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Thienocycloheptapyridazines as new muscarinic agents
D Barlocco1, G Cignarella, F Fanelli
1Ist. Chimica Farmaceutica e Tossicologica, Milano, Italy.
Drug Design and Discovery
|April 1, 1997
Abstract:
A series of thienocycloheptapyridazines (3aa-dd), structurally related to Minaprine, was synthesized and compounds tested for their affinity towards muscarinic receptors. All of them showed Ki values in the micromolar range towards both the antagonist 3H-QNB and the agonist 3H-OXO-M, thus indicating that they act as antagonists at the muscarinic receptors. Moreover a theoretical study was performed on their interaction behaviour with a three dimensional (3-D) model of the human m1 muscarinic receptor.