Design and synthesis of potential dual NK1/NK3 receptor antagonists |
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| Institution: | 1. Plasma Physics Division, U.S. Naval Research Laboratory, Washington, DC 20375, United States;2. Electronics Science and Technology Division, U.S. Naval Research Laboratory, Washington, DC 20375, United States;3. Materials and Sensors Branch, U.S. Naval Research Laboratory, Washington, DC 20375, United States;4. School of Electrical and Electronic Engineering, Merz Court, Newcastle University, Newcastle upon Tyne NE1 7RU, United Kingdom;5. Department of Electrical Engineering, George Mason University, VA 22030, United States;6. Department of Material Science and Engineering, University of Maryland, MD 20742, United States |
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| Abstract: | The tachykinin NK1 and NK3 receptors are a novel drug target for schizophrenia in order to treat not only the positive and cognitive symptoms, but also the associated co-morbid depression and sleep disturbances associated with the disease. A novel class of peptidomimetic derivatives based on a versatile phenylglycine central core was synthesized and tested in vitro as dual NK1/NK3 receptor antagonists. From this series emerged compounds with good NK1 receptor affinity, although only modest dual NK1/NK3 receptor affinity was observed with one of these analogs. |
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| Keywords: | Schizophrenia Neurokinin receptors Peptidomimetic |
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