Synthesis and 5-HT-3 receptor binding activity of 5-[125 I] iodo-2, 3-dimethoxy-N-(1-azabicyclo [2.2. 2] oct-3-yl) benzamide and its 5-halogen-2-alkoxyl homologues
…, WA Hewlett, DE Schmidt, NS Mason, BL Trivedi…
文献索引：De Paulis; Hewlett; Schmidt; Mason; Trivedi; Ebert European Journal of Medicinal Chemistry, 1997 , vol. 32, # 5 p. 385 - 396
(S)-5-Iodo-2, 3-dimethoxy-N-(1-azabicyclo [2.2. 2] oct-3-yl) benzamide (MIZAC) was prepared from 5-iodo-2, 3-dimethoxybenzoyl chloride and (S)-3-aminoquinuclidine.[125I] Iodode-stannylation of its corresponding 5-tri-n-butyltin derivative gave [125I]-MIZAC at 1800 Ci/mmol. Binding of [125I]-MIZAC in rat entorhinal cortex revealed a KD of 1.37±0.21 nM. A series of racemic 2-O-alkyl derivatives of MIZAC were prepared and 5-HT-3 receptor ...
