Radioligand receptor assay

Reichert LE Jr (1976) Follicle-stimulating hormone measurement by a rat testes tubule receptor assay. In Blecher M (ed) Methods in Receptor Research, Part I. Marcel Dekker, Inc., New York and Basel, pp 99-118 Reichert LE, Bhalla VK (1974) Development of a radioligand receptor assay for human follicle stimulating hormone. Endocrinology 94 483-491... 

Simoni M, Weinbauer GF, Nieschlag E (1993) Molecular composition of two different batches of urofollitropin Analysis by immunofluorometric assay, radioligand receptor assay and in vitro bioassay. J Endocrin Invest 16 21-27 Starring PL, Gaines Das RE (1989) The International Standard for pituitary FSH collaborative study of the Standard and of four other purified human FSH preparations of differing molecular composition by bioassays, receptor... 

Catt KJ, Dufau ML, Tsuruhara J. Radioligand-receptor assay of luteinizing hormone and chorionic gonadotropin. J Clin Endocrinol Metab 1972 34 123-32. 

Miscellaneous Glycoproteins. Bovine lutrophin, bovine thyrotrophin, and human chorionic gonadotrophin preparations with carbodi-imide-mediated covalently cross-linked sub-units have been isolated in high yield and characterized by c.d. spectroscopy, radioligand receptor assays, and hormone-specific bioassays. The c.d. spectra of the native and cross-linked hormones did not differ much, suggesting that there is little conformational change on cross-linking. 

There should be specific, saturable binding to the receptor, accompanied by pharmacological characteristics appropriate to the functional effects, demonstrable using a radioactive, eg, tritium or iodine-125, ligand to label the receptor. Radioligand binding assays (1,6) have become a significant means by which to identify and characterize receptors and enzymes (see Immunoassays Radioactive tracers). Isolation of the receptor or expression of the receptor in another cell, eg, an oocyte can be used to confirm the existence of a discrete entity. 

The selectivity for 5-HT4 vs. other 5-HT receptor subtypes was examined in a set of radioligand binding assays available at the time (5-HT1A, 5-HT1D, 5-HT2A., 5-HT2c and 5-HT3) for some of the new compounds. While most derivatives exhibited a high selectivity for 5-HT4 vs. 5-HT3 receptors, structural adjustments of 5 led to profound effects on selectivity vs. other 5-HT receptors. 

Table 6.2 Training set molecules for a1A adrenergic receptor and their affinity measured in a radioligand displacement assay.

Table 7.1 Affinities (mean + SEM, n = 3) for dopamine antagonists at D] receptors obtained by MS-binding assays and radioligand binding assays, respectively [61],...

Wang, J.-X., Yamamura, H. I., Wang, W, Roeske, W. R. The use of the filtration technique in in vitro radioligand binding assays for membrane-bound and solubilized receptors, in Receptor-Ligand Interactions. A Practical Approach, ed. Hulme, E. C., IRL Press, Oxford,... 

Although a very reliable radioligand binding assay with use The search for P2X receptor of a stable ATP analog (e.g. a, p-methylene ATP) and subtype selective ligands... 

The library of mimetics 84 was screened in a radioligand-binding assay against a cloned fMLF receptor. Four compounds corresponding to the contents from the two most active wells were prepared on a larger scale and purified. In both instances, the inhibitory activity was due... 

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