Heterogeneity of alpha-2 adrenergic receptors.

作者: David B. Bylund

DOI: 10.1016/0091-3057(85)90536-2

关键词:

摘要: Alpha adrenergic receptors are subdivided into alpha-1 and alpha-2 subtypes on the basis of their pharmacologic properties. An evaluation data from radioligand binding functional experiments indicates that classified as not a homogeneous group. The best example this heterogeneity is differences in properties rodent non-rodent mammalian species. Prazosin generally has high affinity for receptors, but low while oxymetazoline more potent at receptors. A definition receptor proposed with prazosin having lower (200-300 nM) alpha-2A higher (5-10 alpha-2B Using definition, human platelet appears to have only subtype, all neonatal rat lung subtype. brain roughly equal amounts -2B submandibular gland, about 85% alpha-2A. ability pharmacologically define putative should promote development additional subtype selective drugs which will increase our understanding pharmacology may provide new therapeutic approaches.

参考文章(55)
K P Minneman, A Hedberg, P B Molinoff, Comparison of beta adrenergic receptor subtypes in mammalian tissues. Journal of Pharmacology and Experimental Therapeutics. ,vol. 211, pp. 502- 508 ,(1979)
DB Bylund, JR Martinez, Postsynaptic localization of alpha 2-adrenergic receptors in rat submandibular gland The Journal of Neuroscience. ,vol. 1, pp. 1003- 1007 ,(1981) , 10.1523/JNEUROSCI.01-09-01003.1981
D B Bylund, S B Jones, J Latifpour, Characterization of [3H]yohimbine binding to putative alpha-2 adrenergic receptors in neonatal rat lung. Journal of Pharmacology and Experimental Therapeutics. ,vol. 223, pp. 606- 611 ,(1982)
D B Bylund, D J Feller, Comparison of alpha-2 adrenergic receptors and their regulation in rodent and porcine species. Journal of Pharmacology and Experimental Therapeutics. ,vol. 228, pp. 275- 282 ,(1984)
Peter Lasch, Karl H. Jakobs, Agonistic and antagonistic effects of various α-adrenergic agonists in human platelets Naunyn-schmiedebergs Archives of Pharmacology. ,vol. 306, pp. 119- 125 ,(1979) , 10.1007/BF00498981
Harvey J. Motulsky, Sanford J. Shattil, Paul A. Insel, Characterization of α2-adrenergic receptors on human platelets using [3H]yohimbine Biochemical and Biophysical Research Communications. ,vol. 97, pp. 1562- 1570 ,(1980) , 10.1016/S0006-291X(80)80044-1
J. Ricardo Martinez, David B. Bylund, Jean Camden, Characterization of autonomic receptors in the rat sublingual gland by biochemical and radioligand assays. Naunyn-schmiedebergs Archives of Pharmacology. ,vol. 318, pp. 313- 318 ,(1982) , 10.1007/BF00501171
Spencer Berthelsen, William A. Pettinger, A functional basis for classification of α-adrenergic receptors Life Sciences. ,vol. 21, pp. 595- 606 ,(1977) , 10.1016/0024-3205(77)90066-2