Aromatic analogs of arcaine inhibit MK-801 binding to the NMDA receptor
摘要:
Aromatic analogs of arcaine were shown to have inhibitory effects on the binding of the channel blocking drug [H-3]MK-801 to the NMDA receptor complex. The most potent compound of the series was an N,N'-bis(propyl)guanidinium which inhibited [H-3]MK-801 binding with an IC50 of 0.58 mu M and an IC50 of 12.17 mu M upon addition of 100 mu M spermidine. The increase in IC50 upon addition of spermidine suggests competitive antagonism between the inhibitor and spermidine at the arcaine-sensitive polyamine site of the NMDA receptor complex. (C) 1998 Published by Elsevier Science Ltd. All rights reserved.
The present invention relates to detecting cleavage activity of an enzyme. The various aspects of the invention include an enzyme detection device, kit, method and use for detecting or measuring the presence in a test sample of the activity of an enzyme capable of cleaving a substrate. The invention also relates to indicator and binding molecules useful for carrying out the invention. The enzyme substrate contains a hidden binding site which is only revealed upon cleavage by the enzyme.
Methods for monitoring inflammation status of a subject comprise determining levels of at least one neutrophil activation marker, or at least three markers, in urine samples taken from the subject at multiple time points, wherein increased levels of the at least one neutrophil activation marker, or at least one of the markers, in a urine sample are indicative of or predictive of an exacerbation of inflammation and/or wherein decreased levels of the at least one neutrophil activation marker, or at least one of the markers, in a urine sample following an increase are indicative or predictive of recovery from, or successful treatment of, an exacerbation of inflammation. Corresponding systems, test kits and computer programs are provided.