Curcumol is one of the major components of the essential oil of Rhizome Curcumae with the structure of sesquiterpenoid hemiketal. It exhibits characteristics such as antitumor, ant proliferation, anti-inflammatory, anti-hepatic fibrosis, antioxidant, and antimicrobial activities with low cytotoxicity. Curcumol suppresses the Breast Cancer Cells, Colorectal Cancer Cell Line, lung adenocarcinoma cell lines and others. However, its effect and mechanisms against tumor metastasis are still unclear. Recently was discovered a preliminary mechanism the suppression of breast cancer cell metastasis by curcumol. This mechanism suggested the inhibition of MMP-9 via JNK1/2 and Akt (Ser473)-dependent NF-κB signaling pathways.

PD-217014 or PD-217,014, a new GABA analog was developed by Pfizer as a potent alpha(2)delta ligand of voltage-gated calcium channel, that and possessed visceral analgesic activity. This compound was undergoing phase II clinical trials for the treatment of overactive bladder (OAB) and irritable bowel syndrome (IBS). In addition, PD-217014 was investigated for postherpetic neuralgia treatment. However, all these studies were discontinued.

Norbuprenorphine is a major metabolite of buprenorphine and potent agonist of μ, δ, and κ opioid receptors. Norbuprenorphine is the only known active metabolite of buprenorphine. It has been shown to be a respiratory depressant in rats, but only at concentrations at least 50-fold greater than those observed following application to humans of BuTrans 20 mcg/h. Compared with buprenorphine, norbuprenorphine causes minimal antinociception but greater respiratory depression. In rats, nor-buprenorphine had 1/50th the analgesic potency of buprenor-phine but 10-fold greater respiratory depressant potency. Norbuprenorphine is an in vitro substrate of the efflux transporter P-glycoprotein (Mdr1). Norbuprenorphine is an in vitro and in vivo substrate of P-glycoprotein. P-glycoprotein-mediated efflux influences brain access and antinociceptive, but not the respiratory, effects of norbuprenorphine.

Icometasone (CL09) is a synthetic glucocorticoid corticosteroid. It is a metabolite of Mometasone Furoate. The binding on human serum albumin was shown to be non saturable, suggesting that other proteins were involved in CL09 binding. This binding was demonstrated to be reversible. CL09 was extensively metabolized since no unchanged CL09 was recovered in bile or urine and at least nine metabolites have been detected. It was studied in Europe as an anti-asthmatic agent but investigation is discontinued.

PF-03635659 is a potent, very long dissociative half-life (slow off-rate, >1440 min) muscarinic M3 antagonist. Spirometry data from healthy volunteers in phase I clinical studies illustrate that PF-03635659 provides efficacious 24 h bronchodilation from a single inhaled dose, thus confirming the suitability of PF-03635659 as a novel once-daily inhaled muscarinic M3 receptor antagonist for the treatment of chronic obstructive pulmonary disease (COPD). Safety (tachycardia) and toleration (dry mouth) data from the multidose phase I studies indicate an adverse event profile that is at least noninferior to tiotropium bromide. PF-03635659 had been in phase II clinical trial for the treatment of chronic obstructive pulmonary disease.