[Synthesis and analgesic activity of analogs of U-50488, an opiate kappa-agonist].
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.
Ma
S C
SC
Institute of Materia Medical of general Hospital of Nanjing.
Yang
Y L
YL
Yuan
X M
XM
D019900:3,4-Dichloro-N-methyl-N-(2-(1-pyrrolidinyl)-cyclohexyl)-benzeneacetamide, (trans)-Isomer; D000700:Analgesics / Q000138:chemical synthesis* / Q000494:pharmacology; D000818:Animals; D005260:Female; D051379:Mice; D015394:Molecular Structure; D011759:Pyrrolidines / Q000138:chemical synthesis* / Q000494:pharmacology; D011957:Receptors, Opioid; D017473:Receptors, Opioid, kappa
D000700:Analgesics; D011759:Pyrrolidines; D011957:Receptors, Opioid; D017473:Receptors, Opioid, kappa; D019900:3,4-Dichloro-N-methyl-N-(2-(1-pyrrolidinyl)-cyclohexyl)-benzeneacetamide, (trans)-Isomer