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Hoffmann, R. A wiki for the life sciences where authorship matters. Nature Genetics (2008)
 

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Analgesic and tranquilizing activity of 5,8-disubstituted 1-tetralone Mannich bases.

5,8-Disubstituted 1-tetralone Mannich bases represent semirigid variants of classical (i.e., chlorpromazine) neuroleptic agents. 8-Chloro-5-methoxy-2-morpholinomethyl-1-tetralone exhibits neuroleptic potency in the thiothixene range in animal models. Of greater potential interest, however, is the analgesic potency of the 8-chloro-5-methoxy-2-pyrrolidinomethyl analogue which was in the morphine range. This compound did not induce tolerance nor was its activity reversed by naloxone. Structure-activity relationships of the series are discussed.[1]

References

  1. Analgesic and tranquilizing activity of 5,8-disubstituted 1-tetralone Mannich bases. Welch, W.M., Harbert, C.A., Sarges, R., Stratten, W.P., Weissman, A. J. Med. Chem. (1977) [Pubmed]
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