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- W2137223223 abstract "The labelling by 3H-spiperone of serotonin-S2 receptors in rat frontal cortex tissue adsorbed to glass fibre filters was investigated. For 12 unlabelled serotonin antagonists the dissociation time from serotonin-S2 receptors was measured using rat frontal cortex tissue preparations adsorbed to glass fibre filters. The dissociation half-time varied from 4.8 min for pipamperone to 160 min for ritanserin. The drug-receptor dissociation time was not related to a particular class of chemical structure, or to the lipophilicity or the acid dissociation constant of the drugs. The essential requirement of experimental determination of the drug-receptor dissociation time for each drug individually is illustrated. The possible applications of the knowledge of the drug-receptor dissociation time in in vitro and in vivo receptor studies, in pharmacological and pharmacokinetic studies and in drug design and receptor modelling is discussed. For various serotonin-S2 antagonists, the type of inhibition produced by the drug on 3H-ketanserin binding to serotonin-S2 receptors was determined using suspensions of rat frontal cortical tissue. The observed patterns of inhibition were clearly related to the drug-receptor dissociation times: rapidly dissociating drugs produced competitive inhibition, drugs with dissociation half-times between 15-30 min produced mixed type inhibition, and the very slowly dissociating ritanserin produced non-competitive inhibition." @default.
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- W2137223223 date "1988-01-01" @default.
- W2137223223 modified "2023-09-23" @default.
- W2137223223 title "The Dissociation Rate of Unlabelled Drugs from Receptor Sites: A Poorly Investigated, Yet Important Aspect in Receptor Research. Studies on the Serotonin-S2Receptor" @default.
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- W2137223223 doi "https://doi.org/10.3109/10799898809049011" @default.
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