Conformationally constrained opioid ligands: The Dmt-Aba and Dmt-Aia versus Dmt-Tic scaffold
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منابع مشابه
Conformationally constrained opioid ligands: the Dmt-Aba and Dmt-Aia versus Dmt-Tic scaffold.
Replacement of the constrained phenylalanine analogue 1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid (Tic) in the opioid Dmt-Tic-Gly-NH-Bn scaffold by the 4-amino-1,2,4,5-tetrahydro-indolo[2,3-c]azepin-3-one (Aia) and 4-amino-1,2,4,5-tetrahydro-2-benzazepin-3-one (Aba) scaffolds has led to the discovery of novel potent mu-selective agonists (Structures 5 and 12) as well as potent and selectiv...
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Common to all DMT/OFDM systems is a large peak-to-average ratio (PAR), which can lead to low power efficiency and nonlinear distortion. Tone reservation uses unused or reserved tones to design a peak-canceling signal to lower the PAR of a transmit block. In DMT ADSL systems, the power allocated to these tones may be limited due to crosstalk issues with many users in one twisted pair bundle. Thi...
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Higher Performance A DMT modem has shown in theory and practice that it can provide higher performance than a modem based on traditional SCM. Fig. 1 and 2 compare the throughput analysis of DMT and SCM in the presence of FEXT (far end crosstalk, the most common form of noise in VDSL.) This analysis was done using the assumptions in Table 1. Margin and throughput enhancements of DMT over SCM are...
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BACKGROUND While producing good-quality analgesia, µ-opioid (MOP) receptor activation produces a number of side-effects including tolerance. Simultaneous blockade of δ-opioid (DOP) receptors has been shown to reduce tolerance to morphine. Here, we characterize a prototype bifunctional opioid H-Dmt-Tic-Gly-NH-Bzl (UFP-505). METHODS We measured receptor binding affinity in Chinese hamster ovary...
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ژورنال
عنوان ژورنال: Bioorganic & Medicinal Chemistry Letters
سال: 2009
ISSN: 0960-894X
DOI: 10.1016/j.bmcl.2008.11.051