16036-79-6Relevant articles and documents
Influence of chain length and N-alkylation on the selective serotonin receptor ligand 9-(aminomethyl)-9,10-dihydroanthracene
Runyon, Scott P.,Savage, Jason E.,Taroua, Mohamed,Roth, Bryan L.,Glennon, Richard A.,Westkaemper, Richard B.
, p. 655 - 658 (2001)
Comparison of the serotonin 5-HT2A receptor affinities of chain lengthened and N-alkylated analogues of the novel ligand 9-aminomethyl-9.10-dihydroanthracene (AMDA) and a structurally similar prototypical tricyclic amine imipramine suggests that the two agents bind to the receptor in different fashions. The demonstration that AMDA is highly selective for serotonin receptors (5-HT2A, Ki = 20 nM: 5-HT2C, Ki = 43 nM) versus the dopamine D2 receptor (Ki > 10,000 nM). as well as the serotonin and norepinephrine transporters (Ki >10.000nM) further suggests that AMDA and the nonselective ligand imipramine interact with these target macromolecules in different ways.
OLIGOMER-TRICYCLIC CONJUGATES
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Paragraph 0280 - 0282, (2016/10/10)
The invention provides small molecule drugs that are chemically modified by covalent attachment of a water soluble oligomer. A conjugate of the invention, when administered by any of a number of administration routes, exhibits characteristics that are different from the characteristics of the small molecule drug not attached to the water soluble oligomer.
Synthesis and pharmacological characterization of novel inverse agonists acting on the viral-encoded chemokine receptor US28
Hulshof, Janneke W.,Vischer, Henry F.,Verheij, Mark H.P.,Fratantoni, Silvina A.,Smit, Martine J.,de Esch, Iwan J.P.,Leurs, Rob
, p. 7213 - 7230 (2007/10/03)
G-protein coupled receptors encoded by viruses represent an unexplored class of potential drug targets. In this study, we describe the synthesis and pharmacological characterization of the first class of inverse agonists acting on the HCMV-encoded receptor US28. It is shown that replacement of the 4-hydroxy group of lead compound 1 with a methylamine group results in a significant 6-fold increase in affinity. Interestingly, increasing the rigidity of the spacer by the introduction of a double bond also leads to a significant increase in binding affinity compared to 1. These novel inverse agonists serve as valuable tools to elucidate the role of constitutive signaling in the pathogenesis of viral infection and may have therapeutic potential as leads for new antiviral drugs.
