Etoperidone, associated with several brand names, is an atypical antidepressant which was developed in the 1970s and either is no longer marketed or was never marketed. It is a phenylpiperazine related to trazodone and nefazodone in chemical structure and is a serotonin antagonist and reuptake inhibitor (SARI) similarly to them.
NMDA receptor antagonists are a class of drugs that work to antagonize, or inhibit the action of, the N-Methyl-D-aspartate receptor (NMDAR). They are commonly used as anesthetics for human and non-human animals; the state of anesthesia they induce is referred to as dissociative anesthesia.
Latrepirdine is an antihistamine drug which has been used clinically in Russia since 1983.
Arfendazam (INN) is a drug which is a benzodiazepine derivative. Arfendazam is a 1,5-benzodiazepine, with the nitrogen atoms located at positions 1 and 5 of the diazepine ring, and so is most closely related to other 1,5-benzodiazepines such as clobazam.
Pregnanolone, also known as eltanolone, is an endogenous inhibitory neurosteroid which is produced in the body from progesterone. It is closely related to allopregnanolone, which has similar properties.
Bradanicline is a drug which was being developed by Targacept that acts as a partial agonist at the α7 subtype of the neural nicotinic acetylcholine receptors. It showed cognitive enhancing effects in animal studies, and was being developed through a collaboration between Targacept and AstraZeneca as a potential treatment for schizophrenia and attention deficit disorder. Phase I clinical trials were completed successfully, and it was in phase II trials.
Capeserod (INN; development code SL65.0155) is a selective 5-HT4 receptor partial agonist with Ki = 0.6 nM and IA = 40–50% (relative to serotonin). It potently enhances cognition, learning, and memory, and also possesses antidepressant effects. Capeserod was in phase II clinical trials around 2004–2006 for the treatment of memory deficits and dementia but no new information has surfaced since and it appears to have been abandoned.
Alfatradiol, also known as 17α-estradiol and sold under the brand names Avicis, Avixis, Ell-Cranell Alpha, and Pantostin, is a weak estrogen and 5α-reductase inhibitor medication which is used topically in the treatment of pattern hair loss in men and women. It is a stereoisomer of the endogenous steroid hormone and estrogen 17β-estradiol.
Elinogrel (INN, USAN) was an experimental antiplatelet drug acting as a P2Y12 inhibitor. Similarly to ticagrelor and in contrast to clopidogrel, elinogrel was a reversible inhibitor that acted fast and short (for about 12 hours), and it was not a prodrug but pharmacologically active itself. The substance was used in form of its potassium salt, intravenously for acute treatment and orally for long-term treatment. Development was terminated in 2012.
Drug nomenclature is the systematic naming of drugs, especially pharmaceutical drugs. In the majority of circumstances, drugs have 3 types of names: chemical names, the most important of which is the IUPAC name; generic or nonproprietary names, the most important of which are international nonproprietary names (INNs); and trade names, which are brand names. Under the INN system, generic names for drugs are constructed out of affixes and stems that classify the drugs into useful categories while keeping related names distinguishable. A marketed drug might also have a company code or compound code.
Florbetapir (18F), sold under the brand name Amyvid, is a PET scanning radiopharmaceutical compound containing the radionuclide fluorine-18 that was approved for use in the United States in 2012, as a diagnostic tool for Alzheimer's disease. Florbetapir, like Pittsburgh compound B (PiB), binds to beta-amyloid, however fluorine-18 has a half-life of 109.75 minutes, in contrast to PiB's radioactive half life of 20 minutes. Wong et al. found that the longer life allowed the tracer to accumulate significantly more in the brains of people with AD, particularly in the regions known to be associated with beta-amyloid deposits.
Sufotidine (INN, USAN, codenamed AH25352) is a long-acting competitive H2 receptor antagonist which was under development as an antiulcerant by Glaxo (now GlaxoSmithKline). It was planned to be a follow-up compound to ranitidine (Zantac). When taken in doses of 600 mg twice daily it induced virtually 24-hour gastric anacidity thus closely resembling the antisecretory effect of the proton pump inhibitor omeprazole. Its development was terminated in 1989 from phase III clinical trials based on the appearance of carcinoid tumors in long-term toxicity testing in rodents.
Lanepitant (INN, code name LY303870), developed by Eli Lilly, is a drug which acts as a selective antagonist of the NK1 receptor, and was one of the first compounds developed that act at this target. It was under development as a potential analgesic drug, but despite promising results in initial animal studies, human clinical trials against migraine, arthritis and diabetic neuropathy all failed to show sufficient efficacy to support further development, with the drug being only marginally more effective than placebo and inferior to older comparison drugs such as naproxen. Failure of analgesic action was thought to be due to poor penetration of the blood–brain barrier in humans, but research has continued into potential applications in the treatment of other disorders with a peripheral site of action, such as corneal neovascularization.
Silmitasertib (INN), codenamed CX-4945, is a small-molecule inhibitor of protein kinase CK2, a constitutively active serine/threonine-specific protein kinase that is overexpressed in several types of tumors.
Lecanemab, sold under the brand name Leqembi, is a monoclonal antibody medication used for the treatment of Alzheimer's disease. Lecanemab is an amyloid beta-directed antibody. It is given via intravenous infusion. The most common side effects of lecanemab include headache, infusion-related reactions, and amyloid-related imaging abnormalities, a side effect known to occur with the class of antibodies targeting amyloid.
Flortaucipir (18F), sold under the brand name Tauvid, is a radioactive diagnostic agent indicated for use with positron emission tomography (PET) imaging to image the brain.
Huprine X is a synthetic cholinergic compound developed as a hybrid between the natural product Huperzine A and the synthetic drug tacrine. It is one of the most potent reversible inhibitors of acetylcholinesterase known, with a binding affinity of 0.026nM, as well as showing direct agonist activity at both nicotinic and muscarinic acetylcholine receptors. In animal studies it has nootropic and neuroprotective effects, and is used in research into Alzheimer's disease, and although huprine X itself has not been researched for medical use in humans, a large family of related derivatives have been developed.
