Displacement by .ALPHA.-adrenergic agonists and antagonists of 3H-prazosin bound to the .ALPHA.-adrenoceptors of the dog aorta and the rat brain.
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概要
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To characterize the α<SUB>1</SUB>-adrenoceptors in the dog aorta and the rat brain and to assess the antagonistic potencies of various chemicals inclusive of newly synthesized ones, radioligand binding assays were performed, and the potencies thus obtained were compared with those obtained from pharmacological observations. Reproducible binding to and displacement from the dog aorta of <SUP>3</SUP>H-prazosin were observed. The rank orders of the inhibition of <SUP>3</SUP>H-prazosin binding to the membrane preparations of the aorta expressed as IC50 (the concentration of drugs inhibiting 50% of maximal specific binding of <SUP>3</SUP>H-prazosin) were: prazosin > YM09538 > phentolamine > yohimbine > phenoxybenzamine > labetalol > S-596 > dibenamine > K-351 > propranolol > hydralazine > N-696 for α-blockers and I-epinephrine > clonidine > I-norepinephrine > phenylephrine > I-isoproterenol for agonists. IC50 values of phenoxybenzamine, labetalol, dibenamine and K-351 obtained in the brain preparations were higher than those obtained in the preparation of the aorta. There was a good correlation (r=0.90) between the IC50 values obtained in the dog aorta and in the rat brain, suggesting that the α<SUB>1</SUB>-adrenergic receptors in the dog aorta and the rat brain resemble each other. Good correlations (aorta, r=0.97 and brain, r=0.94) were also observed between IC50 values derived from the binding assay in the aorta or the brain and the pA<SUB>2</SUB> values obtained as regards to the contractile response of the rat aorta to phenylephrine. Thus, this method could be useful for the assessment of newly synthesized chemicals as α-adrenergic antagonists.
- 公益社団法人 日本薬理学会の論文
著者
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Imai Shoichi
Department Of Phamacology Niigata University School Of Medicine
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Nagatomo Takafumi
Department Of Pharmacology Faculty Of Pharmaceutical Sciences Niigata University Of Pharmacy And App
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Nakagawa Yoshito
Department Of Pharmacology Niigata University School Of Medicine
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Tsuchihashi Hiroshi
Department Of Pharmacology Niigata College Of Pharmacy
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NAKAHARA Hajime
Department of Pharmacology, Faculty of Pharmaceutical Sciences, Kyoto University
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SASAKI Setsuko
Department of Pharmacology, Niigata College of Pharmacy
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