Barlocco D, Cignarella G, Fanelli F, Vitalis B, Matyus P, De Benedetti P G
Ist. Chimica Farmaceutica e Tossicologica, Milano, Italy.
Drug Des Discov. 1997 Apr;14(4):273-90.
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.
合成了一系列与米那普明结构相关的噻吩并环庚哒嗪（3aa - dd），并测试了这些化合物对毒蕈碱受体的亲和力。它们对拮抗剂3H - QNB和激动剂3H - OXO - M的Ki值均在微摩尔范围内，因此表明它们在毒蕈碱受体上起拮抗剂作用。此外，还对它们与人类m1毒蕈碱受体的三维（3 - D）模型的相互作用行为进行了理论研究。
