TOPICS
Pharmaceutical Sciences
DATE

February  9, 2023

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February 9, 2023

Stimulation of α1L-adrenoceptor, atypical α1-adrenoceptor, activates store-operated Ca2+ channels and voltage-dependent Ca2+ channels

Dr. Keisuke Obara(left), Prof. Yoshio Tanaka(center),
Dr. Kento Yoshioka(right)
A research group led by Dr. Keisuke Obara, Dr. Kento Yoshioka, and Professor Yoshio Tanaka of the Department of Chemical Pharmacology, Faculty of Pharmaceutical Sciences, Toho University, found that contractions induced by phenylephrine (a nonselective α1-adrenoceptor agonist) in the guinea pig thoracic aorta could be triggered by stimulation of Gq protein-coupled α1L-adrenoceptor (atypical α1-adrenoceptor), followed by activation of store-operated Ca2+ channels (SOCCs) and voltage-dependent Ca2+ channels (VDCCs). These results suggest that 1) SOCC and/or VDCC inhibitors could suppress abnormal contractions in lower urinary and genital tissues such as prostate where α1L-adrenoceptors are abundantly expressed, and 2) these inhibitors could be the new therapeutic agents for lower urinary and genital diseases such as benign prostatic hyperplasia, in addition to α1-adrenoceptor antagonists. The results of this research were published in the journal “Biological and Pharmaceutical Bulletin” in February 2023.

Dr. Keisuke Obara(left), Prof. Yoshio Tanaka(center), Dr. Kento Yoshioka(right)

A research group led by Dr. Keisuke Obara, Dr. Kento Yoshioka, and Professor Yoshio Tanaka of the Department of Chemical Pharmacology, Faculty of Pharmaceutical Sciences, Toho University, found that contractions induced by phenylephrine (a nonselective α1-adrenoceptor agonist) in the guinea pig thoracic aorta could be triggered by stimulation of Gq protein-coupled α1L-adrenoceptor (atypical α1-adrenoceptor), followed by activation of store-operated Ca2+ channels (SOCCs) and voltage-dependent Ca2+ channels (VDCCs). These results suggest that 1) SOCC and/or VDCC inhibitors could suppress abnormal contractions in lower urinary and genital tissues such as prostate where α1L-adrenoceptors are abundantly expressed, and 2) these inhibitors could be the new therapeutic agents for lower urinary and genital diseases such as benign prostatic hyperplasia, in addition to α1-adrenoceptor antagonists. The results of this research were published in the journal “Biological and Pharmaceutical Bulletin” in February 2023.

A schematic summary of this study. Phenylephrine-induced contractions in the guinea pig thoracic aorta can be triggered by stimulation of Gq protein-coupled α1L-adrenoceptor (AR) (atypical α1-AR), followed by activation of store-operated Ca2+ channels (SOCCs) and voltage-dependent Ca2+ channels (VDCCs).

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