Cheng, Yun-Xing published the artcileSynthesis and binding of 6,7,8,9-tetrahydro-5H-pyrido[3,4-d]azepine and related ring-opened analogs at central nicotinic receptors, Recommanded Product: 2-(Benzyl(methyl)amino)ethanol, the publication is European Journal of Medicinal Chemistry (1999), 34(2), 177-190, database is CAplus.
6,7,8,9-Tetrahydro-5H-pyrido[3,4-d]azepine (I) and its N7-Me derivative were synthesized and evaluated as potential nicotinic acetylcholinergic receptor (nAChR) ligands. On the basis that 6,7,8,9-tetrahydro-5H-pyrido[3,4-c]azepine, which binds to nAChR with low affinity (Ki = 1100 nM), possesses an inter-nitrogen distance (4.6 Å) that may be less than optimal, I was designed due to its similar shape but longer inter-nitrogen distance (5.5 Å). Compound I (Ki = 46 nM) was found to bind with enhanced affinity. However, unlike what is seen with nornicotine/nicotine, N-methylation of I reduced affinity (Ki = 268 nM) rather than enhancing it. The results suggest that the title compounds may interact at nicotine receptors in a manner that is somewhat different from that of nicotine. Ring-opening of the pyrido[3,4-d]azepine ring led to a series of 3-(2-aminoethyl)pyridines that retained the affinity of the cyclic compound Subsequent modification, including further chain lengthening (e.g. (aminopropyl)pyridine derivatives) and introduction of unsaturation, ultimately led to the development of a series of 3-(2-aminoethoxy)pyridine derivatives Simple N-substituted derivatives of 3-(2-aminoethoxy)pyridine were found to bind with Ki values of 20 to 35 nM. Because parallel structural changes in several series of related compounds did not result in parallel shifts in nAChR affinity, it is unlikely that all the investigated compounds bind in a similar fashion at these receptors. Nevertheless, some of these compounds represent novel classes of nAChR ligands.
European Journal of Medicinal Chemistry published new progress about 101-98-4. 101-98-4 belongs to alcohols-buliding-blocks, auxiliary class Amine,Benzene,Alcohol, name is 2-(Benzyl(methyl)amino)ethanol, and the molecular formula is C10H15NO, Recommanded Product: 2-(Benzyl(methyl)amino)ethanol.
Referemce:
https://en.wikipedia.org/wiki/Alcohol,
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