RAC BHFF is the potent and selective GABAB receptor positive allosteric modulator that increases the potency and efficacy of GABA. Exhibits anxiolytic and anticonvulsant activity in vivo and is orally active. RAC BHFF reduces alcohol’s reinforcing properties in alcohol-preferring rats and adds further support to the hypothesis that the positive allosteric modulators of the GABAB receptor may constitute a novel class of agents with therapeutic potential for alcohol dependence.

Ro 67-4853 exhibited activity at all group I of metabotropic glutamate receptors including mGluR1 and mGluR5. It enhances the effects of (S)-DHPG in CA3 neurons. Site-directed mutagenesis revealed that valine at position 757 in transmembrane V of mGluR1 is crucial for the activity of multiple classes of allosteric mGluR1 potentiators. The discovery of selective mGluR1 enhancers opens the possibility for therapeutically relevant positive modulation of family 3 G proteincoupled receptors.

CTEP is a compound chemically derived from basimglurant and optimized for utility in rodent studies. CTEP is the first reported mGlu5 inhibitor with both, very long half-life and high oral bioavailability in rodents, classifying as useful pharmacological tool for long-term treatment. CTEP is significantly active in treatment of anxiety in rat and mouse. Chronic treatment with CTEP in a mouse model of Fragile X rescued learning and memory deficits, elevated locomotor activity and increased spine density, suggesting that this treatment may be effective in correcting multiple neurological symptoms. CTEP was able to improve various behavioral alterations induced by chronic social defeat stress.

Trolox (6-Hydroxy-2,5,7,8-tetramethylchroman-2-carboxylic acid) is a synthetic Vitamin E analog exerting antioxidant properties. Trolox is widely used for estimation of antioxidant capacity in the assay based on electron transfer reaction. Trolox-equivalent antioxidant capacity (TEAC) assay is based on the suppression of the absorbance of radical cations of 2,2′-azinobis(3-ethylbenzothiazoline 6-sulfonate) (ABTS) by antioxidants in the test sample when ABTS incubates with a peroxidase (metmyoglobin) and hydrogen peroxide.

Nutlin-3b is pharmacologically inactive enantiomer of an Mdm2 (mouse double minute 2) antagonist and apoptosis inducer nutlin-3. Nutlin-3b binds to MDM2 with 200-fold lower affinity and is 150 times less active in vitro than 3a (an active enantiomer of nutlin-3). Nutlin-3b does not show any effect on the cell cycle and proliferation and has no insignificant effect on gene expression in cancer cells. Nutlin-3b is usually used as a negative control.

1-Hydroxymidazolam (Alpha-hydroxy-midazolam) is pharmacologically active midazolam metabolite, which is, like the parent drug midazolam a neuronal depressant drug. There are numerous studies in which the statements concerning the contribution of 1-Hydroxymidazolam to the clinical actions of midazolam range from “almost equipotent” to “no major contributing factor”. In humans, Hydroxymidazolam is subject to further glucuronidation, followed by renal excretion. In humans, urinary recovery of 1-Hydroxymidazolam glucuronide accounted for 60 to 70% of an administered dose of [14C]midazolam. 1-Hydroxymidazolam and it’s glucuronide were found in patients with renal failure after administration of midazolam and may account for the prolonged sedation observed in those patients.

Ro 4-1284 is a VMAT2 inhibitor. Compond exhibits reserpine-like effect and is used as a tool compound in preclinical studies, its chronic administration lead to such symptoms as deterioration of learning, decrease in locomotion in rearing, intense hypothermia

T863, also known as DGAT-1 inhibitor, is an oral active, selective and potent DGAT1 (Acyl-CoA:diacylglycerol acyltransferase 1) inhibitor, which inhibits triacylglycerol synthesis in cells. It was shown, that treatment of obese mice lead to the reduction of triacylglycerol in serum and liver level and to improve insulin sensitivity.

Ro 5-3335, 7-chloro-5-(2-pyrryl)-3H-1,4-benzo-diazepin-2-(H)-one, is a benzodiazepine compound. Originally Ro 5-3335 was shown to inhibit gene expression controlled by the human immunodeficiency virus-1 (HIV-1) LTR promoter. The inhibition was specific for the viral transcriptional transactivator Tat. The compound did not inhibit the basal activity of the HIV-1 LTR or the activity of promoters not responsive to Tat. In addition Ro 5-3335 was able to interact with RUNX1 and CBFβ directly, repress RUNX1/CBFB-dependent transactivation in reporter assays, and repress runx1-dependent hematopoiesis in zebrafish embryos. Ro5-3335 preferentially killed human CBF leukemia cell lines, rescued preleukemic phenotype in a RUNX1-ETO transgenic zebrafish, and reduced leukemia burden in a mouse CBFB-MYH11 leukemia model.

Dicazepam (known as Ro5-3448, chlorodiazepam and 2'-chloro-diazepam) is a 2’-chloro derivative of diazepam that has emerged as a designer drug and is intended for forensic and research applications. It is metabolized in vivo into the pharmacologically active which can be detected in urine.