title: Molecular pharmacology of beta-adrenoceptors.
abstract: The development of radioligand-binding studies has greatly advanced our knowledge of the molecular pharmacology of beta-adrenoceptors. With this technique it is possible for the first time to directly determine the tissue concentration of beta-adrenoceptors, and by this, the responsiveness of tissues to beta-adrenergic stimulation. One major insight into the molecular pharmacology of beta-adrenoceptors to come from radioligand-binding studies was that the tissue concentration of beta-adrenoceptors is not a fixed number, but is rather dynamically regulated by a variety of drugs, hormones, physiological and pharmacological conditions. Since changes in beta-adrenoceptors assessed in circulating lymphocytes of man mirror changes in density and functional responsiveness of the corresponding myocardial beta-adrenoceptors, alterations in beta-adrenoceptor function can be also studied in human beings. In addition, by means of radioligand-binding studies the coexistence of beta 1- and beta 2-adrenoceptors has been demonstrated in numerous tissues of various species, including human heart and lung. The detailed knowledge of distribution and regulation of beta-adrenoceptors should help to improve the individual effectiveness of drug treatment.
mesh_terms: D000818:Animals; D004082:Dihydroalprenolol / Q000378:metabolism; D006801:Humans; D020120:Iodocyanopindolol; D008954:Models, Biological; D009206:Myocardium / Q000032:analysis; D010869:Pindolol / Q000031:analogs & derivatives / Q000378:metabolism; D011412:Propanolamines / Q000378:metabolism; D011869:Radioligand Assay; D011943:Receptors, Adrenergic, beta / Q000378:metabolism*; D014018:Tissue Distribution
chemical_list: D011412:Propanolamines; D011943:Receptors, Adrenergic, beta; C026777:ICI 118551; C011878:iodohydroxybenzylpindolol; D004082:Dihydroalprenolol; D020120:Iodocyanopindolol; D010869:Pindolol