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Trishomocubanes, a new class of selective and high affinity ligands for the sigma binding site

✍ Scribed by Michael Kassiou; Vu H. Nguyen; Robert Knott; MacDonald J. Christie; Trevor W. Hambley

Publisher: Elsevier Science
Year: 1996
Tongue: English
Weight: 279 KB
Volume: 6
Category: Article
ISSN: 0960-894X
DOI: 10.1016/0960-894x(96)00067-4

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✦ Synopsis

The synthesis, receptor binding, and preliminary structural characterisation of trishomocubanes of types pentacyclo [5.4.0.02'6.03'l°.05'9]undecylamines and 4-azahexacyclo[5.4.1.0E'6.03'l°.05'9.08'll]dodecanes are described. These ligands demonstrated high selectivity and affinity for the sigma binding site.

The chemistry of polycyclic molecules has been of interest over the past five decades but only recently have their pharmacological properties been investigated. The tricyclic amantadine 1 and memantine 2 are clinically used in the treatment of Parkinson's disease and dementia. L2 There is considerable evidence

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