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3 - History of Anaesthesia Society

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Drs C.J.Niemegeers & F Awouters (~eerse, ~elgium)<br />

Janss~~n Reaea~xh has contri'xltsd t.r, anaesthesia mainly by introdllcing<br />

ptent and safe analqesics and neuroleptics. T'le developnent<br />

<strong>of</strong> tllesa corrrpou~ds started 37 years ago, when Paul Janssen evaluated the<br />

ph3m~coloqical activity <strong>of</strong> new mlscules chemically related to<br />

pethidine. It w.3~ t+ Stdrt <strong>of</strong> extensive studies on structure-activity<br />

relationship which led to very rptent and selective camp3unds providhq<br />

gieater clinical efficacy and safety (Figure 1).<br />

Figure 1. Pethidine-related ilevelopnent <strong>of</strong> potent ,Janssen<br />

narcotics and neuroleptics<br />

Early developtent <strong>of</strong> drugs<br />

Via the rmich base, th? propioah..nune R951 was synthesised and further<br />

elaborated to very ptent and specific narcotics and neuroleptics. When<br />

the 3-carbn bridge wss shortend to an ethyl group, narcotic activity<br />

increased; .3ul3?tituents on carbon 4 <strong>of</strong> the pipxidine ring were varied<br />

extensively to end up for optimal activity with the propioanilide group<br />

<strong>of</strong> fentanyl. Men tne 3-carbon bridge was length~n~rl by one methylene<br />

group as in the first butyrophznone, RllS7, neuroleptic activity

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