Transport of somatostatin and substance P by human P-glycoprotein

Expression in Inflammation Substance P Regulates Somatostatin

Eletriptan metabolism by human hepatic CYP450 enzymes and transport by human P-glycoprotein.

"Reaction phenotyping" studies were performed with eletriptan (ETT) to determine its propensity to interact with coadministered medications. Its ability to serve as a substrate for human P-glycoprotein (P-gp) was also investigated since a central mechanism of action has been proposed for this "triptan" class of drug. In studies with a characterized bank of human liver microsome preparations, a ...

Kassinin and substance P stimulate somatostatin release in the rat.

1. The effect of the tachykinin dodecapeptide kassinin, which has been extracted from the skin of several African frogs, on somatostatin release was examined in the rat and compared with that of the neuropeptide substance P. 2. Equimolar doses of the two peptides were injected intravenously and the animal killed at specified intervals after injection. Somatostatin was measured by a specific rad...

Substance P hydrolysis by human serum cholinesterase.

Highly purified human serum cholinesterase (EC 3.1.1.8, also known as pseudocholinesterase and butyrylcholinesterase) had peptidase activity toward substance P. Digestion of substance P was monitored by high performance liquid chromatography, which separated three product peptides. The cleavages occurred sequentially. The first peptide to appear as Arg1-Pro2. The Km for this hydrolysis was 0.3 ...

P-Glycoprotein Transport of Neurotoxic Pesticides.

P-glycoprotein (P-gp) has been associated with a number of neurodegenerative diseases, including Parkinson's disease, although the mechanisms remain unclear. Altered transport of neurotoxic pesticides has been proposed in Parkinson's disease, but it is unknown whether these pesticides are P-gp substrates. We used three in vitro transport models, stimulation of ATPase activity, xenobiotic-induce...