α_<1B>-Adrenoceptor Subtype Mediating the Phenylephrine-Induced Contractile Response in Rabbit Corpus Cavernosum Penis

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概要

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• The α<SUB>1</SUB>-adrenoceptor subtype mediating contraction to phenylephrine in rabbit corpus cavernosum penis (CCP) was investigated using selective α<SUB>1</SUB>-adrenoceptor subtype antagonists. WB4101 ((2-(2, 6-dimethoxy-phenoxyethyl)-aminomethyl-l, 4-benzodioxane) hydrochloride), 5-methylurapidil and tamsulosin concentration-dependently produced a parallel rightward shift of the concentration-response curve to phenylephrine, yielding pK<SUB>B</SUB> values of 8.05, 7.59 and 9.21, respectively. The slopes of the Schild plots were not different from unity. These antagonists did not affect the maximum response to phenylephrine. Oxymetazoline (1 μM), which initially caused a small contraction, produced a parallel rightward shift of the concentration-response curve to phenylephrine with an apparent pK<SUB>B</SUB> value of 6.99. However, oxymetazoline seemed to act as a non-surmountable antagonist to the phenylephrine-induced contraction, reducing the maximum response by 71.1 %. Chloroethylclonidine (25 and 100 μM) produced a parallel rightward shift of the concentration-response curve to phenylephrine without altering the maximum response. These results show that the α<SUB>1</SUB>-adrenoceptor in rabbit CCP has a relatively low affinity for WB4101, 5-methylurapidil, tamsulosin and oxymetazoline and is sensitive to inactivation by chloroethylclonidine. It is suggested that the α<SUB>1</SUB>-adrenoceptor subtype mediating contraction to phenylephrine in rabbit CCP has the characteristics of the α<SUB>1B</SUB>-adrenoceptor subtype.

• 社団法人 日本薬理学会の論文
• 1996-08-01

著者

• UCHIYAMA Toshimitsu

  Departments of Pharmacology Faculty of Medicine, Toho University

• FURUKAWA Katsuo

  Department of Pharmacology, Faculty of Medicine, Toho University

• Chess-williams Russell

  Department Of Biomedical Science School Of Biological Sciences University Of Sheffield

• Chess-williams Russell

  Department Of Biomedical Science Faculty Of Medicine University Of Sheffield

• Furukawa Katsuo

  Department Of Pharmacology Faculty Of Medicine Toho University

• Furukawa Katsuo

  Department Of Pharmacology Toho University School Of Medicine

• Uchiyama Toshimitsu

  Department Of Pharmacology Faculty Of Medicine Toho University

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• α_-Adrenoceptor Subtype Mediating the Phenylephrine-Induced Contractile Response in Rabbit Corpus Cavernosum Penis

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