By John W. Kebabian (auth.), George Poste, Stanley T. Crooke (eds.)
Dopamine, as well as its significance as a precursor of norepinephrine, is referred to now to be an enormous neurotransmitter in regulating sensible actions in a couple of significant organ platforms, together with the imperative ner vous method. the cardiovascular procedure, the kidney, and the intestine. fresh advances in our knowing of the sensible position of dopamine, its mechanism of motion and the pharmacology of dopaminergic brokers have happened on a vast entrance. the previous couple of years have witnessed major growth within the identity and type of vital and peripheral dopamine receptors and the criteria that have an effect on their responsiveness to inhibitory and stimulatory ligands. those advances were paralleled via new insights into the contribution of changes in dopaminergic reg ulation in inflicting sickness and the application of dopamine agonists and an tagonists as healing modalities. This quantity, the 1st in a chain of guides bobbing up from the yearly Smith Kline and French examine Symposium on New Horizons in Therapeutics, offers a accomplished survey of present study on peripheral dopamine receptors and the physiologic and healing con sequences of stimulating pre-and postsynaptic dopamine receptors. learn in dopamine pharmacology mirrors the impressive advert vances which are taking place within the box of pharmacology at huge as a con series of the involvement of an ever-larger variety of clinical dis ciplines within the research of drug action.
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Extra info for Dopamine Receptor Agonists
Long, J. , Flynn, 1. , Cannon, 1. , and Lee, T. , 1980, Neurochemical and behavioral evidence for a selective presynaptic dopamine receptor agonist, Science 210:1141-1143. 20 DOPAMINE RECEPTORS Grewe, C. , and Kebabian, J. , 1982, Dopamine stimulates production of cyclic AMP by the salivary gland of the cockroach, Nauphoeta cinerea, Cell. Mol. Neurobiol. 2:6569. Grewe, C. , Frey, E. , Cote, T. , and Kebabian, J. , 1982, YM-09151-2: A potent antagonist for a peripheral Dz-dopamine receptor, Eur.
1. , 1983, Peripheral dopamine receptors: A classification based on potency series and specific antagonism, Trends Pharmacol. Sci. 4:64-66. Goldman, M. , Kebabian, J. , and Eskay, R. , 1983, a-Melanocytestimulating hormone-like peptides in the intermediate lobe of the rat pituitary gland: Characterization of content and release in vitro, Endocrinology 112:435-441. Goodale, D. , Rusterholz, D. , Long, J. , Flynn, 1. , Cannon, 1. , and Lee, T. , 1980, Neurochemical and behavioral evidence for a selective presynaptic dopamine receptor agonist, Science 210:1141-1143.
Nonspecific binding alone is measured in parallel sets of test tubes containing, in addition, excess of a nonradioactive drug known to block the receptors of interest [( + )butac1amol more often than not for dopamine receptors]. Specific binding is then determined by simple subtraction. Receptor number and affinity for the radioligand are determined by conducting saturation experiments utilizing increasing concentrations of radioligand. The affinity of nonradioactive drugs is determined in "competition" experiments in which 25 Radioligand Binding Studies Table I.
Dopamine Receptor Agonists by John W. Kebabian (auth.), George Poste, Stanley T. Crooke (eds.)