46112-46-3Relevant articles and documents
Building addressable libraries: The use of a mass spectrometry cleavable linker for monitoring reactions on a microelectrode array
Chen, Ceng,Nagy, Gabriella,Walker, Amy V.,Maurer, Karl,McShea, Andy,Moeller, Kevin D.
, p. 16020 - 16021 (2006)
Time-of-flight secondary ion mass spectrometry (TOF SIMS) has been used in conjunction with a mass spectrometry cleavable linker to determine the percent conversion of reactions that were conducted site-selectively on an addressable microelectrode array.
Nitroxide derivative of ROCK kinase inhibitor
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, (2020/06/17)
The invention provides a small molecular compound of a NO donor. The small molecular compound is characterized in that the small molecular compound is a compound shown represented by structural formula I shown in the description, or a stereoisomer, a geometrical isomer, a tautomer, a racemate, a deuterated isotope derivative, a hydrate, a solvate, a metabolite, a pharmaceutically acceptable salt or a prodrug thereof; and in the formula I, ring A is a substituted or unsubstituted heteroaromatic ring, X is selected from (CH2)n, n is selected from 0, 1, 2 and 3, R is a substituent group of terminal -O-NO2, R is selected from hydrogen, a hydroxyl group, halogen, an amino group, a cyano group, a substituted or unsubstituted alkyl group, a substituted or unsubstituted alkoxy group, a substituted or unsubstituted alkenyl group, a substituted or unsubstituted alkynyl group and a substituted or unsubstituted heteroalkyl group, and R and R are respectively and independently selected from hydrogen, a substituted or unsubstituted alkyl group, a substituted or unsubstituted naphthenic base or an amino protecting group, or R and R are connected to form a substituted or unsubstituted cyclic heteroalkyl group. The compound has a high-activity inhibition effect on ROCK kinase.
Evaluation of N-phenyl homopiperazine analogs as potential dopamine D 3 receptor selective ligands
Li, Aixiao,Mishra, Yogesh,Malik, Maninder,Wang, Qi,Li, Shihong,Taylor, Michelle,Reichert, David E.,Luedtke, Robert R.,MacH, Robert H.
, p. 2988 - 2998 (2013/07/05)
A series of N-(2-methoxyphenyl)homopiperazine analogs was prepared and their affinities for dopamine D2, D3, and D4 receptors were measured using competitive radioligand binding assays. Several ligands exhibited high binding affinity and selectivity for the D3 dopamine receptor compared to the D2 receptor subtype. Compounds 11a, 11b, 11c, 11f, 11j and 11k had Ki values ranging from 0.7 to 3.9 nM for the D3 receptor with 30- to 170-fold selectivity for the D 3 versus D2 receptor. Calculated log P values (log P = 2.6-3.6) are within the desired range for passive transport across the blood-brain barrier. When the binding and the intrinsic efficacy of these phenylhomopiperazines was compared to those of previously published phenylpiperazine analogues, it was found that (a) affinity at D2 and D3 dopamine receptors generally decreased, (b) the D3 receptor binding selectivity (D2:D3 Ki value ratio) decreased and, (c) the intrinsic efficacy, measured using a forskolin-dependent adenylyl cyclase inhibition assay, generally increased.