15-keto Prostaglandin F1alpha (15-keto PGF1alpha) is the initial metabolite of PGF1alpha via 15-hydroxy PGDH. In mammals, oxidation of C-15 markedly attenuates receptor binding and activity. In fish, the 15-keto compounds serve as post-ovulatory pheromones and are more active than the parent prostaglandins.Formal...

Metaxalone is a skeletal muscle relaxant. It inhibits the proliferation of, and induces apoptosis in, RAW 264.7 cells in vitro when used at concentrations ranging from 1 to 100 µM. Metaxalone also reduces LPS-induced increases in COX-1, COX-2, and NF-kB levels and inhibits LPS-induced production of TNF-alpha, IL-6,...

Ramiprilat is the active metabolite of ramipril (Cay-15558) and functions as an angiotensin-converting enzyme inhibitor (pKi = 9.08 in human heart) to suppress the conversion of angiotensin I to angiotensin II and the degradation of bradykinin, thereby preventing vasoconstriction. Furthermore, ramiprilat is reported...

The cystic fibrosis (CF) gene encodes a cAMP-regulated chloride channel, the CF transmembrane conductance regulator (CFTR). CFTR inhibitor II, also known as GlyH-101, is a glycine hydrazide that selectively and reversibly blocks the CFTR channel (Ki = 4.3 µM). This compound binds to a site at the external pore of...

Carmustine is a DNA alkylating agent. It inhibits cell growth and induces cell cycle arrest at the G2/M phase in C6 rat glioma cells when used at a concentration of 10 µM. In vivo, carmustine (0.3 and 6.7 mg/kg per day) reduces tumor growth in a C6 rat glioma model. Carmustine (0.5 mg/kg, i.p.) also reduces the...