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Cancer; pain

s1 Receptor;
s2 receptor

In vitro and mouse studies suggest adamantine phenylalkylamines could help treat cancer and reduce neuropathic pain induced by cancer drugs. In human cancer cell lines, adamantine phenylalkylamines that bound the s1 and s2 receptors showed antiproliferative activity and selectivity over normal human cell lines. In four different mouse xenograft models of cancer, one phenylalkylamine had better activity than several marketed chemotherapeutics and showed antimetastatic effects. In a mouse model of neuropathic pain, the compound had an analgesic effect. Next steps could include testing the compound in additional animal models.
At least seven companies have compounds targeting the s1 receptor in Phase II testing or earlier for cancer or neurology indications, including pain.

SciBX 5(45); doi:10.1038/scibx.2012.1188
Published online Nov. 15, 2012

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Riganas, S. et al. J. Med. Chem.; published online Oct. 24, 2012;
Contact: George B. Foscolos, National and Kapodestrian University of Athens, Athens, Greece