[D-Thr2, Thz5]- and [D-Met2, Thz5]-enkephalinamides: Potent analgesics by intravenous injection |
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| Authors: | Donald Yamashiro Liang-fu Tseng Choh Hao Li |
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| Affiliation: | 1. Hormone Research Laboratory University of California San Francisco, California 94143, USA;1. Departments of Psychiatry and Pharmacology University of California San Francisco, California 94143, USA |
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| Abstract: | Two enkephalin analogs, [D-Met2, Thz5]-enkephalinamide and [D-Thr2, Thz5]-enkephalinamide, have been synthesized by the solid-phase method. When injected centrally, [D-Thr2, Thz5]-enkephalinamide is 3.5 times more potent than the [D-Met2, Thz5] analog. However, the two are equipotent and 4.2–4.8 times more potent than morphine when injected intravenously. |
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