Related Products of 473257-60-2, The reaction rate of a catalyzed reaction is faster than the reaction rate of the uncatalyzed reaction at the same temperature.473257-60-2, Name is Ethyl 5-chloro-6-fluoro-1H-indole-2-carboxylate, molecular formula is C11H9ClFNO2. In a Article，once mentioned of 473257-60-2
The non-P1 and non-P2 muscle relaxant effect of ATP in rabbit thoracic aorta has recently been attributed to a putative P3 purinoceptor, which is activated by either adenosine or ATP. Since the physiological roles of this putative P3 purinoceptor and of a new [3H]-5?-N-ethylcarboxamidoadenosine (NECA)-binding protein from rat brain membranes called P3 purinoceptor-like protein (P3LP), due to its ligand specificity, have not been fully elucidated, we needed a specific ligand to obtain further information about the receptor. We examined the structure-activity relationship (SAR) of various 5?-N-substituted-carboxamidoadenosine derivatives toward P3LP and discovered a hydrophobic binding region near the 5?-N-substituted-carboxamide group. From the linear alkyl N-substituted derivatives, the N-n-pentyl derivative 10 was found to be the most potent ligand with a Ki value of 12 nM. In the series of the N-cycloalkyl derivatives, the N-cyclohexyl derivative 27 was the strongest ligand with a Ki value of 18 nM. On the other hand, the N-substituents having branched alkyl side chains and bulky cycloalkyl groups did not show any potent affinities for P3LP. Therefore, the hydrophobic pocket accommodates approximately a 10-carbon-atom-long linear alkyl side chain, while a considerably stronger hydrophobic binding region of about a 5-carbon-atom-long depth exists near the nitrogen atom of the amide group. This pocket also allows substitution with bulky hydrophobic groups since the 5?-N-cycloalkyl derivatives have high affinities. We also examined the receptor selectivity for the selected nucleosides 10 and 27 with 1 [9-(6,7-dideoxy-beta-D-allohept-5-ynofuranosyl)adenine, HAK2701] and NECA versus P1 purinoceptor subtypes, such as adenosine A1, A2A, A2B, and A3 receptors, and found that 27 is the most selective ligand for P3LP.
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Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles