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Mivacurium for example has a molecular length of 3.6 nm when stretched out, far from the 2 to 2.1 nm optimum. Mivacurium, atracurium, and doxacurium have greater N-N distance and molecular length than d-tubocurarine even when bent. To make them fit, they have flexible connections that give their onium heads a chance to position themselves ...
These chemicals inhibit the action of DAT and, to a lesser extent, the other monoamine transporters, but their effects are mediated by separate mechanisms. Monoamine transporters are established targets for many pharmacological agents that affect brain function, including the psychostimulants cocaine and amphetamine .
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 ...
[4] The term "anticholinergic" is typically used to refer to antimuscarinics that competitively inhibit the binding of ACh to muscarinic acetylcholine receptors; such agents do not antagonize the binding at nicotinic acetylcholine receptors at the neuromuscular junction, although the term is sometimes used to refer to agents that do so. [3] [5]
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.
A protein kinase inhibitor (PKI) is a type of enzyme inhibitor that blocks the action of one or more protein kinases. [1] Protein kinases are enzymes that phosphorylate (add a phosphate, or PO 4, group) to a protein and can modulate its function. [2] The phosphate groups are usually added to serine, threonine, or tyrosine amino acids on the ...
The 5α-epimers exhibit much greater binding properties then their 5β counterparts, as can be seen with compounds 3/4 and 5/6 in table 1. These results indicate the importance of a correct angle between the A and B-ring junction for better binding to the active site of aromatase.
Untransformed human cells exhibit normal cellular behavior and mediate their growth and proliferation via interplay between environmental nutrients, growth factor signaling, and cell density. As cell density increases and the culture becomes confluent, they initiate cell cycle arrest and downregulate proliferation and mitogen signaling pathways ...