Methoxy-PEPy is a selective ligand for the Metabotropic Glutamate Subtype 5 (mGlu5) Receptor. [3H]Methoxy-PEPy is used as a radiolabel to study mGlu5 R distribution and binding with other agents.

CDPPB is a drug used in scientific research which acts as a positive allosteric modulator (PAM) selective for the metabotropic glutamate receptor subtype mGluR5 CDPPB was shown to be the first systemically available mGlu5 PAM, thus allowing for behavioral assessment in antipsychotic models, including reversal of amphetamine-induced hyperlocomotion and reversal of deficits in prepulse inhibition, both of which have translational validity in patients with schizophrenia eliciting positive symptoms and cognitive deficits in sensorimotor gating, respectively. CDPPB was shown to be efficacious in both of these models at moderate subcutaneous (s.c.) doses between 10 and 30 mg/kg. Numerous in vivo studies using CDPPB have recently surfaced which continue to add evidence and support for the potential to treat CNS disorders associated with aberrant NMDA receptor function, including the cognitive impairments and negative symptoms of schizophrenia.

SCH 546738 is a potent and non-competitive CXCR3 antagonist. It was efficacious in multiple preclinical disease models. SCH 546738 may serve as a treatment of autoimmune diseases, including rheumatoid arthritis and multiple sclerosis, and to prevent transplant rejection.

Epothilone A is a natural compound, originally discovered from the myxobacterium Sorangium cellulosum. Epothilones A, a macrolide compound, stabilizes polymerized microtubules, leading to mitotic arrest and cytotoxicity in proliferating cells. While epothilone A shows potent antineoplastic activity in vitro, these effects were not seen in preclinical in vivo models due to its poor metabolic stability and unfavorable pharmacokinetics.

J-113397 (ComB) is the first potent and selective small molecule ORL1 antagonist. Merck, in collaboration with Banyu, is developing J-113397 with potential use in the treatment of pain. Preclinical development is underway in Japan, however, no recent development has been reported. In addition to antinociceptive properties J-113397 exerts antiparkinsonian action in animal models.

MONTELUKAST, (S)- is a Montelukast impurity A. Montelukast is a leukotriene receptor antagonist (LTRA) used for the maintenance treatment of asthma and to relieve symptoms of seasonal allergies. Montelukast sodium possesses one chiral carbon center, and a racemic form of montelukast sodium contains equal amounts of the two enantiomeric forms, i.e., the S and R optical isomers. The biologically active form of montelukast sodium is the R stereoisomer. Since the biological activity of the two enantiomers can be different, it is imperative that the amount of the S stereoisomer in the commercial product be controlled to within acceptable limits. The amount of the S optical isomer of montelukast should be lower than 0.15%

L-768242 (GW-405,833) is a potent and selective partial agonist for the cannabinoid CB2 receptor with marked anti-inflammatory and anti-hyperalgesic activity in high doses. L-768242 suppresses pathological pain in preclinical models without unwanted central side effects of CB1 agonists. L-768242 dose-dependently reversed established mechanical allodynia in models of neuropathic (i.e. partial sciatic nerve ligation (PSNL) model) and inflammatory (i.e. complete Freund's adjuvant (CFA) model) pain. Despite substantial penetration to the CNS L-768242 did not produce cannabimimetic deficits below doses of 100 mg/kg i.p. Anti-allodynic efficacy of L-768242 was opioid-independent as systemic administration of naltrexone did not block the anti-hyperalgesic or antinociceptive effects of L-768242. In in vitro studies, L-768242 was reported to behave as a partial agonist at human CB2 receptors and, alternately, a potent inverse agonist at both human and rat CB2 receptors and a weak agonist at rat CB1 receptors. L-768242 was suggested to act as a non-competitive CB1 antagonist as L-768242 non-competitively antagonized CP55,940-induced adenylyl cyclase activity, ERK1/2 phosphorylation, PIP2 signaling and CB1 internalization in vitro in HEK cells transfected with CB1 and showed a complex, time-dependent effect on arrestin recruitment in CHO cells. Anti-allodynic efficacy of L-768242 is CB1-dependent but does not seem to involve engagement of the CB1 receptor’s orthosteric site.

Indinavir lactone is a product of the primary degradation pathway for indinavir, which is the primary active ingredient in the HIV anti-retroviral therapy Crixivan. Degradation of Indinavir occurs when exposed to moisture or elevated temperature.

Threo-indinavir is an epimer of indinavir, which is the primary active antiretroviral ingredient in the HIV treatment Crixivan.

L-838,417 is a subtype-selective GABAA modulator, acting as a partial agonist at alpha2, alpha3 and alpha5 subtypes and an antagonist at the alpha1 subtype. L-838,417 displays anxiolytic effects in vivo and is used as a tool compound to study roles of GABAA subunits.