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.
Thienocycloheptapyridazines as new muscarinic agents / D., Barlocco; G., Cignarella; Fanelli, Francesca; B., Vitalis; P., Matyus; DE BENEDETTI, P. G.. - In: DRUG DESIGN AND DISCOVERY. - ISSN 1055-9612. - ELETTRONICO. - 14:(1997), pp. 273-290.
Thienocycloheptapyridazines as new muscarinic agents
FANELLI, Francesca;
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.
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