PT - JOURNAL ARTICLE AU - Masayuki Takeda AU - Kenji Obara AU - Takaki Mizusawa AU - Yoshihiko Tomita AU - Kei Arai AU - Toshiki Tsutsui AU - Akihiko Hatano AU - Kota Takahashi AU - Shintaro Nomura TI - Evidence for β<sub>3</sub>-Adrenoceptor Subtypes in Relaxation of the Human Urinary Bladder Detrusor: Analysis by Molecular Biological and Pharmacological Methods DP - 1999 Mar 01 TA - Journal of Pharmacology and Experimental Therapeutics PG - 1367--1373 VI - 288 IP - 3 4099 - http://jpet.aspetjournals.org/content/288/3/1367.short 4100 - http://jpet.aspetjournals.org/content/288/3/1367.full SO - J Pharmacol Exp Ther1999 Mar 01; 288 AB - The purpose of the present study was to confirm the presence of β3-adrenoceptor subtype in the relaxation of human urinary bladder detrusor tissue by reverse transcription-polymerase chain reaction (PCR); direct sequencing of the PCR product, in situ hybridization; and isometric contraction. Using reverse transcription-PCR, the mRNAs of three receptor subtypes (β1, β2, and β3) were expressed in the human urinary bladder detrusor tissue. Direct sequencing of the PCR product of the above β3-adrenoceptor revealed no mutation in the amplified regions. In situ hybridization with digoxygenin-labeled oligonucleotide probe revealed the presence of the mRNA of β3-adrenoceptor subtype in the smooth muscle of the urinary bladder. The relaxant effects of isoproterenol (a nonselective β-adrenoceptor agonist); ZD7114, BRL37344, and CGP12177A (putative selective β3-adrenoceptor agonists); and SR59230A (a putative selective β3-adrenoceptor antagonist) were tested using an isometric contraction technique. Isoproterenol in either the presence or absence of both atenolol (a β1-adrenoceptor-selective antagonist) and butoxamine (a β2-adrenoceptor-selective antagonist) revealed a relaxant effect on the carbachol-induced contraction of the human urinary bladder detrusor. Both BRL37344 and CGP12177A also revealed relaxant effects on the human urinary bladder detrusor, but ZD7114 did not elicit any relaxation. These results suggest that β3-adrenoceptor may have some role in urine storage in the human urinary bladder. The American Society for Pharmacology and Experimental Therapeutics