Ro20-8065

Bretazenil (Ro16-6028) is an imidazopyrrolobenzodiazepine anxiolytic drug which is derived from the benzodiazepine family, and was invented in 1988. It is most closely related in structure to the GABA antagonist flumazenil, although its effects are somewhat different. It is classified as a high-potency benzodiazepine due to its high affinity binding to benzodiazepine binding sites where it acts as a partial agonist. Its profile as a partial agonist and preclinical trial data suggests that it may have a reduced adverse effect profile. In particular bretazenil has been proposed to cause a less strong development of tolerance and withdrawal syndrome. Bretazenil differs from traditional 1,4-benzodiazepines by being a partial agonist and because it binds to α₁, α₂, α₃, α₄, α₅ and α₆ subunit containing GABA_A receptor benzodiazepine receptor complexes. 1,4-benzodiazepines bind only to α₁, α₂, α₃ and α₅GABA_A benzodiazepine receptor complexes.

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.

CL-218,872 is a sedative and hypnotic drug used in scientific research. It has similar effects to sedative-hypnotic benzodiazepine drugs such as triazolam, but is structurally distinct and so is classed as a nonbenzodiazepine hypnotic.

Ro48-6791 is a drug, an imidazobenzodiazepine derivative developed by Hoffman-LaRoche in the 1990s.

Ro48-8684 is a water-soluble benzodiazepine derivative developed by Hoffman-LaRoche in the 1990s, which was designed along with Ro48-6791 as an improved replacement for midazolam, but ultimately proved to have little advantages over the parent drug and has not been introduced into clinical practice.

Triflunordazepam is a drug which is a benzodiazepine derivative with high GABA_A receptor affinity, and has anticonvulsant effects.

Pyrazolam (SH-I-04) is a benzodiazepine derivative originally developed by a team led by Leo Sternbach at Hoffman-La Roche in the 1970s. It has since been "rediscovered" and sold as a designer drug since 2012.

In pharmacology, GABA_A receptor positive allosteric modulators, also known as GABAkines or GABA_A receptor potentiators, are positive allosteric modulator (PAM) molecules that increase the activity of the GABA_A receptor protein in the vertebrate central nervous system.

Flubromazolam (JYI-73) is a triazolobenzodiazepine (TBZD), which are benzodiazepine (BZD) derivatives. Flubromazolam is reputed to be highly potent, and concerns have been raised that clonazolam and flubromazolam in particular may pose comparatively higher risks than other designer benzodiazepines, due to their ability to produce strong sedation and amnesia at oral doses of as little as 0.5 mg. Life-threatening adverse reactions have been observed at doses of only 3 mg of flubromazolam.

Desmethylflunitrazepam (also known as norflunitrazepam, Ro05-4435 and fonazepam) is a benzodiazepine that is a metabolite of flunitrazepam and has been sold online as a designer drug. It has an IC₅₀ value of 1.499 nM for the GABA_A receptor.

Irazepine 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.

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 GABA_A 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.

GL-II-73 (GL-ii-073) is a benzodiazepine derivative related in chemical structure to compounds such as midazolam and adinazolam. It is described as an α₅ preferring positive allosteric modulator of the benzodiazepine site of GABA_A receptors, with weaker activity at α₂ and α₃ and no significant affinity for the α₁ subtype. In animal tests it was found to produce effects consistent with antidepressant, anxiolytic and nootropic actions.

Fluclotizolam is a thienotriazolodiazepine derivative which was first synthesised in 1979, but was never marketed. It has subsequently been sold as a designer drug, first being definitively identified in 2017.

Ro20-8552 is a benzodiazepine derivative with sedative and anxiolytic effects, which has been sold as a designer drug.

Ro09-9212 is a thienodiazepine derivative with sedative and anxiolytic effects, which has been sold as a designer drug.

Ro07-9749 is a benzodiazepine derivative with sedative and anxiolytic effects, which has been used as an internal standard in the analysis of other benzodiazepines, and also sold as a designer drug.

Fluetizolam is a thienotriazolodiazepine derivative with potent sedative and anxiolytic effects, which has been sold as a designer drug.

Ro07-5220 (6'-Chlorodiclazepam) is a benzodiazepine derivative with sedative, anxiolytic, anticonvulsant and muscle relaxant effects, which has been sold as a designer drug.