JZL184 is an irreversible inhibitor for monoacylglycerol lipase (MAGL), the primary enzyme responsible for degrading the endocannabinoid 2-arachidonoylglycerol (2-AG). Selectivity of JZL 184 over other serine hydrolases makes it useful compound to study endogenous 2-AG signaling. Administration of JZL184 to mice was reported to cause dramatic elevation of brain 2-AG leading to several cannabinoid-related behavioral effects. JZL184 was found effective in preclinical models of anxiety and chemotherapy-induced neuropathic pain.

A-317491 (ABT-202) is a non-nucleotide antagonist of P2X3 and P2X2/3 receptor activation. A-317491 potently blocked recombinant human and rat P2X3 and P2X2/3 receptor-mediated calcium flux (Ki = 22-92 nM) and was highly selective (IC50 >10 uM) over other P2 receptors and other neurotransmitter receptors, ion channels, and enzymes. A-317491 also blocked native P2X3 and P2X2/3 receptors in rat dorsal root ganglion neurons. Blockade of P2X3 containing channels was stereospecific because the R-enantiomer (A-317344) of A-317491 was significantly less active at P2X3 and P2X2/3 receptors. A-317491 dose-dependently (ED50 = 30 umolkg s.c.) reduced complete Freund's adjuvant-induced thermal hyperalgesia in the rat. Studies indicate that the P2X3 receptor is implicated in both neuropathic and inflammatory pain. P2X3 receptor is a promising target for therapeutic intervention in cancer patients for pain management. ABT-202 had been in phase I clinical trials by Abbott and NeuroSearch for the treatment of pain. However, this research has been discontinued.

Gelsemine is the principal alkaloid in Gelsemium sempervirens Ait. A single intrathecal injection of gelsemine produced potent and specific antinociception in formalin-induced tonic pain, bone cancer-induced mechanical allodynia, and spinal nerve ligation-induced painful neuropathy. Gelsemine exhibits potent and specific antinociception in chronic pain by acting at spinal α3 glycine receptors. Gelsemine is an effective agent for treatment of both neuropathic pain and sleep disturbance in PSNL mice; anterior cingulate cortex might play a role in the hypnotic effects of gelsemine.

Songorine is a diterpenoid alkaloid which can be isolated from the genus Aconitum. Songorin has demonstrated anti-inflammatory, anti-anxiolytic and the ability to promote wound healing. The Anti-anxiolytic properties appear to be linked to the agonistic activity of the Dopamine D2 receptor as shown in rat hippocampal slices. The wound healing effect is the result of songorine's ability to stimulate the development of mesenchymal progenitor cells, although the exact mechanism of action remains unclear.

Ginkgolide A (GA, BN52020), is a terpene lactone constituent of Ginkgo biloba, the ginkgo tree, is the oldest living tree, with a long history of use in traditional Chinese medicine. Ginkgolide A is an effective antagonist of platelet activating factor, an ubiquitous phospholipid that acts as a mediator of numerous pathophysiological conditions. Ginkgolide A displays anxiolytic, antiinflammatory properties, protects from cerebral ischemia in animal models.

(-)-Sesamin is a lignan present in sesam oil and a number of medicinal plants. It exerts various pharmacological effects, such as prevention of hyperlipidemia, hypertension, and carcinogenesis. Moreover, (-)-sesamin has chemopreventive and anticancer activity in vitro and in vivo. (-)-Sesamin is an inhibitor of human mitochondrial Lon protease and DNA damage agents to activate the DNA damage checkpoints as well induce apoptosis in NSCLC cells. (-)-Sesamin is an antioxidant, showing effective 1,1-diphenyl-2-picrylhydrazyl (DPPH) radical scavenging activity.

Poppy acid occurs in opium (Papaver somniferum) and other Papaver species. Meconic acid has been described as a mild narcotic, but it has little or no physiological action, and is not now used medicinally. Its chemical reactions are of importance in toxicology as a valuable indication of the presence of opium.

Imidazenil is an imidazo-benzodiazepine derivative with high intrinsic efficacy and selectivity for α2-, α3-, and α5- but low intrinsic efficacy for α1-containing GABA(A) receptors. It has an unusual profile of effects, producing some of the effects associated with normal benzodiazepines such as anticonvulsant and anxiolytic effects, yet without any notable sedative or amnestic effects. It has been suggested as a safe and effective treatment for anxiety, a potent yet non-sedating anticonvulsant and as a novel treatment for schizophrenia.

Myricitrin is a naturally occurring polyphenol hydroxy flavonoid. Myricitrin has a variety of beneficial properties, such as antiviral, antimicrobial, antinociceptive, and anticarcinogenic activities. In particular, myricitrin possesses stronger oxidative resistance and free radical scavenging activity than other flavonol rhamnosides or quercetin. Myricitrin showed antipsychotic-like effects in animal models at doses that did not induce catalepsy or alter locomotor activity, suggesting that myricitrin may be a potential drug treatment for the positive symptoms of schizophrenia.

CP 154526 hydrochloride is a selective, non-peptide corticotropin releasing hormone receptor 1 (CRF1) antagonist. CP 154526 readily penetrates the CNS following peripheral administration. In the clinic, CP-154,526 may have important therapeutic utility in treating depression and anxiety as well as other diseases where excessive stimulation of CRF receptors contributes to pathology. The CRF1 receptor antagonist CP-154,526 attenuated the acquisition and prevented the expression of EtOH-induced psychomotor sensitization.