Characterization of two [3H]ketanserin recognition sites in rat striatum.
Two [3H]ketanserin recognition sites are present in the rat striatum. The high-affinity site (KD, 0.39 nM) is similar to the 5-hydroxytryptamine2 (5-HT2) site previously characterized by various investigators. The low-affinity site (KD, 21.8 nM) has a unique pharmacologic specificity and is preferentially localized to rat striatum and septum. Conventional 5-HT2 antagonists as well as 5-HT and 5-HT uptake inhibitors are ineffective at inhibiting [3H]-ketanserin binding to this low-affinity site. Also, chronic treatment with p-chlorophenylalanine, which depletes brain 5-HT, upregulates only the high-affinity site. Thus, in the striatum and septum, [3H]ketanserin labels a unique recognition site. This site has recently been shown to be associated with dopaminergic nerve endings and may regulate biogenic amine release.
D000818:Animals; D001667:Binding, Competitive; D002540:Cerebral Cortex / Q000378:metabolism; D003342:Corpus Striatum / Q000378:metabolism*; D010134:Fenclonine / Q000494:pharmacology; D006165:Guanylyl Imidodiphosphate / Q000494:pharmacology; D006892:Hydroxydopamines / Q000494:pharmacology; D007650:Ketanserin / Q000378:metabolism*; D008297:Male; D016627:Oxidopamine; D051381:Rats; D011919:Rats, Inbred Strains; D011985:Receptors, Serotonin / Q000378:metabolism*; D012688:Septum Pellucidum / Q000378:metabolism; D012701:Serotonin / Q000378:metabolism; D012702:Serotonin Antagonists / Q000378:metabolism
D006892:Hydroxydopamines; D011985:Receptors, Serotonin; D012702:Serotonin Antagonists; D012701:Serotonin; D006165:Guanylyl Imidodiphosphate; D016627:Oxidopamine; D007650:Ketanserin; D010134:Fenclonine