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Arylacetamides as peripherally restricted kappa opioid receptor agonists
Analogues of the kappa (κ) opioid receptor agonist, ICI 199441, were prepared. K i values for these analogues at the cloned human κ opioid receptor ranged from 0.058 to 25 nM. Trifluoromethylaryl derivatives were potent analgesics when administered subcutaneously in the rat and were more peripherall...
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| Published in: | Bioorganic & medicinal chemistry letters 2000-11, Vol.10 (22), p.2567-2570 |
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| Main Authors: | , , , , , , , , , , |
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| Language: | English |
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| cited_by | cdi_FETCH-LOGICAL-c389t-9d5d707c20d531e7c5e8dfb4856618052edbcc389f1a9acfb3a36cc63bdc10c53 |
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| cites | cdi_FETCH-LOGICAL-c389t-9d5d707c20d531e7c5e8dfb4856618052edbcc389f1a9acfb3a36cc63bdc10c53 |
| container_end_page | 2570 |
| container_issue | 22 |
| container_start_page | 2567 |
| container_title | Bioorganic & medicinal chemistry letters |
| container_volume | 10 |
| creator | Kumar, Virendra Marella, Michael A. Cortes-Burgos, Luz Chang, An-Chih Cassel, Joel A. Daubert, Jeffrey D. DeHaven, Robert N. DeHaven-Hudkins, Diane L. Gottshall, Susan L. Mansson, Erik Maycock, Alan L. |
| description | Analogues of the kappa (κ) opioid receptor agonist, ICI 199441, were prepared.
K
i values for these analogues at the cloned human κ opioid receptor ranged from 0.058 to 25
nM. Trifluoromethylaryl derivatives were potent analgesics when administered subcutaneously in the rat and were more peripherally restricted than the parent compound, ICI 199441. |
| doi_str_mv | 10.1016/S0960-894X(00)00519-9 |
| format | article |
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| identifier | ISSN: 0960-894X |
| ispartof | Bioorganic & medicinal chemistry letters, 2000-11, Vol.10 (22), p.2567-2570 |
| issn | 0960-894X 1464-3405 |
| language | eng |
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| source | ScienceDirect Freedom Collection 2022-2024 |
| subjects | Acetamides - chemistry Acetamides - pharmacology Analgesics Analgesics, Opioid - chemistry Analgesics, Opioid - pharmacology Animals Biological and medical sciences Medical sciences Molecular Structure Neuropharmacology Pharmacology. Drug treatments Pyrrolidines - chemistry Pyrrolidines - pharmacology Rats Receptors, Opioid, kappa - agonists |
| title | Arylacetamides as peripherally restricted kappa opioid receptor agonists |
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