3-Hydroxymethyl-beta-carboline (3-HMC) is a benzodiazepine receptor antagonist both in vitro and in vivo. It antagonizes both the anticonvulsant and “anxiolytic” actions of diazepam. 3-HMC decreases sleep and reverses the hypnotic actions of flurazepam. 3-HMC is an active antagonist of the cerebrovascular and cerebral metabolic depression produced by flurazepam and can stimulate cerebral blood flow and cerebral O2 consumption at high doses when given alone. 3-HMC has the ability to specifically antagonize fentanyl anesthesia.

Alpha-ergocryptine is a component of the ergotoxine complex; it is the main ergot alkaloid of Japanese & South American wid grasses. Alpha-ergocryptine is an agonist at the D2 dopamine receptor. Alpha-ergocryptine effectively decreases intraocular pressure in the alpha-chymotrypsin-induced model of ocular hypertension.

JDTic demonstrated high affinity for the kappa opioid receptor in the binding assay and highly potent and selective kappa antagonism in the [(35)S]GTP-gamma-S assay. This drug was in phase I of clinical trials for the treatment of cocaine abuse, but development was stopped because of incidence of non-sustained ventricular tachycardia.

P-88-8991, (-)- is a metabolite of Iloperidone. It has functional affinity for noradrenergic, dopaminergic and serotoninergic receptors. Humans produce only one enantiomer stereospecifically following administration of Iloperidone. Preclinical studies revealed that P-88-8991, (-)- might be useful for the treatment of psychotic disorders such as schizophrenia and bipolar disorders.

P-88-8991, (+)- is a metabolite of Iloperidone. It has functional affinity for noradrenergic, dopaminergic and serotoninergic receptors. Humans produce only one enantiomer stereospecifically following administration of Iloperidone. Preclinical studies revealed that P-88-8991, (+)- might be useful for the treatment of psychotic disorders such as schizophrenia and bipolar disorders.

Tribufos is an organophosphate defoliant used for cotton crops. It is specifically used to defoliate cotton in preparation for machine harvesting. Tribufos inhibits CB1 in vivo, without cholinergic poisoning signs, by 50% at 50 mg/kg intraperitoneally with a recovery half-time of 3-4 days, indicating covalent derivatization.

MK-912 is non-specific alpha-2 adrenergic receptor antagonist, with high affinity for the alpha-2-A, alpha-2B, and alpha-2C variants. Originally developed by Merk & Co, it has been investigated for potential therapeutic properties for the treatment of depression and diabetes. MK-912 is also regularly used as a molecular probe in biomedical studies seeking information about alpha-2 adrenergic receptors.

RO1138452 (also known as CAY10441) is one of the more potent high-affinity ligands and functional antagonists for the human IP (prostacyclin) receptor, it antagonizes the carbaprostacyclin-induced activation of human neuroblastoma adenylate cyclase, blocking cyclic AMP accumulation in a dose-dependent manner. RO1138452 is an orally bioavailable compound, demonstrated analgesic activity in rodents.

Saikosaponin A is a triterpene saponin found in Bupleurum that exhibits anti-inflammatory, analgesic, neuromodulatory, anticancer, and immunosuppressive activities. Saikosaponin A decreases production of TNF-α, IL-1β, and IL-2 and increases mechanical withdrawal thresholds and thermal withdrawal thresholds in animal models of chronic constructive injury. Saikosaponin A also decreases self-administration of cocaine and morphine. In colon carcinoma cells, saikosaponin A causes activation of caspases 2, 3, 8, and 9 and PARP, induces apoptosis, and decreases expression of Bcl-2 and XIAP. Additionally, this compound inhibits the proliferation and activation of ConA-treated T cells, inducing G0/G1 phase cell cycle arrest and decreasing expression of TNF-α, IL-2, and IFN-γ.

4’-Hydroxyflavanone is a flavonoid that can be found naturally in parsley, onions, berries, tea, and citrus fruits. 4-Hydroxyflavanone is an inhibitor of SREBP maturation and lipid synthesis, and 4-Hydroxyflavanone may have major potential as a pharmaceutical preparation against hepatic steatosis and dyslipidemia.