Specific [3H]LY278584 binding to 5-HT3 recognition sites in rat cerebral cortex.
Binding of [3H]LY278584 a 1-methyl-indazole-carboxamide, to putative 5-HT3 recognition sites in membranes isolated from cerebral cortex of rat brain, is examined. Specific binding of [3H]LY278584 accounts for 83-93% of total binding. The unlabelled LY278584 has 500 times greater affinity for [3H]LY278584 recognition sites than its 2-methyl analogue (LY278989), and their potencies parallel their antagonism of the peripheral 5-HT3 receptors. Moreover, the order of potencies of other known antagonists of 5-HT3 receptors supports the conclusion that [3H]LY278584 binds to putative 5-HT3 receptors in cortical membranes.
Wong
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Lilly Research Laboratories, Eli Lilly and Company, Lilly Corporate Center, Indianapolis 46285.
Robertson
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Reid
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LR
D000818:Animals; D002540:Cerebral Cortex / Q000187:drug effects / Q000378:metabolism*; D066298:In Vitro Techniques; D007191:Indazoles / Q000378:metabolism*; D008297:Male; D011720:Pyrazoles / Q000378:metabolism*; D051381:Rats; D011919:Rats, Inbred Strains; D011985:Receptors, Serotonin / Q000187:drug effects / Q000378:metabolism*; D012702:Serotonin Antagonists / Q000378:metabolism*; D014326:Tropanes / Q000378:metabolism
D007191:Indazoles; D011720:Pyrazoles; D011985:Receptors, Serotonin; D012702:Serotonin Antagonists; D014326:Tropanes; C061531:LY 278584