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External inhibition is the observed decrease of the response of a conditioned reaction when an external (distracting) stimulus that was not part of the original conditioned response set is introduced.
Most competitive inhibitors function by binding reversibly to the active site of the enzyme. [1] As a result, many sources state that this is the defining feature of competitive inhibitors. [ 7 ] This, however, is a misleading oversimplification , as there are many possible mechanisms by which an enzyme may bind either the inhibitor or the ...
Leupeptin inhibits serine proteinases (trypsin (K i =3.5 nM), plasmin (K i = 3.4 nM), porcine kallikrein), and cysteine proteinases (papain, cathepsin B (K i = 4.1 nM), endoproteinase Lys-C). It does not inhibit α-chymotrypsin or thrombin. Leupeptin is a competitive transition state inhibitor and its inhibition may be relieved by an excess of ...
[3] Tetrahydrofolate synthesis pathway. Classes of small-molecules employed as inhibitors of dihydrofolate reductase include diaminoquinazoline and diaminopyrroloquinazoline, Most of the above specified inhibitors are structural analogues of the substrate dihydrofolate and bind to the active site of the enzyme.
IV dose 1-1.5mg/kg or 3 to 5 x ED 95. Paralysis occurs in one to two minutes. Clinical duration of action (time from drug administration to recovery of single twich to 25% of baseline) is 7-12 minutes. If IV access is unavailable, intramuscular administration 3-4mg/kg. Paralysis occurs at 4 minutes.
Reversible inhibitors produce different types of inhibition depending on whether they bind to the enzyme, the enzyme-substrate complex, or both. Enzyme inhibitors play an important role in all cells, since they are generally specific to one enzyme each and serve to control that enzyme's activity.
Uncompetitive inhibition is present within biological systems in a number of ways. In fact, it often becomes clear that the traits of inhibition specific to uncompetitive inhibitors, such as their tendency to act at their best at high concentrations of substrate, are essential to some important bodily functions operating properly. [7]
Index inducer or just inducer predictably induce metabolism via a given pathway and are commonly used in prospective clinical drug-drug interaction studies. [2]Strong, moderate, and weak inducers are drugs that decreases the AUC of sensitive index substrates of a given metabolic pathway by ≥80%, ≥50% to <80%, and ≥20% to <50%, respectively.