Synthesis and SAR exploration of dinapsoline analogues

SY Sit, K Xie, S Jacutin-Porte, KM Boy, J Seanz…

Index: Sit, Sing-Yuen; Xie, Kai; Jacutin-Porte, Swanee; Boy, Kenneth M.; Seanz, James; Taber, Matthew T.; Gulwadi, Amit G.; Korpinen, Carolyn D.; Burris, Kevin D.; Molski, Thaddeus F.; Ryan, Elaine; Xu, Cen; Verdoorn, Todd; Johnson, Graham; Nichols, David E.; Mailman, Richard B. Bioorganic and Medicinal Chemistry, 2004 , vol. 12, # 4 p. 715 - 734

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Citation Number: 20

Abstract

Dinapsoline is a full D1 dopamine receptor agonist that produces robust rotational activity in the unilateral 6-OHDA rat model. This compound is orally active, and shows a low tendency to cause tolerance in rat models. The active enantiomer was determined to have the S-(+) configuration, and the opposite enantiomer is essentially devoid of biological activity. Taken together, dinapsoline has significant metabolic and pharmacological advantages over ...