Publisher： Bentham Science Publishers
E-ISSN： 1873-4286|18|7|938-949
ISSN： 1381-6128
Source： Current Pharmaceutical Design, Vol.18, Iss.7, 2012-03, pp. : 938-949
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Abstract
Although several pieces of information are still missing about sigma-2 ( 2) receptor, the production of high affinity 2 receptor ligands allowed important acquisitions. Morphans such as CB64D and CB184 were the first truly 2-selective ligands synthesized, and their use in cell cultures highlighted the relationship between 2 receptors and cell proliferation, shedding light on important diagnostic and therapeutic potentials with which 2 ligands are endowed. The most significant classes of compounds are herein discussed. The design and Structure-Affinity Relationship studies (SAfiR) of 2 receptor ligands belonging to the classes of morphans, indoles (siramesine analogues), granatanes, flexible benzamides and N-cyclohexylpiperazines are reported, together with the biological results which these compounds provided giving a crucial contribution to the 2 receptor research. The pharmacophore models which were generated on the basis of different classes of the 2 ligands and the attempts for 2 receptor purification are briefly described.
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