Electric Literature of 25021-08-3, The reaction rate of a catalyzed reaction is faster than the reaction rate of the uncatalyzed reaction at the same temperature.25021-08-3, Name is 2-(2,5-Dioxo-2,5-dihydro-1H-pyrrol-1-yl)acetic acid, molecular formula is C6H5NO4. In a Article£¬once mentioned of 25021-08-3
Design and Synthesis of Naltrexone-Derived Affinity Labels with Nonequilibrium Opioid Agonist and Antagonist Activities. Evidence for the Existence of Different mu Receptor Subtypes in Different Tissues
A series of beta-funaltrexamine (2, beta-FNA) analogues (3-14) were synthesized that contain a variety of electrophilic groups attached at the 6beta-position of the opiate.The opioid agonist and antagonist activities of these ligands were evaluated in the guinea pig ileum (GPI) and mouse vas deferens (MVD) in vitro assays.Several of the compounds behaved like beta-FNA in that they exhibited reversible agonist activity at kappa opioid receptors and irreversible antagonist activity at mu opioid receptors.The rank order of irreversible antagonism for a series of related Michael acceptors did not parallel their intrinsic chemical reactivity, confirming that the degree of covalent binding is in part dependent on the spatial disposition of the electrophilic center relative to the receptor nucleophile (secondary recognition).The maleimidoacetamide 8 behaved very differently from beta-FNA in that it exhibited considerably greater irreversible mu antagonism in MVD relative to the mu blockage in the GPI.This suggests that different proportions of mu receptor subtypes exist in the two tissues.Several of the agents tested, including some nonreactive control compounds, displayed an unusual type of persistent kappa agonist activity in the GPI.This activity, which was reversed by addition of naxolone, reappeared upon washing.Receptor models have been presented to explain this effect.A few of the reactive ligands displayed a true nonreversible kappa agonist activity, suggesting a covalent association with the receptor.Of note in this regard was the propiolamide 6, which appeared to be an irreversible mixed agonist-antagonist at kappa and mu receptors.
We¡¯ll also look at important developments in the pharmaceutical industry because understanding organic chemistry is important in understanding health, medicine, the role of 25021-08-3, and how the biochemistry of the body works.Electric Literature of 25021-08-3
Reference£º
Pyrroline – Wikipedia,
1-Pyrroline | C4H7N – PubChem