Summary
[3H]205–501, a noncatechol dopaminergic agonist, is presented as a ligand with high affinity (KD ∼ 1 nM) and high selectivity for dopamine receptors. pKi values of dopaminergic agonists derived from competition isotherms in the [3H]205–501 binding assay correlate very well with their potency in the acetylcholine release assay, which is controlled by dopamine D2 receptors. There is however no correlation with their potency stimulating adenylate cyclase, a process controlled by dopamine D1 receptors. Thus [3H]205–501 is the first agonist ligand selective for dopamine D2 receptors.
Similar content being viewed by others
References
Bacopoulos, N. G.: Dopaminergic3H-agonist receptors in rat brain. Life Sci.34, 307–315 (1984).
Brown, E. M., Aurbach, G. D., Hauser, D., Troxler, F.: Β-adrenergic receptor interactions. Characterization of iodohydroxybenzylpindolol as a specific ligand. J. Biol. Chem.251, 1232–1238 (1976).
Burt, D. R., Creese, I., Snyder, S. H.: Properties of [3H]haloperidol and [3H]dopamine binding associated with dopamine receptors in calf brain membranes. Mol. Pharmacol.12, 800–812 (1976).
Cheng, Y. C., Prusoff, W. H.: Relationship between the inhibition constant Ki and the concentration of inhibitor which caused 50% inhibition (IC50) of an enzymatic reaction. Biochem. Pharmacol.22, 3099–3108 (1973).
Closse, A., Frick, W., Dravid, A., Balliger, G., Hauser, D., Sauter, A., Tobler, H. J.: Classification of drugs according to receptor binding profiles, Naunyn-Schmiedeberg's Arch. Pharmacol.327, 95–101 (1984).
Creese, I., Burt, D. R., Snyder, S. H.: Dopamine receptor binding predicts clinical and pharmacological potencies of antischizophrenic drugs. Science192, 481–483 (1976).
Creese, I., Schneider, R., Snyder, S. H.:3H-Spiroperidol labels dopamine receptors in pituitary and brain. Eur. J. Pharmacol.46, 371–381 (1977).
Creese, I., Hamblin, M. W., Leff, S. E., Sibley, D. R.: CNS dopamine receptors. In: Biochemical Studies of CNS Receptors (Iversen, L. L., Iversen, S. D., Snyder, S. H., eds.), pp. 81–138. New York: Plenum Press. 1983 a.
Creese, I., Sibley, D. R., Hamblin, M. W., Leff, S. E.: The classification of dopamine receptors, relationship to radioligand binding. Ann. Rev. Neurosci.6, 43–71 (1983 b).
Enjalbert, A., Bockaert, J.: Pharmacological characterisation of the D2 dopamine receptor negatively coupled with adenylate cyclase in rat pituitary. Mol. Pharmacol.23, 576–584 (1983).
Euvrard, C., Premont, J., Oberlander, C., Boissier, J. R., Bockaert, J.: Is dopamine-sensitive adenylate cyclase involved in regulating the activity of striatal cholinergic neurons? Naunyn-Schmiedeberg's Arch. Pharmacol.309, 241–245 (1979).
Flückiger, E., Briner, U., Bürki, H. R., Marbach, P., Wagner, H. R., Doepfner, W.: Two novel prolactin release-inhibiting 8α-aminoergolines. Experientia35, 1677–1678 (1979).
Frandsen, E. K., Krishna, G.: A simple ultrasensitive method for the assay of cyclic AMP and cyclic GMP in tissues. Life Sci.23, 529–542 (1976).
Giger, R., Jaton, A. L., Vigouret, J. M., Closse, A., Enz, A., Markstein, R.: Pharmakochemie der Abeorphine: neuartige Apomorphin-Derivate mit Dibenz[cd,f]indol-Grundgerüst, Jahrestagung Schweiz. Chem. Gesellschaft, Bern, 19. Oktober 1984.
Hertting, G., Zumstein, A., Jackisch, R., Hoffmann, J., Starke, K.: Modulation by endogenous dopamine of the release of acetylcholine in the caudate nucleus of the rabbit. Naunyn Schmiedeberg's Arch. Pharmacol.315, 111–117 (1980).
Hjorth, S., Carlson, A., Wikström, H., Lindberg, P., Sanchez, D., Hacksell, U., Arvidsson, L. E., Svensson, U., Nikon, J. L. G.: 3-PPP, a new centrally acting DA receptor agonist with selectivity for autoreceptors. Life Sci.28, 1225–1238 (1981).
Iorio, L. C., Barnett, A., Leitz, F. H., Houser, V. P., Korduba, C. A.: Seh 23390, a potential benzazepine antipsychotic with unique interactions on dopaminergic systems. J. Pharmacol. Exp. Therap.226, 462–468 (1983).
Kebabian, J. W., Calne, D. B.: Multiple receptors for dopamine. Nature227, 93–96 (1979).
Kebabian, J. W., Petzold, G. L., Greengard, P.: Dopamine-sensitive adenylate cyclase in caudate nucleus of rat brain and its similarity to the dopamine receptor. Proc. Natl. Acad. Sci. U.S.A.69, 2145–2149 (1972).
König, J. F. R., Klippel, R. A.: The Rat Brain: A Stereotaxic Atlas. New York: Krieger. 1970.
Leysen, J. E., Gommeren, W.: Different kinetic properties of neuroleptic receptor binding in the rat striatum and frontal cortex. Life Sci.23, 447–452 (1978).
Leysen, J. E., Gommeren, W.: Optimal conditions for [3H]apomorphine binding and anomalous equilibrium binding of [3H]apomorphine and [3H]spiperone to rat striatal membranes: Involvement of surface phenomena versus multiple binding sites. J. Neurochem. 36, 201–219 (1981).
Nordmann, R., Petcher, T.J.: Octahydrobenzo[g]quinolines: Potent dopamine agonists which show the relationship between ergolines and apomorphine. J. Med. Chem. (1985, in press).
Roemer, D., Büscher, H., Hill, R. C., Maurer, R., Petcher, T. J., Welle, H. B. A., Bakel, H. C. C. K., Akkerman, A. M.: Bremazocine: A potent, long-acting opiate kappa-agonist. Life Sci.27, 971–978 (1980).
Seeman, P.: Brain dopamine receptors. Pharmacol. Rev.32, 229–313 (1981).
Seiler, M. P., Markstein, R.: Further characterization of structural requirements for agonists at the striatal dopamine D-l receptor. Mol. Pharmacol.22, 281–289 (1982).
Sokoloff, P., Martres, M. P., Schwartz, J. C.: Three classes of dopamine receptor (D-2, D-3, D-4) identified by binding studies with [3H]apomorphine and [3H]-domperidone. Naunyn-Schmiedeberg's Arch. Pharmacol.315, 89–102 (1980).
Stoof, J. C., Thieme, R. E., Vrijmoed-de, Vries, Mulder, A. H.: In vitro acetylcholine release from rat caudate nucleus as a new model for testing drugs with dopamine receptor activity. Naunyn-Schmiedeberg's Arch. Pharmacol.309, 119–124 (1979).
Theodorou, A., Hall, E., Jenner, M. D., Marsden, C. D.: Cation regulation differentiates specific binding of [3H]sulpiride and [3H]spiperone to rat striatal preparations. J. Pharmacol.32, 441–444 (1981).
Tobler, H. J., Engel, G.: Affinity spectra: A novel way for the evaluation of equilibrium binding experiments. Naunyn-Schmiedeberg's Arch. Pharmacol.322, 183–192 (1983).
Withy, R. M., Mayer, R. J., Strange, P. G.: Use of [3H]spiperone for labelling dopaminergic and serotoninergic receptors in bovine caudate nucleus. J. Neurochem.37, 1144–1154 (1981).
Zahniser, N. R., Molinoff, P. B.: Thermodynamic differences between agonist and antagonist interactions with binding sites for [3H]spiroperidol in rat striatum. Mol. Pharmacol.23, 303–309 (1983).
Author information
Authors and Affiliations
Rights and permissions
About this article
Cite this article
Closse, A., Frick, W., Markstein, R. et al. [3H]205-501, a Non-catechol dopaminergic agonist, labels selectively and with high affinity dopamine D2 receptors. J. Neural Transmission 62, 231–248 (1985). https://doi.org/10.1007/BF01252239
Received:
Revised:
Issue Date:
DOI: https://doi.org/10.1007/BF01252239