclic three-ringed pyrazolylalkyl piperazine derivative. Enpiprazole has a cataleptic action very similar to that of neuroleptics, and its effect on muscle relaxation is comparable with that of diazepam. Enpiprazole exerts anxiolytic properties in animals.

Efegatran (GYKI 14766; LY 294468) is a tripeptide D-methyl-phenylalanyl-prolyl-arginal thrombin inhibitor. It was developed by IVAX for the potential treatment of thromboembolic disorders, mainly myocardial infarction. However, information about the further development is not available.

Belarizine was studied as a cerebral vasodilator.

Tasuldine is as an orally active bronchosecretolytic agent that was clinically effective in human. However, information about the further development and use of this drug is not available.

Tisocalcitate is the vitamin D derivative. Tisocalcitate ointment is currently in phase 2 clinical development for mild to moderate psoriasis. Early studies have shown that, unlike other vitamin D3 analogues, tisocalcitate does not affect calcium metabolism. Tisocalcitate ointments were tolerated well and were safe to use on healthy skin. Tisocalcitate had been in phase II clinical trial for the treatment of psoriasis. However, this development was discontinued.

Nemifitide is a peptide analog of melanocyte-inhibiting factor (MIF) that has been reported to relieve depressive symptoms in a very short period. Tetragenex (formerly Innapharma) was developing nemifitide with potential in the treatment of depression. Clinical data obtained from two pilot clinical studies, double-blind, placebo-controlled, parallel-design, in-patient and outpatient, suggested that nemifitide may have the following advantages over current therapies: rapid onset of action (3–5 d), short period of administration (5–10 doses over a 1–2 wk period), and a relatively long duration of treatment effect (3–6 months). The mechanism of action of nemifitide was investigated by evaluating its in-vitro receptor binding and in-vivo localization in the rat brain as well as its interactions with psychoprobes indicative of specific neurotransmitter pathways in acute studies in rats. The results of these studies indicate that nemifitide readily crosses the blood–brain barrier and is localized mainly in the amygdala, hippocampus and frontal cortex of the rat brain. Its in-vitro binding to several receptors including 5-HT-2A, as well as its significant interaction with d-fenfluramine in the rat, suggest the participation of the serotonergic pathway in its mode of action in a different way than that observed with SSRI antidepressants.

Adicillin (Penicillin N) is a penicillin derivative produced by Cephalosporium acremonium. Adicillin is dextrorotatory. Inactivated by penicillinase as is penicillin G, but differs from the common penicillin by its antibacterial activity and hydrophilic character. Active against Sarcina lutea, Proteus vulgaris, Salmonella typhimurium, Diplococcus pneumoniae. Shows practically no activity against B. subtilis and Staph. aureus. The toxicity is somewhat less than that of penicillin G, although penicillin N is excreted more slowly.

Chloroserpidine is deserpidine derivative with hypotensive and sedative action