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The novel alpha-2 adrenergic radioligand [3H]-MK912 is alpha-2C selective among human alpha-2A, alpha-2B and alpha-2C adrenoceptors

Uhlén, S.; Porter, A.C.; Neubig, R.R.

Journal of Pharmacology and Experimental Therapeutics 271(3): 1558-1565

1994

ISSN/ISBN: 0022-3565
PMID: 7996470
Document Number: 430129
We have determined the binding affinities of the novel alpha-2 adrenoceptor antagonist radioligand [3H]-MK912 for the cloned human alpha-2A, alpha-2B and alpha-2C adrenoceptors. The KD-values were 1.25 nM, 1.36 nM and 0.086 nM for the alpha-2A, alpha-2B and alpha-2C subtypes, respectively. Thus, the selectivity of [3H]-MK912 for the human alpha-2C adrenoceptor vs. the human alpha-2A and alpha-2B adrenoceptors is 14-fold and 16-fold, respectively. The alpha-2C selectivity, and the very high affinity of [3H]-MK912 for the alpha-2C adrenoceptor subtype (KD = 86 pM) makes this radioligand a promising tool for studying the role of alpha-2C adrenoceptors in the human. A selection of antagonists useful for differentiating between the human alpha-2A, alpha-2B and alpha-2C adrenoceptor subtypes is discussed.

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Bakinovskiĭ, L.V.; Gomtsian, A.R.; Baĭramova, N.E.; Kochetkov, N.K. 1985: Synthesis of oligosaccharide fragments of O-specific polysaccharides of Shigella flexneri. III. Synthesis of the tetrasaccharide Glc alpha 1-3Rha alpha 1-2(Glc alpha 1-3)Rha alpha 1-OMe and the pentasaccharide GlcNAc beta 1-2(Glc alpha 1-3)Rha alpha 1-2(Glc alpha 1-3)Rha alpha 1-OMe Bioorganicheskaia Khimiia 11(5): 655-661
Clineschmidt, B.V.; Flataker, L.M.; Faison, E.P.; Haubrich, D.R. 1980: Alpha-methyldopa reduces locomotor activity in rats via its metabolite, alpha-methylnorepinephrine, acting on alpha 2-adrenoceptors Archives Internationales de Pharmacodynamie et de Therapie 244(2): 231-243
Smyth, D.D.; Umemura, S.; Pettinger, W.A. 1986: Alpha 1-adrenoceptor blockade and altered renal alpha 2-adrenoceptors: a model(?) for the study of genetically altered alpha 2-adrenoceptors in hypertensive rats Journal of Hypertension. Suppl: Official Journal of the International Society of Hypertension 4(3): S205-S208
Carcillo, J.A.; Litten, R.Z.; Suba, E.A.; Roth, B.L. 1988: Alterations in rat aortic alpha 1-adrenoceptors and alpha 1-adrenergic stimulated phosphoinositide hydrolysis in intraperitoneal sepsis Circulatory Shock 26(3): 331-339
Renouard, A.; Widdowson, P.S.; Millan, M.J. 1994: Multiple alpha 2 adrenergic receptor subtypes. I. Comparison of [3H]RX821002-labeled rat R alpha-2A adrenergic receptors in cerebral cortex to human H alpha2A adrenergic receptor and other populations of alpha-2 adrenergic subtypes Journal of Pharmacology and Experimental Therapeutics 270(3): 946-957
Udagawa, Y.; Armstrong, S.S.; Waites, G.T.; Bell, S.C.; Horne, C.H.; Thomson, A.W. 1985: Immunohistochemical localization of murine alpha 1-pregnancy-associated protein (alpha 1-PAP) in non-pregnant females: a comparative study with human pregnancy-associated alpha 2-glycoprotein (alpha 2-PAG) Clinical and Experimental Immunology 61(2): 397-405
Takeda, M.; Takagi, T. 1980: Effects of a new bronchodilator, (alpha RS)-3-formamido-4-hydroxy-alpha-[[[(alpha RS)-p-methoxy-alpha-methylphenethyl] amino] methyl] benzyl alcohol fumarate dihydrate (BD 40A) on gastric acid secretion and gastrointestinal motility Nihon Yakurigaku Zasshi. Folia Pharmacologica Japonica 76(3): 185-191
Bebök, Z.; Szekeres, G.; Horváth, G.; Duda, E.; Németh, P. 1993: Creation of monoclonal antibodies against tumor necrosis factor-alpha (TNF-alpha) and transforming growth factor alpha (TFG-alpha), their definition and possible use Orvosi Hetilap 134(24): 1303-1307
Jakobs, K.H. 1978: Synthetic alpha-adrenergic agonists are potent alpha-adrenergic blockers in human platelets Nature 274(5673): 819-820
Price, D.T.; Lefkowitz, R.J.; Caron, M.G.; Berkowitz, D.; Schwinn, D.A. 1994: Localization of mRNA for three distinct alpha 1-adrenergic receptor subtypes in human tissues: implications for human alpha-adrenergic physiology Molecular Pharmacology 45(2): 171-175
Trendelenburg, A.U.; Limberger, N.; Rump, L.C. 1994: Alpha 2-adrenergic receptors of the alpha 2c subtype mediate inhibition of norepinephrine release in human kidney cortex Molecular Pharmacology 45(6): 1168-1176
Hieble, J.P.; Sulpizio, A.C.; Nichols, A.J.; Willette, R.N.; Ruffolo, R.R. 1988: Pharmacologic characterization of SK&F 104078, a novel alpha-2 adrenoceptor antagonist which discriminates between pre- and postjunctional alpha-2 adrenoceptors Journal of Pharmacology and Experimental Therapeutics 247(2): 645-652
Robertson, I.G.; Guthenberg, C.; Mannervik, B.; Jernström, B. 1986: Differences in stereoselectivity and catalytic efficiency of three human glutathione transferases in the conjugation of glutathione with 7 beta,8 alpha-dihydroxy-9 alpha,10 alpha-oxy-7,8,9,10-tetrahydrobenzo(a)pyrene Cancer Research 46(5): 2220-2224
Tsvetkova, I.V.; Karpova, E.A.; Voznyĭ, I.V.; Zolotukhina, T.V.; Biriukov, V.B.; Semiachkina, A.N. 1991: Use of 4-methylumbelliferryl-alpha-L-iduronide and 4-trifluoromethylumbelliferryl-alpha-L-iduronide for detecting alpha-L-iduronidase deficiencies in human tissue and for rapid prenatal diagnosis of Hurler disease Voprosy Meditsinskoi Khimii 37(1): 74-77
Panse, P.; Zeiller, P.; Sensch, K.H. 1971: Absorption and effect of N-(alpha, alpha, alpha-trifluoro-m-tolyl)-anthranilic acid after cutaneous application Arzneimittel-Forschung 21(10): 1605-1608
Khalepo, A.I.; Lapina, L.M.; Popova, S.M.; Vorontsov, R.S. 1984: Determination of the maximum allowable concentration of alpha, alpha, alpha-trifluoro-4-chlorotoluene in the air of the work zone Gigiena Truda i Professional'nye Zabolevaniya (5): 49-51
Li, L.; Li, Z.H. 1990: X-ray diffraction studies on the configuration of 2 xi, 17 alpha-diethynyl-2 xi, 17 beta-dihydroxy-A-nor-5 alpha-androstane alpha-epimer Yao Xue Xue Bao 25(6): 435-437
Doi, M.; Ishida, T.; Polese, A.; Formaggio, F.; Crisma, M.; Toniolo, C.; Broxterman, Q.B.; Kamphuis, J. 1995: (S)-C alpha-ethyl, C alpha-benzylglycine [(S)-(alpha Et)Phe] peptides fold in left-handed helical structures Peptide Research 8(5): 294-297
Gomeza, J.; Mary, S.; Brabet, I.; Parmentier, M.L.; Restituito, S.; Bockaert, J.; Pin, J.P. 1996: Coupling of metabotropic glutamate receptors 2 and 4 to G alpha 15, G alpha 16, and chimeric G alpha q/i proteins: characterization of new antagonists Molecular Pharmacology 50(4): 923-930
O'Hara, C.M.; Tang, L.; Taussig, R.; Todd, R.D.; O'Malley, K.L. 1996: Dopamine D2L receptor couples to G alpha i2 and G alpha i3 but not G alpha i1, leading to the inhibition of adenylate cyclase in transfected cell lines Journal of Pharmacology and Experimental Therapeutics 278(1): 354-360