Reference of 28537-70-4, Catalysts function by providing an alternate reaction mechanism that has a lower activation energy than would be found in the absence of the catalyst. In some cases, the catalyzed mechanism may include additional steps.In a article, 28537-70-4, molcular formula is C12H12N2O4, introducing its new discovery.
A New Class of Bradykinin Antagonists: Synthesis and in Vitro Activity of Bissuccinimidoalkane Peptide Dimers
A systematic study on the dimerization of the bradykinin (BK) antagonist D-Arg0-Arg1-Pro2-Hyp3-Gly4-Phe5-Ser6-D-Phe7-Leu8-Arg9 has been performed.The first part of this study involved compounds wherein dimerization was carried out by sequentially replacing each amino acid with cysteine and cross-linking with bismaleimidohexane.The second part of this study utilized a series of bissuccinimidoalkane dimers wherein the intervening methylene chain was varied systematically from n = 2 to n = 12 while the point of dimerization was held constant at position 6.The biological activities of these dimers were then evaluated on BK-induced smooth muscle contraction in two different isolated tissue preparations: guinea pig ileum (GPI) and rat uterus (RU).Several of the dimeric BK antagonists displayed remarkable activites and long durations of action.In addition, dimerization at position 4, 7, 8, or 9 produced dimeric analogues with markedly reduced potency.Rank order of antagonist potency as a function of dimerization position is as follows: rat uterus, 6 > 5 > 0 > 2 > 1 >3 >> 4, 7, 8, 9; guinea pig ileum, 6 > 5 > 3 > 2 > 1 > 0 >> 4, 7, 8, 9.Evaluation of the linker length as represented by the number of methylene units indicated an optimal distance between the two monomeric peptides of six to eight methylene moieties.These studies also revealed that the carbon-chain length significantly affected the duration of action in vitro and resulted in partial agonism effects when n > 8.The optimum activity in vitro was achieved with dimerization at position 6 and n = 6 (designated herein as compound 25; alternatively, CP-0127).Similar effects in potency were also seen when the monomeric antagonist D-Arg0-Arg1-Pro2-Hyp3-Gly4-Phe5-Ser6-D-Phe7-Phe8-Arg9 (NPC-567) was dimerized using similar chemistry.These results suggest that the development of BK antagonists of significant therapeutic potential may be possible using a dimerization strategy that can overcome the heretofore limiting problems of potency and in vivo duration of action found with many of the BK antagonists in the literature.
The proportionality constant is the rate constant for the particular unimolecular reaction. the reaction rate is directly proportional to the concentration of the reactant. I hope my blog about 28537-70-4 is helpful to your research. Reference of 28537-70-4
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Pyrroline – Wikipedia,
1-Pyrroline | C4H7N – PubChem