Comparison of α<SUB>1</SUB>-Adrenoceptors between Rat Brain and Spleen
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概要
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Scatchard analyses of <SUP>3</SUP>H-prazosin binding in rat brain membranes showed biphasic curves, which identified the presence of α<SUB>1High</SUB>- and α<SUB>1Low</SUB>-affinity sites. The α<SUB>1High</SUB>-affinity site was completely inhibited by 0.1 μM phenoxybenzamine. On the other hand, <SUP>3</SUP>H-prazosin binding in rat spleen membranes resulted in linear curves that were identical to the binding curve for the α<SUB>1High</SUB>-affinity site in the brain. The displacement potencies of α<SUB>1</SUB>-adrenergic antagonists were characterized by <SUP>3H</SUP>-prazosin binding to α<SUB>1High</SUB>-affinity sites in the rat spleen and brain and α<SUB>1Low</SUB>-affinity sites in the brain in the presence of 0.1 μM of phenoxybenzamine. The affinities of WB-4101, phenoxybenzamine, phentolamine, chlorpromazine, labetalol and nifedipine for brain α<SUB>1High</SUB>-affinity sites were significantly higher than those in the spleen. The affinities of most ligands for α<SUB>1Low</SUB>-affinity sites were significantly lower than those for both α<SUB>1High</SUB>-affinity sites in the brain and spleen, but chlorethylclonidine was significantly selective for α<SUB>1Low</SUB>-affinity sites, and bunazosin, dibenamine and 5HT had the same affinities for the α<SUB>1Low</SUB>- and both α<SUB>1High</SUB>-affinity sites. These results show that two α<SUB>1</SUB>-adrenoceptor subtypes, α<SUB>1High</SUB>- and α<SUB>1Low</SUB>-affinity, are present in the rat brain and that a different α<SUB>1High</SUB>-subtype, exists in the rat spleen.
著者
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Kinami Junji
Department Of Pharmacology Niigata College Of Pharmacy
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Nagatomo Takafumi
Department Of Pharmacology Faculty Of Pharmaceutical Sciences Niigata University Of Pharmacy And App
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Tsuchihashi Hiroshi
Department Of Pharmacology Niigata College Of Pharmacy
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Maruyama Keiko
Department Of Clinical Laboratory Science Kanazawa University Graduate School Kanazawa University
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Mano Fumie
Department of Pharmacology, Niigata College of Pharmacy
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Baba Shoko
Department of Pharmacology, Niigata College of Pharmacy
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