Meluadrine (Hoku 81) is a beta-adrenergic receptor agonist with tocolytic activity. Meluadrine binds to and activates beta-2 adrenergic receptors of myometrial smooth muscle in the uterus, thereby activates adenyl cyclase, an enzyme that catalyzes the conversion of adenosine triphosphate (ATP) to cyclic-3',5'-adenosine monophosphate (cAMP). Increased cAMP levels leads to a reduction in intracellular calcium concentration, thereby causes smooth muscle relaxation and decreases the intensity of uterine contractions. Meluadrine is a bronchodilator, and one of the metabolites of tulobuterol. Meluadrine was approximately 8 times more potent than tulobuterol, approximately twice as potent as salbutamol, and approximately as potent as isoprenaline in relaxing effect on the isolated tracheal smooth muscle preparation of guinea pigs.

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.

Belarizine was studied as a cerebral vasodilator.

ALFETAMINE (aletamine) is an antidepressant and analgesic. The pharmacologic activity profile of aletamine closely resembles that of the tricyclic antidepressants imipramine and amitriptyline. Effects shared are antagonism of RO4-1284-induced ptosis and depressed exploratory behavior, depression of spontaneous motor activity, prolongation of hexobarbital hypnosis and anticonvulsant action in mice, hypotension and potentiation of norepinephrine pressor effects in dogs, antimuricidal effects, hypothermia in rats and local anesthesia in rabbits and guinea pigs. Aletamine differed from imipramine and amitriptyline as follows: (1) aletamine exerted no apparent central or peripheral anticholinergic effect as suggested by lack of influence on tremorine-induced tremors or salivation; (2) although aletamine was less potent on a milligram basis than imipramine and amitriptyline in preventing RO4-1284 depression, aletamine was more potent than imipramine in counteracting existing reserpine depression (ptosis, depressed exploratory behavior) in mice. Amitriptyline was inactive against reserpine depression. The pharmacologic effects of aletamine differ in several respects from those of d-amphetamine. The effects of aletamine on spontaneous motor activity, hexobarbital hypnosis and body temperature in rodents and on blood pressure in dogs are in opposite direction to those of amphetamine. In further contrast to amphetamine, grouping of mice has no influence on the toxicity of aletamine. Aletamine does not appear to be an inhibitor of monoamine oxidase in vivo since it does not enhance tryptamine-induced convulsions in rats.

Veliflapon (BAY X1005, DG-031) is an enantioselective inhibitor of 5-lipoxygenase activating protein, or FLAP. There are variants in the gene encoding FLAP, and the gene encoding leukotriene A4 hydrolase (LTA4H) linked to risk of heart attack. These variants appear to confer increased risk of heart attack by increasing the production of leukotriene B4 (LTB4), a potent driver of inflammation produced in atherosclerotic plaques. deCODE licensed veliflapon (BAY X1005, DG-031) from Bayer AG, which developed it originally for the treatment of asthma.

Trospectomycin is an aminocyclitol antibiotic similar in structure to spectinomycin. The drug was originally developed by Pharmacia & Upjohn. It is a 6'-propyl analogue of spectinomycin, and lacks the aminosugars in glycosidic linkage which are thought to be responsible for the ototoxicity and nephrotoxicity associated with the aminoglycosides. The mechanism of action of trospectomycin is similar to that of its parent compound, spectinomycin: it binds to the bacterial 30S ribosome and inhibits protein synthesis. The transport mechanism for its delivery to its target site does not appear to be oxygen dependent, and this explains the in-vitro activity of trospectomycin against anaerobic organisms. Trospectomycin has activity against a broad spectrum of pathogenic organisms including Streptococcus, Haemophilus, Gardnerella, Neisseria, Peptococcus, Peptostreptococcus, Bacteroides, Mobiluncus, Chlamydia, Mycoplasma and Ureaplasma spp. Results of in-vivo testing suggest potential utility in a variety of clinical conditions including non-gonococcal urethritis, chlamydial cervicitis, gonorrhoea, pelvic inflammatory disease, pneumonia, anaerobic infections and meningitis. Trospectomycin progressed to late stage clinical trials for treatment of pelvic inflammatory disease (chlamydia) before being abandoned for commercial reasons as the third generation cephalosporins and second generation macrolides in development and use were judged superior at the time.

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.

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.