Synthesis and in vitro muscarinic activities of a series of 1,3-diazacycloalkyl carboxaldehyde oxime derivatives |
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Authors: | Plate Ralf Jans Christan G J M Plaum Marc J M de Boer Thijs |
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Affiliation: | Department of Medicinal Chemistry, N.V. Organon, PO Box 20, 5340 BH, Oss, The Netherlands. ralf.plate@organon.com |
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Abstract: | A series of 1,3-diazacycloalkyl carboxaldehyde oxime derivatives was synthesized and tested for muscarinic activity in receptor binding assays using [3H]-oxotremorine-M (OXO-M) and [3H]-pirenzepine (PZ) as ligands. Potential muscarinic agonistic or antagonistic properties of the compounds were determined using binding studies measuring their potencies to inhibit the binding of OXO-M and PZ. Preferential inhibition of OXO-M binding was used as an indicator for potential muscarinic agonistic properties; this potential was confirmed in functional studies on isolated organs. |
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