Characteristics of [3H]5-hydroxytryptamine binding to iris-ciliary body tissue of the rabbit. 1995

G Chidlow, and L M De Santis, and N A Sharif, and N N Osborne
Nuffield Laboratory of Ophthalmology, University of Oxford, United Kingdom.

OBJECTIVE This study sought to identify, characterize, and localize subtypes of 5-hydroxytryptamine (HT) receptors in rabbit iris-ciliary body. METHODS Radioligand binding assays were performed with [3H]5-hydroxytryptamine on membranes prepared from rabbit iris-ciliary bodies and on tissue sections subsequently developed by autoradiography. RESULTS [3H]5-HT appeared to bind to a single population of receptors in membrane preparations of rabbit iris-ciliary body. The apparent affinity of the ligand (KD) was 2.19 nM, and the density of binding sites was 58.3 fmol/mg protein. Binding of [3H] 5-HT exhibited guanosine-5-triphosphate sensitivity. Competitive inhibition experiments were performed to differentiate between 5-HT receptor subtypes. A relative potency order of 5-CT > 5-HT = 8-OH-DPAT > ipsapirone > RU24969 > sumatriptan > ritanserin > ketanserin was demonstrated. The apparent inhibitory constants for the ligands tested fit with the profile expected of binding to 5-HT1A receptors. Inhibition studies with [3H] 5-HT plus 100 nM 8-OH-DPAT (which inhibits binding to 5-HT1A receptors only) representing total binding, indicated that no further displacement occurred when ligands preferentially selective for 5-HT1B, 5-HT1D alpha,1D beta, or 5-HT2C were tested. Total binding of [3H] 5-HT in tissue sections developed by autoradiography was displaced completely by 100 nM 8-OH-DPAT. Melatonin showed little affinity for the [3H] 5-HT binding sites. CONCLUSIONS A population of 5-HT1A receptors is present in rabbit ciliary processes. There is no evidence to suggest the presence of 5-HT1D alpha, 5-HT1D beta, 5-HT2B, or 5-HT2C receptors in the iris-ciliary body.

UI MeSH Term Description Entries
D007498 Iris The most anterior portion of the uveal layer, separating the anterior chamber from the posterior. It consists of two layers - the stroma and the pigmented epithelium. Color of the iris depends on the amount of melanin in the stroma on reflection from the pigmented epithelium.
D008550 Melatonin A biogenic amine that is found in animals and plants. In mammals, melatonin is produced by the PINEAL GLAND. Its secretion increases in darkness and decreases during exposure to light. Melatonin is implicated in the regulation of SLEEP, mood, and REPRODUCTION. Melatonin is also an effective antioxidant.
D011817 Rabbits A burrowing plant-eating mammal with hind limbs that are longer than its fore limbs. It belongs to the family Leporidae of the order Lagomorpha, and in contrast to hares, possesses 22 instead of 24 pairs of chromosomes. Belgian Hare,New Zealand Rabbit,New Zealand Rabbits,New Zealand White Rabbit,Rabbit,Rabbit, Domestic,Chinchilla Rabbits,NZW Rabbits,New Zealand White Rabbits,Oryctolagus cuniculus,Chinchilla Rabbit,Domestic Rabbit,Domestic Rabbits,Hare, Belgian,NZW Rabbit,Rabbit, Chinchilla,Rabbit, NZW,Rabbit, New Zealand,Rabbits, Chinchilla,Rabbits, Domestic,Rabbits, NZW,Rabbits, New Zealand,Zealand Rabbit, New,Zealand Rabbits, New,cuniculus, Oryctolagus
D011869 Radioligand Assay Quantitative determination of receptor (binding) proteins in body fluids or tissue using radioactively labeled binding reagents (e.g., antibodies, intracellular receptors, plasma binders). Protein-Binding Radioassay,Radioreceptor Assay,Assay, Radioligand,Assay, Radioreceptor,Assays, Radioligand,Assays, Radioreceptor,Protein Binding Radioassay,Protein-Binding Radioassays,Radioassay, Protein-Binding,Radioassays, Protein-Binding,Radioligand Assays,Radioreceptor Assays
D011985 Receptors, Serotonin Cell-surface proteins that bind SEROTONIN and trigger intracellular changes which influence the behavior of cells. Several types of serotonin receptors have been recognized which differ in their pharmacology, molecular biology, and mode of action. 5-HT Receptor,5-HT Receptors,5-Hydroxytryptamine Receptor,5-Hydroxytryptamine Receptors,Receptors, Tryptamine,Serotonin Receptor,Serotonin Receptors,Tryptamine Receptor,Tryptamine Receptors,Receptors, 5-HT,Receptors, 5-Hydroxytryptamine,5 HT Receptor,5 HT Receptors,5 Hydroxytryptamine Receptor,5 Hydroxytryptamine Receptors,Receptor, 5-HT,Receptor, 5-Hydroxytryptamine,Receptor, Serotonin,Receptor, Tryptamine,Receptors, 5 HT,Receptors, 5 Hydroxytryptamine
D002462 Cell Membrane The lipid- and protein-containing, selectively permeable membrane that surrounds the cytoplasm in prokaryotic and eukaryotic cells. Plasma Membrane,Cytoplasmic Membrane,Cell Membranes,Cytoplasmic Membranes,Membrane, Cell,Membrane, Cytoplasmic,Membrane, Plasma,Membranes, Cell,Membranes, Cytoplasmic,Membranes, Plasma,Plasma Membranes
D002924 Ciliary Body A ring of tissue extending from the scleral spur to the ora serrata of the RETINA. It consists of the uveal portion and the epithelial portion. The ciliary muscle is in the uveal portion and the ciliary processes are in the epithelial portion. Corpus Ciliare,Corpus Ciliaris,Bodies, Ciliary,Body, Ciliary,Ciliare, Corpus,Ciliares, Corpus,Ciliari, Corpus,Ciliaris, Corpus,Ciliary Bodies,Corpus Ciliares,Corpus Ciliari
D000818 Animals Unicellular or multicellular, heterotrophic organisms, that have sensation and the power of voluntary movement. Under the older five kingdom paradigm, Animalia was one of the kingdoms. Under the modern three domain model, Animalia represents one of the many groups in the domain EUKARYOTA. Animal,Metazoa,Animalia
D001345 Autoradiography The making of a radiograph of an object or tissue by recording on a photographic plate the radiation emitted by radioactive material within the object. (Dorland, 27th ed) Radioautography
D001667 Binding, Competitive The interaction of two or more substrates or ligands with the same binding site. The displacement of one by the other is used in quantitative and selective affinity measurements. Competitive Binding

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