BRL-50481 is a selective inhibitor of phosphodiesterase 7 (PDE 7) that has acceptable selectivity for in vitro studies. Studies suggest that BRL-50481 is used to inhibit the activity of hrPDE7A1 which is usually expressed in baculovirus-infected Spodoptera frugiperda in a competitive manner. In osteoblasts, BRL-50481increases mineralization and bALP as a result of PDE7 silencing which upregulates several osteogenic genes. Further studies show that BRL-50481increases apoptosis in CLL cells via a mitochondrial-dependent process, and is associated with increased cAMP accumulation and down-regulation of the antiapoptotic protein survivin. BRL-50481 is a inhibitor of PDE7A.

LY-320135 is a substituted benzofuran which is structurally distinct from the aminoalkylindole and pyrazole type cannabinoid antagonists, AM630 and SR141716A, respectively. LY-320135 is a potent and selective canniboid CB1 receptor antagonist/inverse agonist. LY-320135 is selective (~70 fold) over canniboid CB2 receptors. LY-320135 is widely used in research, particularly for elucidating the mechanisms by which many CB1 antagonists act as inverse agonists at higher doses. LY-320135 shows weak binding to both 5-HT2 (Ki = 6.4 uM) and muscarinic receptors (Ki = 2.1 uM).

N-Ethyl-3-piperidyl benzilate (JB-318) is an anticholinergic drug. It is a potent hallucinogenic agent. JB-318 is a psychotomimetic, it has an antitremor action in patients with Parkinson disease.

Friedelin is a natural compound with promising proprieties. On its own or with chemical modification it is possible to introduce relevant biological activities, e.g. anti-cancer, anti-aging and agrochemical. Its availability in significant amounts has been a major drawback on its regular use and in the pursuit of different applications. Cork and cork-derived materials (e.g. black condensate) are the most relevant sources of Friedelin in nature (up to 10% in concentration). Friedelin has being shown to possess marked antioxidant and liver protective effects. Friedelin has also being demonstrated to possess potent anti-inflammatory, analgesic and antipyretic activities.

SCH-58261 is an antagonist of the Adenosine A2A receptor with a Kd of 2.3 nM. It was initially identified and developed by Schering-Plough as a potential treatment for neurological conditions such as Parkinson's Disease and Depression. However, the compound suffered from poor solubility and is not active when orally dosed. SCH-58261 became the scaffold for the development of Preladenant (SCH 412348), which did progress to Phase III clinical trials before being discontinued. There has also been an investigation of SCH-58261 as a treatment of hypotension in rat models.

DL-Tetrahydropalmatine (dl-THP), an active component isolated from Corydalis species (a Chinese herbal medicine). dl-THP has inhibitory effects on liver injury induced by carbon tetrachloride in mice. The drug demonstrated anxiolytic and anti-nociceptive effects in animal models. dl-THP may act through inhibition of amygdaloid dopamine release to inhibit an epileptic attack – it is a very effective anti-epileptogenic and anticonvulsant agent. dl-THP has been found to have antihypertensive effects. It acts through the 5-HT2 and/or D2-receptor antagonism in the hypothalamus to induce hypotension and bradycardia in rats.

Scutellarin is the main bioactive component of Breviscapine prepared from the traditional Chinese herb Erilgeron breviscapus (Vant) Hand-Mazz. Scutellarin demonstrated protective effect on cardiovascular and cerebrovascular ischemia. The potential cytoprotective effects of the drug against cerebrovascular ischemia were evidenced by reducing cerebral infarct sizes, ameliorating neurological deficit and inhibiting neuronal apoptosis. Scutellarin is capable of inhibiting I(Na) in neurons through predominantly affecting the inactivated state of I(Na). Scutellarin may alleviate cognitive impairment in a mouse model of hypoxia by promoting proliferation and neuronal differentiation of neural stem cells. Scutellarin might play an therapeutic role by inhibiting oxidative stress and apoptosis in Alzheimer's disease treatment.

CP-465022 is a potent, and selective noncompetitive AMPA receptor antagonist. It provides neuroprotective efficacy after cerebral ischemia on the basis of the activity in experimental ischemia models. CP-465022 inhibits AMPA receptor-mediated whole cell currents in rat cortical neurons in primary culture with an IC50 value of 30 nM but only weakly inhibits NMDA, g-aminobutyric acid, or kainate receptor-mediated currents. CP-465022 binds to the AMPA receptor with high affinity (IC50 = 36 nM) and displays potent anticonvulsant activity. The compound does not discriminate among AMPA receptors composed of different homomeric or heteromeric subunit combinations. Furthermore, CP-465022 inhibits AMPA receptor activity in a noncompetitive manner that is neither voltage- nor use-dependent. When administered to rodents systemically, CP-465022 inhibits AMPA receptor-mediated synaptic transmission and chemically induced seizures.

Tetrahydrodeoxycorticosterone (THDOC) is a neuroactive steroid. Neurosteroids represent a class of endogenous steroids that are synthesized in the brain, the adrenals, and the gonads. It potentiates synaptic GABAA-receptor function. THDOC is extremely potent positive allosteric modulators of GABAA receptors with sedative, anxiolytic, and anticonvulsant properties. THDOC can regulate gene expression via the progesterone receptor. The induction of DNA-binding and transcriptional activation of the progesterone receptor requires intracellular oxidation of the neurosteroids into progesterone receptor-active 5 alpha-pregnane steroid. THDOC is involved in the pathophysiology of premenstrual syndrome, catamenial epilepsy, major depression, and stress-sensitive brain disorders.

DBO-83 is a 3,8-diazabicyclo[3.2.1]octane derivative with antinociceptive properties. DBO-83 exhibits high affinity for the α4β2 subtype and is a full agonist at α4β2 and ganglionic receptors but lacks appreciable activity at neuromuscular receptors. DBO-83 exhibits antinociceptive activity in both rat and mouse models of acute and persistent pain. In addition DBO-83 modulates memory functions in rodents.