Lactams

Flutazolam (Coreminal, MS-4101) is a drug which is a benzodiazepine derivative. It was invented in Japan, and this is the main country in which it has been used medically. It has sedative, muscle relaxant, anticonvulsant, and anxiolytic effects similar to those produced by other benzodiazepine derivatives, and though it is around the same potency as diazepam, it produces a more marked sedation and impaired coordination. It is indicated for the treatment of insomnia. Its major active metabolite is n-desalkylflurazepam, also known as norflurazepam, which is also a principal metabolite of fluraze

chemical compound

K252a is an alkaloid isolated from Nocardiopsis bacteria. This staurosporine analog is a highly potent cell permeable inhibitor of CaM kinase and phosphorylase kinase (IC50 = 1.8 and 1.7 nmol/L, respectively). At higher concentrations it is also an efficient inhibitor of serine/threonine protein kinases (IC50 of 10 to 30 nmol/L).

Lorlatinib, sold under the brand name Lorbrena in the United States, Canada, and Japan, and Lorviqua in the European Union, is an anti-cancer medication used for the treatment of non-small cell lung cancer. It is an orally administered inhibitor of anaplastic lymphoma kinase (ALK) and C-ros oncogene 1 (ROS1), two enzymes that play a role in the development of cancer. It was developed by Pfizer.

Dibenzepin, sold under the brand name Noveril among others, is a tricyclic antidepressant (TCA) used widely throughout Europe for the treatment of depression. It has similar efficacy and effects relative to other TCAs like imipramine but with fewer side effects.

Flutoprazepam (Restas) is a drug which is a benzodiazepine. It was patented in Japan by Sumitomo in 1972 and its medical use remains mostly confined to that country. Its muscle relaxant properties are approximately equivalent to those of diazepam - however, it has more powerful sedative, hypnotic, anxiolytic and anticonvulsant effects and is around four times more potent by weight compared to diazepam. It is longer acting than diazepam due to its long-acting active metabolites, which contribute significantly to its effects. Its principal active metabolite is n-desalkylflurazepam, also known as

Elfazepam is a drug which is a benzodiazepine derivative. Presumably it has sedative and anxiolytic actions like those of other benzodiazepines.

Vinburnine (or eburnamonine, Vincamone) is a vasodilator. Vincamone is a vinca alkaloid and a metabolite of vincamine.

Zomebazam produced by Hoechst is a pyrazolodiazepinone derivative drug with anxiolytic properties. It is structurally related to razobazam and zometapine.

Dimiracetam is a nootropic drug of the racetam family, derivatives of which may have application in the treatment of neuropathic pain.

The drug udenafil is marketed under the trade name Zydena. It is within the PDE5 inhibitor class (which also includes avanafil, sildenafil, tadalafil, and vardenafil). Like other PDE5 inhibitors, it is used to treat erectile dysfunction. Udenafil was developed by Dong-A Pharmaceutical. It has fairly rapid onset of action (peak plasma concentration after 1 to 1.5 hours), and has long duration of action (plasma half-life of 11 to 13 hours). Udenafil's pharmacokinetics allows once-daily dosage (in addition to on-demand use). Typical doses are 100 and 200 mg. Udenafil is available in Korea, R

Merocyanines are a class of polymethine dyes which are clearly defined by set structural properties. Merocyanines belong to the group of dyes referred to as functional dyes, where their applications are not only determined by their colour, but also their valuable chemical properties.

CNQX or cyanquixaline (6-cyano-7-nitroquinoxaline-2,3-dione) is a competitive AMPA/kainate receptor antagonist. Its chemical formula is C9H4N4O4. CNQX is often used in the retina to block the responses of OFF-bipolar cells for electrophysiology recordings.

Alnespirone (S-20,499) is a selective 5-HT1A receptor full agonist of the azapirone chemical class. It produces antidepressant, anxiolytic, and antiaggressive effects.

Riamilovir, sold under the brand name Triazavirin, is a broad-spectrum antiviral drug developed in Russia through a joint effort of Ural Federal University, Russian Academy of Sciences, Ural Center for Biopharma Technologies and Medsintez Pharmaceutical. It has a novel triazolotriazine core, which represents a new structural class of non-nucleoside antiviral drugs.

Mexazolam (marketed under the trade names Melex and Sedoxil) is a drug which is a benzodiazepine derivative. Mexazolam has been trialed for anxiety and was found to be effective in alleviating anxiety at one week follow-up. Mexazolam is metabolised via the CYP3A4 pathway. HMG-CoA reductase inhibitors including simvastatin, simvastatin acid, lovastatin, fluvastatin, atorvastatin and cerivastatin inhibit the metabolism of mexazolam, but not the HMG-CoA reductase inhibitor pravastatin. Its principal active metabolites are chlorodesmethyldiazepam (also known as chloronordiazepam or delorazepam, tr

Dihydroergocristine is an ergot alkaloid. Alongside dihydroergocornine and dihydroergocryptine, it is one of the components of ergoloid mesylates.

Etozolin (also known as Diulozin, Elkapin, or Etopinil) is a loop diuretic used in Europe. It is believed to be discontinued.

Oxyphenisatine (or oxyphenisatin) is a laxative. It is closely related to bisacodyl, sodium picosulfate, and phenolphthalein. Long-term use is associated with liver damage, and as a result, it was withdrawn in most countries in the early 1970s. The acetate derivative oxyphenisatine acetate was also once used as a laxative.

Vargulin, also called Cypridinid luciferin, Cypridina luciferin, or Vargula luciferin, is the luciferin found in the ostracod Cypridina hilgendorfii, also named Vargula hilgendorfii. These bottom dwelling ostracods emit a light stream into water when disturbed presumably to deter predation. Vargulin is also used by the midshipman fish, Porichthys.

Exatecan is a drug which is a structural analog of camptothecin with antineoplastic activity.

chemical compound

Herbimycin is a benzoquinone ansamycin antibiotic that binds to Hsp90 (Heat Shock Protein 90) and alters its function. Hsp90 client proteins play important roles in the regulation of the cell cycle, cell growth, cell survival, apoptosis, angiogenesis and oncogenesis.

Pidotimod is an immunostimulant.

Sepiapterin, sold under the brand name Sephience, is a medication used for the treatment of hyperphenylalaninemia. Sepiapterin is a phenylalanine hydroxylase activator. It is also metabolite that is naturally synthesized in the human body.

Telenzepine is a thienobenzodiazepine acting as selective M1 antimuscarinic. It is used in the treatment of peptic ulcers. Telenzepine is atropisomeric, in other words the molecule has a stereogenic C–N-axis. In neutral aqueous solution it displays a half-life for racemization of the order of 1000 years. The enantiomers have been resolved. The activity is related to the (+)-isomer which is about 500-fold more active than the (–)-isomer at muscarinic receptors in the rat cerebral cortex.

2-Oxoquazepam (Sch 15725) is a benzodiazepine derivative and one of the major active metabolites of quazepam (Doral).

Azasetron is an antiemetic which acts as a 5-HT3 receptor antagonist, pKi = 9.27 It is used in the management of nausea and vomiting induced by cancer chemotherapy (such as cisplatin chemotherapy). Azasetron hydrochloride is given in a usual dose of 10 mg once daily by mouth or intravenously. It is approved for marketing in Japan, and marketed exclusively by Torii Pharmaceutical Co., Ltd. under the trade names "Serotone I.V. Injection 10 mg" and "Serotone Tablets 10 mg". Pharmacokinetics data from S. Tsukagoshi.

DIMBOA (2,4-dihydroxy-7-methoxy-1,4-benzoxazin-3-one) is a naturally occurring hydroxamic acid, a benzoxazinoid. DIMBOA is a powerful antibiotic present in maize, wheat, rye, and related grasses,

Flutemazepam was initially first synthesized in 1965, but was not further described until a team at Stabilimenti Chimici Farmaceutici Riuniti SpA in the mid-1970s. It is a short-acting (9–25 hr elimination half-life) fluorinated analogue of temazepam that has powerful hypnotic, sedative, amnesiac, anxiolytic, anticonvulsant and skeletal muscle relaxant properties. Flutemazepam has been shown to have similar pharmacological properties to temazepam, but with more powerful sedative-hypnotic and anxiolytic properties. It has been found to be effective for the treatment of the most severe states of

Tanespimycin ('17-N-allylamino-17-demethoxygeldanamycin, 17-AAG') is a derivative of the antibiotic geldanamycin that is being studied in the treatment of cancer, specifically in younger patients with certain types of leukemia or solid tumors, especially kidney tumors.

Premazepam is a drug in the pyrrolodiazepine class. It is a partial agonist of benzodiazepine receptors and was shown in 1984 to possess both anxiolytic and sedative properties in humans but was never marketed.

Motrazepam (Ro06-9098) is a drug which is a benzodiazepine derivative.

Pyrithyldione (Presidon, Persedon) is a psychoactive drug invented in 1949. An improved method of manufacture was patented by Roche in 1959. It was used as a hypnotic or sedative and presumed to be less toxic than barbiturates. Today, this substance is no longer used. Agranulocytosis was sometimes reported as adverse effect. Pyrithyldione is also a CYP2D6 inducer but is not as potent as glutethimide. In studies, it increased the O-demethylation of codeine by 20%.

Evodiamine is a chemical compound extracted from the plant genus Tetradium, which has been shown to reduce fat uptake in mouse studies. It is suspected that its mechanism of action is similar to that of capsaicin. As such, it has been included in some dietary supplements. Neither its fat-burning effects in humans nor any potential side effects have been empirically established.

Nortetrazepam is a drug which is a benzodiazepine derivative. It is one of the major metabolites of tetrazepam.

Triflunordazepam (also known as Ro5-2904) is a drug which is a benzodiazepine derivative with high GABAA receptor affinity, and has anticonvulsant effects.

chemical compound

chemical compound, pesticide synergist

Ergovaline is an ergopeptine and one of the ergot alkaloids. It is usually found in endophyte-infected species of grass like Tall fescue or Perennial Ryegrass. It is toxic to cattle feeding on infected grass, probably because it acts as a vasoconstrictor.

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.

SCH-48461 is a cholesterol absorption inhibitor.

Indobufen is a platelet aggregation inhibitor. It acts as a reversible cyclooxygenase inhibitor.

Fenobam is an imidazole derivative developed by McNeil Laboratories in the late 1970s as a novel anxiolytic drug with an at-the-time-unidentified molecular target in the brain. Subsequently, it was determined that fenobam acts as a potent and selective negative allosteric modulator of the metabotropic glutamate receptor subtype mGluR5, and it has been used as a lead compound for the development of a range of newer mGluR5 antagonists.

Fosazepam is a drug belonging to the benzodiazepine class, which are primarily anti-anxiety and sedative-hypnotic agents. It is a water soluble derivative of diazepam which has been substituted with a dimethylphosphoryl group to improve solubility in water. At equipotent doses (100 mg fosazepam and 10 mg diazepam), it possesses sedative and anxiolytic properties that are qualitatively and quantitatively similar to the effects of diazepam, with equal sedative-hypnotic, anti-convulsive, and muscle relaxant effects. In comparison to an equipotent dose of nitrazepam (100 mg fosazepa

Albaconazole (development code UR-9825) is an experimental triazole antifungal. It has potential broad-spectrum activity. The drug blocks a number of CYP450 liver enzymes.

Telcagepant (INN; development code MK-0974) is a calcitonin gene-related peptide receptor antagonist which was an investigational drug for the acute treatment and prevention of migraine, developed by Merck & Co.

Pagoclone is an anxiolytic agent from the cyclopyrrolone family, related to better-known drugs such as the sleeping medication zopiclone. It was synthesized by a French team working for Rhone-Poulenc & Rorer S.A. Pagoclone belongs to the class of nonbenzodiazepines, which have similar effects to the older benzodiazepine group, but with quite different chemical structures. It was never commercialised.

Nitrazepate (Lorzem) is a drug which is a benzodiazepine derivative and has anxiolytic properties. It is normally produced as its potassium salt, potassium nitrazepate.

Mosapramine (Cremin) is an atypical antipsychotic used in Japan for the treatment of schizophrenia. It is a potent dopamine antagonist with high affinity to the D2, D3, and D4 receptors, and with moderate affinity for the 5-HT2 receptors.

Ergoloid mesylates (USAN), co-dergocrine mesilate (BAN) or dihydroergotoxine mesylate, trade name Hydergine, is a mixture of the methanesulfonate salts of three dihydrogenated ergot alkaloids (dihydroergocristine, dihydroergocornine, and alpha- and beta-dihydroergocryptine).

Triflubazam is a drug which is a 1,5-benzodiazepine derivative, related to clobazam. It has sedative and anxiolytic effects, with a long half-life and duration of action.

Indirubin is a chemical compound most often produced as a byproduct of bacterial metabolism. For instance, it is one of the compounds responsible for the generally benign condition purple urine bag syndrome, resulting from bacteria metabolizing indoxyl sulfate found naturally in urine.

Iclazepam (Clazepam) is a drug which is a benzodiazepine derivative. It has sedative and anxiolytic effects similar to those produced by other benzodiazepine derivatives, and is around the same potency as chlordiazepoxide.

Binospirone (MDL-73,005-EF) is a drug which acts as a partial agonist at 5-HT1A somatodendritic autoreceptors but as an antagonist at postsynaptic 5-HT1A receptors. It has anxiolytic effects.

Talastine (trade name Ahanon) is an antihistamine.

Ritanserin, also known by its developmental code name R-55667, is a serotonin receptor antagonist which was under development for the treatment of anxiety disorders and major depressive disorder but was never marketed. It was also investigated for treatment of insomnia, especially to enhance sleep quality by significantly increasing slow wave sleep by virtue of potent and concomitant serotonin 5-HT2A and 5-HT2C receptor antagonism. The drug is taken orally.

Dihydroergocornine is an ergot alkaloid. Alongside dihydroergocristine and dihydroergocryptine, it is one of the three components of ergoloid.

Clazolam (SAH-1123), also referred to as isoquinazepon, is a drug which is a fused benzodiazepine and tetrahydroisoquinoline derivative. It was developed in the 1960s but was never marketed. It possesses anxiolytic effects and is also claimed to have antidepressant properties.

Lofendazam is an organic molecule which is a benzodiazepine derivative. Lofendazam is a 1,5-benzodiazepine, with the nitrogen atoms located at positions 1 and 5 of the diazepine ring; therefore, lofendazam is most closely related to other 1,5-benzodiazepines such as clobazam.