Cortex fraxini, a famous Chinese herbal folk medicine, is used for the clinical treatment of hyperuricemia, arthritis, diarrhea, liver-protective. and bacillary dysentery. Fraxin, a main active component isolated from Cortex fraxini, possesses a variety of bioactivities such as anti-inflammatory, antioxidant, analgesic, antimicrobial, antiviral, immunomodulatory, anti-hyperuricemia and diuresis. And a recent study indicated that fraxin showed potent hepatoprotective effects in vitro and in vivo, presumably through reducing Oxidative Stress. Fraxin protects cells from oxidative stress.

8-Hyroxy-2-Dipropylaminotetralin Hydrobromide (8-OH-DPAT) is a chemical predominantly used in research settings. It is widely regarded as the first identified complete agonist of the 5-HT1a receptor, for which it has a Ki = 3.18 nM. 8-OH-DPAT also acts as an agonist of the 5-HT7 receptor, and as a substrate of the Sodium dependent serotonin transporter (SERT). Although it has never progressed to human clinical trials 8-OH-DPAT has been studied in animal models for a number of conditions both for its own potential and as a benchmark for other compounds.

Thioperamide is an antihistamine at H3 and H4 receptors. Thioperamide behaves as both antagonist and inverse agonist.Thioperamide is under preclinical development with Glaxo Wellcome (UK) for the treatment of short-term memory impairment. It has also demonstrated antiarrhythmic effects in preclinical trials. Active development of thioperamide appears to have been discontinued.

RO-20-1724 is a potent inhibitor of Phosphodiesterase 4 (PDE4) originally developed by Roche. It showed some promise as a potential treatment for psoriasis, but it was discontinued when it could not match the efficacy of existing treatments. RO-20-1724 was also investigated as a potential treatment for asthma and septic shock.

Salidroside (Rhodioloside) is a glucoside which was isolated in 1926 from Salix triandra L. (Salicaceae). It is thought to be one of the compounds responsible for the antidepressant and anxiolytic actions of this plant, along with rosavin. Also was investigated that salidroside may be a promising candidate for the treatment of inflammatory liver injury and promotes skeletal regeneration in cell-autonomous and cell-non-autonomous ways and might be a potential therapy for accelerating fracture healing.

JWH-210 is an analgesic chemical from the naphthoylindole family, which acts as a potent cannabinoid agonist at both the CB1 and CB2 receptors. JWH-210 is one of the most potent 4-substituted naphthoyl derivatives in the naphthoylindole series, having a higher binding affinity. The physiological and toxicological properties of this compound have not been evaluated in humans.

Nafadotride is a highly potent and competitive dopamine D3 receptor antagonist (D3DR), with efficacy against D2DR and D4DR as well. Nafadotride displayed a high affinity for dopamine D2 and D3 receptors, but a low affinity for doparnine D1 and D4. At dopamine D2 and D3 receptors, the potency was concentrated on the l-enantiomer, which was 7 and 20 times, respectively, more potent than the d-enantiomer. dl-Nafadotride, l-nafadotride and d-nafadotride were 6, 10 and 2 times, respectively, more potent at dopamine D3 than at D2 receptors. As compared to haloperidol, a D 2 receptor preferring antipsychotic, the behavioral profile of nafadotride is characterized by stimulant properties on locomotor activity of rats habituated to their environment occurring at low dosage, i.e. in the range of 1 mg/kg. In contrast, nafadotride exerts typical D 2 receptor blocking responses at much higher dosage: for instance, about 100-fold higher dosages were required to observe extrapyramidal effects like catalepsy.

Wikstromol is the enantiomer of nortrachelogenin, isolated from Trachelospermum asiaticum var. intermedium and Pinus palustris. Wikstromol exhibited acetylcholinesterase (AChE) inhibitory. It has been found to be active against P-388 lymphocytic leukemia growth implanted in mice. The reason for this is at present unclear, although it is possible that wikstromol is either metabolized to an active antileukemic agent by the host or else serves as a biological response modifier.

BRL-15572 is a 5-HT1D receptor antagonist with pKi of 7.9, also shows a considerable affinity at 5-HT1A and 5-HT2B receptors, exhibiting 60-fold selectivity over 5-HT1B receptor.

AMG-9810, is a TRPV1 (vanilloid receptor 1) antagonist which blocks all known modes of TRPV1 activation, including heat, proton, and endogenous ligand activation. TRPV1 is a membrane-bound cation channel in peripheral sensory neurons. Inhibition of this receptor has been noted to cause anti-inflammatory effects. In murine dorsal root ganglion primary neuron studies, this compound has been shown to block capsaicin-evoked depolarization and calcitonin gene-related peptide release. Screening of AMG 9810 against a panel of G protein-coupled receptors and ion channels indicated selectivity toward TRPV1. In vivo, AMG-9810 is effective at preventing capsaicin-induced eye wiping in a dose-dependent manner, and it reverses thermal and mechanical hyperalgesia in a model of inflammatory pain induced by intraplantar injection of complete Freund's adjuvant. AMG-9810 is the first cinnamide TRPV1 antagonist reported to block capsaicin-induced eye wiping behavior and reverse hyperalgesia in an animal model of inflammatory pain.