Effects of sigma receptor ligands on scehdule-controlled behavior of rats: Relation to sigma and PCP receptor binding affinity

Eleven drugs were examined for their ability to inhibit sigma and phencyclidine (PCP) receptor binding, as labelled by (+)( super(3)H)-R-3-(3-hydroxyphenyl)-N-(1-propyl)piperidine ((+)-3-PPP), ( super(3)H)ditolylguanidine (DTG), (+)( super(3)H)N-allylnormetazocine (NANM) and ( super(3)H)1-(1-(2-thie...

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Published in:Psychopharmacology 1991-01, Vol.104 (2), p.157-163
Main Authors: Wettstein, J G, Roman, F J, Rocher, M-N, Junien, J-L
Format: Article
Language:English
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Summary:Eleven drugs were examined for their ability to inhibit sigma and phencyclidine (PCP) receptor binding, as labelled by (+)( super(3)H)-R-3-(3-hydroxyphenyl)-N-(1-propyl)piperidine ((+)-3-PPP), ( super(3)H)ditolylguanidine (DTG), (+)( super(3)H)N-allylnormetazocine (NANM) and ( super(3)H)1-(1-(2-thienyl)cyclohexyl)-4iperidine (TCP), in membrane preparations from whole rat brain. The same drugs were studied for their effects under a fixed-ratio (FR) schedule of food reinforcement in rats. The binding affinities of all 11 drugs for either the ( super(3)H)DTG, (+)( super(3)H)-3-PPP, (+)( super(3)H)NANM or ( super(3)H)TCP site did not correlate significantly with the potenties of the same drugs for decreasing FR behavior. The results further indicate that it is difficult to distinguish between purported sigma agonists and antagonist drugs.
ISSN:0033-3158