Characterization of a serotonin receptor in the cnidarian Renilla koellikeri: a radiobinding analysis.
Serotonin (5-HT) binding sites in membrane preparations from the sea pansy Renilla koellikeri were identified using [3H]5-HT as radioligand and unlabelled 5-HT as displacer of specific binding. Saturation and kinetic studies revealed a mixed population of [3H]5-HT binding sites which as a whole displayed slow association kinetics, saturability, negligible dissociation and low affinity. The dopaminergic antagonist trifluoperazine specifically displaced the non-dissociated binding sites, allowing the characterization of a homogenous population of saturable sites exhibiting faster association and full dissociation. Scatchard analysis of this population revealed a KD of 23-34 nM and binding site density (Bmax) of 8.5-20.6 pmol/mg protein depending on body region. The pharmacological profile of the dissociable [3H]5-HT binding sites could not be categorized with that of any of the existing vertebrate and invertebrate 5-HT receptor subtypes in the current nomenclature. Especially noteworthy was the absolute inability of LSD, a ligand of choice for all hitherto identified invertebrate 5-HT receptors, to compete for the binding sites in sea pansy membrane preparations. It is proposed that these binding sites represent an evolutionary forerunner of the primordial 5-HT receptor that diversified as multiple subtypes in higher invertebrates and vertebrates.
Hajj-Ali
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Département de Pathologie, Faculté de Médecine, Université de Montréal, Québec, Canada.
Anctil
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D000818:Animals; D003063:Cnidaria / Q000378:metabolism*; D016244:Guanosine 5'-O-(3-Thiotriphosphate) / Q000494:pharmacology; D006153:Guanosine Diphosphate / Q000031:analogs & derivatives / Q000494:pharmacology; D011869:Radioligand Assay; D011985:Receptors, Serotonin / Q000032:analysis*; D013873:Thionucleotides / Q000494:pharmacology
D011985:Receptors, Serotonin; D013873:Thionucleotides; D006153:Guanosine Diphosphate; D016244:Guanosine 5'-O-(3-Thiotriphosphate); C023427:guanosine 5'-O-(2-thiodiphosphate)