Synthesis and Characterization of Radioiodinated N-(3-Iodopropen-1-yl)-2. beta.-carbomethoxy-3. beta.-(4-chlorophenyl) tropanes: Potential Dopamine Reuptake Site …

MM Goodman, MP Kung, GW Kabalka…

Index: Goodman; Kung; Kabalka; Switzer Journal of Medicinal Chemistry, 1994 , vol. 37, # 10 p. 1535 - 1542

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Citation Number: 90

Abstract

N-(3-iodopropen-l-yl)-2~-carbomethoxy-3~-(4-chlorophenyl) tropane by iododemetalation of the corresponding 3-(tri-n-butylstannyl) derivatives. Competition binding data of various dopamine reuptake ligands with rat striatal tissue preparation for either [12611-12 or [1261]- 13 exhibited the following order of potency: E-13> 2-12> GBR 12909>> mazindol>>>(-)- cocaine. Tissue distribution studies in rats showed that the E-13 was the best analogue. E- ...