Benzodiazepines

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.

Sulazepam is a benzodiazepine derivative. It is the thioamide derivative of diazepam. It is metabolised into diazepam, desmethyldiazepam and oxydiazepam. It has sedative, muscle relaxant, hypnotic, anticonvulsant and anxiolytic properties like those of other benzodiazepines. It was never marketed.

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

Devazepide (L-364,718, MK-329) is benzodiazepine drug, but with quite different actions from most benzodiazepines, lacking affinity for GABAA receptors and instead acting as an CCKA receptor antagonist. It increases appetite and accelerates gastric emptying, and has been suggested as a potential treatment for a variety of gastrointestinal problems including dyspepsia, gastroparesis and gastric reflux. It is also widely used in scientific research into the CCKA receptor.

QH-II-66 (QH-ii-066) is a sedative drug which is a benzodiazepine derivative. It produces some of the same effects as other benzodiazepines, but is much more selective than most other drugs of this class and so produces somewhat less sedation and ataxia than other related drugs such as diazepam and triazolam, although it still retains anticonvulsant effects.

Tuclazepam is a drug which is a benzodiazepine derivative.

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.

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.

Pivoxazepam is a drug which is a benzodiazepine derivative. It is the pivalate (2,2-dimethylpropanoate) ester of oxazepam. It has sedative and anxiolytic actions like those of other benzodiazepines. Compared to its parent drug, oxazepam, pivoxazepam is more rapidly absorbed and slightly more sedative.

Proflazepam (Ro10-3580) is a drug which is a benzodiazepine derivative.

Ro5-4864 ('''4'-chlorodiazepam') is a drug which is a benzodiazepine derivative of diazepam. However unlike most benzodiazepine derivatives, Ro5-4864 lacks affinity for GABAA receptors and lacks typical benzodiazepine effects, instead being sedative yet also convulsant and anxiogenic in effects. Ro5-4864 was found to be a potent ligand for the "peripheral benzodiazepine receptor", later renamed to mitochondrial translocator protein 18kDa (TSPO). Despite its convulsant effects, at lower doses Ro5-4864 has proved to be neuroprotective and has become widely used for research into the role of the

Irazepine (Ro 7-1986/1) is a benzodiazepine derivative containing isothiocyanate functional group. It is a non-competitive benzodiazepine binding site antagonist. Irazepine and other alkylating benzodiazepines, such as kenazepine, bind to brain benzodiazepine receptors in a non-competitive (covalent) fashion in vitro, and may exert a long-lasting anticonvulsant effect.

GYKI-52895 is a drug which is a 2,3-benzodiazepine derivative that also shares the 3,4-methylenedioxyamphetamine pharmacophore. Unlike other similar drugs, GYKI 52895 is a selective dopamine reuptake inhibitor (DRI), which appears to have an atypical mode of action compared to other DRIs. Its DRI activity is shared by numerous addictive drugs including amphetamine and its derivatives (e.g. dextromethamphetamine), cocaine, and methylphenidate and its derivatives (e.g. ethylphenidate). However, dopaminergic drugs are also prone to producing emetic effects such as in the case of apomorphine.

Difludiazepam (Ro07-4065) is a benzodiazepine derivative which is the 2',6'-difluoro derivative of fludiazepam. It was invented in the 1970s but was never marketed, and has been used as a research tool to help determine the shape and function of the GABAA receptors, at which it has an IC50 of 4.1nM. Difludiazepam has subsequently been sold as a designer drug, and was first notified to the EMCDDA by Swedish authorities in 2017.

chemical compound