[Synthesis and analgesic activity of analogs of U-50488, an opiate kappa-agonist]
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Assessment of Morphine-induced Hyperalgesia and Analgesic Tolerance in Mice Using Thermal and Mechanical Nociceptive Modalities
Published on: July 29, 2014
Abstract:
In this paper, we report the synthesis and analgesic activities in mouse hot plate test and writhing test of some analogs of U-50488, a kappa-agonist. Results showed that compounds in which the amino group was pyrrolinyl had higher kappa-agonist activity and the substitution of two chlorine atoms in 3 and 4-positions of the benzene nucleus was very important to kappa-activity. Furthermore, all of compounds in which the amino group was piperidyl, piperazinyl or morpholinyl exhibited very weak kappa-agonist activity.
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