author_facet Nakamura, Seigo
Taniguchi, Takanobu
Suzuki, Fumiko
Akagi, Yoshio
Muramatsu, Ikunobu
Nakamura, Seigo
Taniguchi, Takanobu
Suzuki, Fumiko
Akagi, Yoshio
Muramatsu, Ikunobu
author Nakamura, Seigo
Taniguchi, Takanobu
Suzuki, Fumiko
Akagi, Yoshio
Muramatsu, Ikunobu
spellingShingle Nakamura, Seigo
Taniguchi, Takanobu
Suzuki, Fumiko
Akagi, Yoshio
Muramatsu, Ikunobu
British Journal of Pharmacology
Evaluation of α1‐adrenoceptors in the rabbit iris: pharmacological characterization and expression of mRNA
Pharmacology
author_sort nakamura, seigo
spelling Nakamura, Seigo Taniguchi, Takanobu Suzuki, Fumiko Akagi, Yoshio Muramatsu, Ikunobu 0007-1188 1476-5381 Wiley Pharmacology http://dx.doi.org/10.1038/sj.bjp.0702675 <jats:p> <jats:list list-type="explicit-label"> <jats:list-item><jats:p>Subtypes of α<jats:sub>1</jats:sub>‐adrenoceptor in rabbit iris have been examined in functional, binding and molecular biological experiments.</jats:p></jats:list-item> <jats:list-item><jats:p>In functional studies, exogenous and endogenous noradrenaline produced contractions of the iris dilator muscle. The contractile responses to noradrenaline were competitively antagonized by a range of α<jats:sub>1</jats:sub>‐adrenoceptor antagonists (pA<jats:sub>2</jats:sub> values): prazosin (8.1), WB4101 (8.2), BMY7378 (5.9), YM617 (9.5), JTH‐601 (8.8), HV723 (7.8) and KMD‐3213 (9.8). The same order of inhibitory potency was seen in the adrenergic responses to electrical stimulation. This affinity profile corresponds well to that of the putative α<jats:sub>1L</jats:sub>‐adrenoceptor, which has been proposed in lower urinary tract tissues.</jats:p></jats:list-item> <jats:list-item><jats:p>In binding studies on rabbit iris membrane however, prazosin, KMD‐3213 and WB4101 displayed high affinity (pK<jats:sub>d</jats:sub> or pK<jats:sub>i</jats:sub>: 9.6, 10.3, 9.6, respectively), and BMY7378 displayed low affinity (pK<jats:sub>i</jats:sub>: 6.9). These results show that the binding sites typically correspond to α<jats:sub>1A</jats:sub>‐adrenoceptor subtype in character, and we could not detect the significant amount of α<jats:sub>1L</jats:sub>‐adrenoceptor subtype.</jats:p></jats:list-item> <jats:list-item><jats:p>The expression of the three distinct mRNAs that encode proteins of α<jats:sub>1a</jats:sub>‐, α<jats:sub>1b</jats:sub>‐ and α<jats:sub>1d</jats:sub>‐adrenoceptors was studied using reverse transcription‐polymerase chain reaction (RT–PCR). RT–PCR demonstrated the strongest expression of the α<jats:sub>1a</jats:sub>‐adrenoceptor, weak expression of the α<jats:sub>1b</jats:sub>‐ adrenoceptor and undetectable expression of the α<jats:sub>1d</jats:sub>‐adrenoceptor.</jats:p></jats:list-item> <jats:list-item><jats:p>The present study suggests that α<jats:sub>1A</jats:sub>‐adrenoceptor is a major subtype detectable in binding and RT–PCR studies in rabbit iris, but that the adrenergic contractions of iris dilator muscle are mediated <jats:italic>via</jats:italic> activation of α<jats:sub>1</jats:sub>‐adrenoceptor subtype having low affinity for prazosin and WB4101.</jats:p></jats:list-item> </jats:list> </jats:p><jats:p><jats:italic>British Journal of Pharmacology</jats:italic> (1999) <jats:bold>127</jats:bold>, 1367–1374; doi:<jats:ext-link xmlns:xlink="http://www.w3.org/1999/xlink" ext-link-type="doi" xlink:href="10.1038/sj.bjp.0702675">10.1038/sj.bjp.0702675</jats:ext-link></jats:p> Evaluation of α<sub>1</sub>‐adrenoceptors in the rabbit iris: pharmacological characterization and expression of mRNA British Journal of Pharmacology
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series British Journal of Pharmacology
source_id 49
title Evaluation of α1‐adrenoceptors in the rabbit iris: pharmacological characterization and expression of mRNA
title_unstemmed Evaluation of α1‐adrenoceptors in the rabbit iris: pharmacological characterization and expression of mRNA
title_full Evaluation of α1‐adrenoceptors in the rabbit iris: pharmacological characterization and expression of mRNA
title_fullStr Evaluation of α1‐adrenoceptors in the rabbit iris: pharmacological characterization and expression of mRNA
title_full_unstemmed Evaluation of α1‐adrenoceptors in the rabbit iris: pharmacological characterization and expression of mRNA
title_short Evaluation of α1‐adrenoceptors in the rabbit iris: pharmacological characterization and expression of mRNA
title_sort evaluation of α<sub>1</sub>‐adrenoceptors in the rabbit iris: pharmacological characterization and expression of mrna
topic Pharmacology
url http://dx.doi.org/10.1038/sj.bjp.0702675
publishDate 1999
physical 1367-1374
description <jats:p> <jats:list list-type="explicit-label"> <jats:list-item><jats:p>Subtypes of α<jats:sub>1</jats:sub>‐adrenoceptor in rabbit iris have been examined in functional, binding and molecular biological experiments.</jats:p></jats:list-item> <jats:list-item><jats:p>In functional studies, exogenous and endogenous noradrenaline produced contractions of the iris dilator muscle. The contractile responses to noradrenaline were competitively antagonized by a range of α<jats:sub>1</jats:sub>‐adrenoceptor antagonists (pA<jats:sub>2</jats:sub> values): prazosin (8.1), WB4101 (8.2), BMY7378 (5.9), YM617 (9.5), JTH‐601 (8.8), HV723 (7.8) and KMD‐3213 (9.8). The same order of inhibitory potency was seen in the adrenergic responses to electrical stimulation. This affinity profile corresponds well to that of the putative α<jats:sub>1L</jats:sub>‐adrenoceptor, which has been proposed in lower urinary tract tissues.</jats:p></jats:list-item> <jats:list-item><jats:p>In binding studies on rabbit iris membrane however, prazosin, KMD‐3213 and WB4101 displayed high affinity (pK<jats:sub>d</jats:sub> or pK<jats:sub>i</jats:sub>: 9.6, 10.3, 9.6, respectively), and BMY7378 displayed low affinity (pK<jats:sub>i</jats:sub>: 6.9). These results show that the binding sites typically correspond to α<jats:sub>1A</jats:sub>‐adrenoceptor subtype in character, and we could not detect the significant amount of α<jats:sub>1L</jats:sub>‐adrenoceptor subtype.</jats:p></jats:list-item> <jats:list-item><jats:p>The expression of the three distinct mRNAs that encode proteins of α<jats:sub>1a</jats:sub>‐, α<jats:sub>1b</jats:sub>‐ and α<jats:sub>1d</jats:sub>‐adrenoceptors was studied using reverse transcription‐polymerase chain reaction (RT–PCR). RT–PCR demonstrated the strongest expression of the α<jats:sub>1a</jats:sub>‐adrenoceptor, weak expression of the α<jats:sub>1b</jats:sub>‐ adrenoceptor and undetectable expression of the α<jats:sub>1d</jats:sub>‐adrenoceptor.</jats:p></jats:list-item> <jats:list-item><jats:p>The present study suggests that α<jats:sub>1A</jats:sub>‐adrenoceptor is a major subtype detectable in binding and RT–PCR studies in rabbit iris, but that the adrenergic contractions of iris dilator muscle are mediated <jats:italic>via</jats:italic> activation of α<jats:sub>1</jats:sub>‐adrenoceptor subtype having low affinity for prazosin and WB4101.</jats:p></jats:list-item> </jats:list> </jats:p><jats:p><jats:italic>British Journal of Pharmacology</jats:italic> (1999) <jats:bold>127</jats:bold>, 1367–1374; doi:<jats:ext-link xmlns:xlink="http://www.w3.org/1999/xlink" ext-link-type="doi" xlink:href="10.1038/sj.bjp.0702675">10.1038/sj.bjp.0702675</jats:ext-link></jats:p>
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author Nakamura, Seigo, Taniguchi, Takanobu, Suzuki, Fumiko, Akagi, Yoshio, Muramatsu, Ikunobu
author_facet Nakamura, Seigo, Taniguchi, Takanobu, Suzuki, Fumiko, Akagi, Yoshio, Muramatsu, Ikunobu, Nakamura, Seigo, Taniguchi, Takanobu, Suzuki, Fumiko, Akagi, Yoshio, Muramatsu, Ikunobu
author_sort nakamura, seigo
container_issue 6
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container_title British Journal of Pharmacology
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description <jats:p> <jats:list list-type="explicit-label"> <jats:list-item><jats:p>Subtypes of α<jats:sub>1</jats:sub>‐adrenoceptor in rabbit iris have been examined in functional, binding and molecular biological experiments.</jats:p></jats:list-item> <jats:list-item><jats:p>In functional studies, exogenous and endogenous noradrenaline produced contractions of the iris dilator muscle. The contractile responses to noradrenaline were competitively antagonized by a range of α<jats:sub>1</jats:sub>‐adrenoceptor antagonists (pA<jats:sub>2</jats:sub> values): prazosin (8.1), WB4101 (8.2), BMY7378 (5.9), YM617 (9.5), JTH‐601 (8.8), HV723 (7.8) and KMD‐3213 (9.8). The same order of inhibitory potency was seen in the adrenergic responses to electrical stimulation. This affinity profile corresponds well to that of the putative α<jats:sub>1L</jats:sub>‐adrenoceptor, which has been proposed in lower urinary tract tissues.</jats:p></jats:list-item> <jats:list-item><jats:p>In binding studies on rabbit iris membrane however, prazosin, KMD‐3213 and WB4101 displayed high affinity (pK<jats:sub>d</jats:sub> or pK<jats:sub>i</jats:sub>: 9.6, 10.3, 9.6, respectively), and BMY7378 displayed low affinity (pK<jats:sub>i</jats:sub>: 6.9). These results show that the binding sites typically correspond to α<jats:sub>1A</jats:sub>‐adrenoceptor subtype in character, and we could not detect the significant amount of α<jats:sub>1L</jats:sub>‐adrenoceptor subtype.</jats:p></jats:list-item> <jats:list-item><jats:p>The expression of the three distinct mRNAs that encode proteins of α<jats:sub>1a</jats:sub>‐, α<jats:sub>1b</jats:sub>‐ and α<jats:sub>1d</jats:sub>‐adrenoceptors was studied using reverse transcription‐polymerase chain reaction (RT–PCR). RT–PCR demonstrated the strongest expression of the α<jats:sub>1a</jats:sub>‐adrenoceptor, weak expression of the α<jats:sub>1b</jats:sub>‐ adrenoceptor and undetectable expression of the α<jats:sub>1d</jats:sub>‐adrenoceptor.</jats:p></jats:list-item> <jats:list-item><jats:p>The present study suggests that α<jats:sub>1A</jats:sub>‐adrenoceptor is a major subtype detectable in binding and RT–PCR studies in rabbit iris, but that the adrenergic contractions of iris dilator muscle are mediated <jats:italic>via</jats:italic> activation of α<jats:sub>1</jats:sub>‐adrenoceptor subtype having low affinity for prazosin and WB4101.</jats:p></jats:list-item> </jats:list> </jats:p><jats:p><jats:italic>British Journal of Pharmacology</jats:italic> (1999) <jats:bold>127</jats:bold>, 1367–1374; doi:<jats:ext-link xmlns:xlink="http://www.w3.org/1999/xlink" ext-link-type="doi" xlink:href="10.1038/sj.bjp.0702675">10.1038/sj.bjp.0702675</jats:ext-link></jats:p>
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spelling Nakamura, Seigo Taniguchi, Takanobu Suzuki, Fumiko Akagi, Yoshio Muramatsu, Ikunobu 0007-1188 1476-5381 Wiley Pharmacology http://dx.doi.org/10.1038/sj.bjp.0702675 <jats:p> <jats:list list-type="explicit-label"> <jats:list-item><jats:p>Subtypes of α<jats:sub>1</jats:sub>‐adrenoceptor in rabbit iris have been examined in functional, binding and molecular biological experiments.</jats:p></jats:list-item> <jats:list-item><jats:p>In functional studies, exogenous and endogenous noradrenaline produced contractions of the iris dilator muscle. The contractile responses to noradrenaline were competitively antagonized by a range of α<jats:sub>1</jats:sub>‐adrenoceptor antagonists (pA<jats:sub>2</jats:sub> values): prazosin (8.1), WB4101 (8.2), BMY7378 (5.9), YM617 (9.5), JTH‐601 (8.8), HV723 (7.8) and KMD‐3213 (9.8). The same order of inhibitory potency was seen in the adrenergic responses to electrical stimulation. This affinity profile corresponds well to that of the putative α<jats:sub>1L</jats:sub>‐adrenoceptor, which has been proposed in lower urinary tract tissues.</jats:p></jats:list-item> <jats:list-item><jats:p>In binding studies on rabbit iris membrane however, prazosin, KMD‐3213 and WB4101 displayed high affinity (pK<jats:sub>d</jats:sub> or pK<jats:sub>i</jats:sub>: 9.6, 10.3, 9.6, respectively), and BMY7378 displayed low affinity (pK<jats:sub>i</jats:sub>: 6.9). These results show that the binding sites typically correspond to α<jats:sub>1A</jats:sub>‐adrenoceptor subtype in character, and we could not detect the significant amount of α<jats:sub>1L</jats:sub>‐adrenoceptor subtype.</jats:p></jats:list-item> <jats:list-item><jats:p>The expression of the three distinct mRNAs that encode proteins of α<jats:sub>1a</jats:sub>‐, α<jats:sub>1b</jats:sub>‐ and α<jats:sub>1d</jats:sub>‐adrenoceptors was studied using reverse transcription‐polymerase chain reaction (RT–PCR). RT–PCR demonstrated the strongest expression of the α<jats:sub>1a</jats:sub>‐adrenoceptor, weak expression of the α<jats:sub>1b</jats:sub>‐ adrenoceptor and undetectable expression of the α<jats:sub>1d</jats:sub>‐adrenoceptor.</jats:p></jats:list-item> <jats:list-item><jats:p>The present study suggests that α<jats:sub>1A</jats:sub>‐adrenoceptor is a major subtype detectable in binding and RT–PCR studies in rabbit iris, but that the adrenergic contractions of iris dilator muscle are mediated <jats:italic>via</jats:italic> activation of α<jats:sub>1</jats:sub>‐adrenoceptor subtype having low affinity for prazosin and WB4101.</jats:p></jats:list-item> </jats:list> </jats:p><jats:p><jats:italic>British Journal of Pharmacology</jats:italic> (1999) <jats:bold>127</jats:bold>, 1367–1374; doi:<jats:ext-link xmlns:xlink="http://www.w3.org/1999/xlink" ext-link-type="doi" xlink:href="10.1038/sj.bjp.0702675">10.1038/sj.bjp.0702675</jats:ext-link></jats:p> Evaluation of α<sub>1</sub>‐adrenoceptors in the rabbit iris: pharmacological characterization and expression of mRNA British Journal of Pharmacology
spellingShingle Nakamura, Seigo, Taniguchi, Takanobu, Suzuki, Fumiko, Akagi, Yoshio, Muramatsu, Ikunobu, British Journal of Pharmacology, Evaluation of α1‐adrenoceptors in the rabbit iris: pharmacological characterization and expression of mRNA, Pharmacology
title Evaluation of α1‐adrenoceptors in the rabbit iris: pharmacological characterization and expression of mRNA
title_full Evaluation of α1‐adrenoceptors in the rabbit iris: pharmacological characterization and expression of mRNA
title_fullStr Evaluation of α1‐adrenoceptors in the rabbit iris: pharmacological characterization and expression of mRNA
title_full_unstemmed Evaluation of α1‐adrenoceptors in the rabbit iris: pharmacological characterization and expression of mRNA
title_short Evaluation of α1‐adrenoceptors in the rabbit iris: pharmacological characterization and expression of mRNA
title_sort evaluation of α<sub>1</sub>‐adrenoceptors in the rabbit iris: pharmacological characterization and expression of mrna
title_unstemmed Evaluation of α1‐adrenoceptors in the rabbit iris: pharmacological characterization and expression of mRNA
topic Pharmacology
url http://dx.doi.org/10.1038/sj.bjp.0702675